37th ACS National Medicinal Chemistry Symposium

Discovery and Development of Macrocyclic Peptides for the Treatment of Complement-Mediated Disorders

Dr Susan ASHWELL

RA PHARMA, Cambridge, United States
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Dr Susan ASHWELL

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Vice President, Chemistry, Ra Pharmaceuticals

Prior to joining Ra Pharmaceuticals, Sue was a Senior Director at FORMA Therapeutics in Watertown. Previously she was a Director in the Boston-based Oncology group of AstraZeneca where she had multiple roles including line and project leadership. Before AZ, she was a medicinal chemist with Wyeth-Ayerst Research in the CNS area. During her career she has been involved with a number of programs that have resulted in clinical candidates in the Oncology, CNS disorders and Inflammation therapeutic areas. Sue received her Ph.D. the University of Newcastle upon Tyne, prior to conducting postdoctoral research at the University of Illinois at Chicago and Imperial College, London.

Impact of Structure Based Drug Design in GPCR Lead Optimisation Strategies

Dr Miles CONGREVE

SOSEI HEPTARES, Welwyn Garden City, United Kingdom
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Dr Miles CONGREVE

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Senior Vice President, Head of Drug Discovery

Miles Congreve is Senior Vice President, Head of Drug Discovery at Sosei Heptares, having previously held leadership positions at Astex Therapeutics and GSK. At Heptares Miles leads a group of ~60 scientists and is responsible for delivery of the company’s drug discovery pipeline. Miles has a background in structure and fragment-based drug design, participating in the discovery of several agents including Erdafitinib (Balversa), Lanabecestat, Vofopitant and Onalespib and is a co-inventor of the marketed drug Ribociclib (Kisquali). Miles obtained a BSc in biological chemistry from Leicester University and a PhD in synthetic chemistry from Cambridge University. Miles is co-author of over 150 publications and patents. In 2015 Miles was co-recipient of the RSC Malcolm Campbell Memorial Prize for the seminal contributions to GPCR drug discovery made by Sosei Heptares.

Translating RNA Sequence into Lead Small Molecule Medicines

Prof. Matthew DISNEY

SCRIPPS RESEARCH INSTITUTE, Jupiter, United States
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Prof. Matthew DISNEY

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Matt Disney is a Professor in the Departments of Chemistry and Neuroscience at The Scripps Research Institute’s Florida campus. For the past 12 years, his research efforts have been focused exclusively on developing approaches to drug RNA with small molecules. He has pioneered synergistic computational and experimental approaches to tackle this difficult molecular recognition problem by developing Inforna, an approach that identifies druggable RNAs and small molecules to target them via sequence-based design. He has also developed target validation approaches that allow one to identify target RNAs and binding sites within them by crosslinking small molecule RNAs in cells. These approaches have been broadly leveraged to target RNAs in many disease settings. Prof. Disney’s professional accolades include the NIH Director’s Pioneer Award, the Tetrahedron Young Investigator Award, and the Raymond and Beverly Sackler International Prize in the Physical Sciences, among numerous other awards.

Structural Approach to Identify Lead Scaffolds for Protein-Protein Interaction Targets

Prof. Kyle HADDEN

UNIVERSITY OF CONNECTICUT, Storrs, United States
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Prof. Kyle HADDEN

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Professor Hadden received his BS in Chemistry from Wofford College in 2000 and his Ph.D. in Medicinal Chemistry from the Medical University of South Carolina in 2004. During postdoctoral studies at the University of Kansas, he worked on developing small molecule Hsp90 inhibitors as anti-cancer chemotherapeutics. Professor Hadden started his independent career in the Department of Pharmaceutical Sciences in the School of Pharmacy at the University of Connecticut in 2009. The overall research focus in the Hadden lab is to utilize a medicinal chemistry/chemical biology approach to understand the mechanisms through which dysregulation of cellular signaling contributes to the onset of human cancer and apply this knowledge to develop improved therapeutics. Major ongoing projects include the development of hedgehog pathway modulators as therapeutic agents and the identification and development of small molecule inhibitors of translesion synthesis.

Protein Degradation beyond Oncology

Dr Nello MAINOLFI

KYMERA THERAPEUTICS, Cambridge, United States
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Dr Nello MAINOLFI

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Founder, President & Chief Executive Officer

Nello started his drug discovery career at the Novartis Institutes for Biomedical Research, leading teams to identify multiple novel potential medicines that have entered clinical development across a series of disease areas. Notably he led the team that discovered and developed the first complement factor B inhibitor now in late clinical development across a range of indications. Before founding Kymera, Mainolfi was an Entrepreneur in Residence at Atlas Venture and had previously led discovery research at cancer metabolism startup Raze Therapeutics. Nello has authored >60 papers and patents and has written reviews in the areas of medicinal chemistry, drug discovery and protein degradation. Nello was trained at Imperial College, University of London and The Scripps Research Institute in California.

Integrating DNA-Encoded Library Technologies in Lead Discovery

Dr Lisa MARCAURELLE

GSK, Cambridge, United States
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Dr Lisa MARCAURELLE

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Dr Lisa Marcaurelle is Director of Chemistry at GlaxoSmithKline in Cambridge, MA where she leads the DNA-Encoded Library Chemistry platform, focused on library synthesis and lead discovery. Prior to joining GSK in 2018, Lisa worked at various Cambridge-based biotech companies including Warp Drive Bio (Sr. Director, Chemistry 2016-2018), H3 Biomedicine (VP, Discovery Chemistry, 2011-2016) and Infinity Pharmaceuticals (Lead Sr. Scientist, 2002-2007). Lisa also spent some time in academia working at the Broad Institute (Director, Chemistry, 2007-2011) where she led the creation of the Broad’s diversity-oriented (DOS) screening collection. Lisa is an active member of the American Chemical Society. She is the 2020 Chair of the Division of Organic Chemistry, past-chair (2019) of the National Organic Chemistry Symposium and a Councilor for the Northeastern Section of the ACS. Lisa obtained a Ph.D. in Chemistry in 2001 from UC Berkeley working with Carolyn Bertozzi and did post-doctoral work at MIT with Peter Seeberger (2001-2002). She received her undergraduate degree in Chemistry from the College of the Holy Cross in Worcester, MA.

Discovery and Optimization of Novel PARG Inhibitors

Dr Hilary BECK

IDEAYA BIOSCIENCES, SOUTH SAN FRANCISCO, United States
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Dr Hilary BECK

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Hilary is currently a Director of Medicinal Chemistry at IDEAYA where her teams are discovering drugs targeting several DNA damage repair pathways. Previously, Hilary was Principal Investigator at Flexus and FLX Biosciences, serving pivotal roles in the discovery of linrodostat, FLX475 and RPT193. Hilary began her industrial career at Amgen in South San Francisco, where she made major contribution to multiple clinical candidates including AMG-232. Hilary received her B.A. from Boston University and holds a Ph. D. is Organic Synthesis from the University of Texas at Austin. She was also an American Cancer Society post-doctoral fellow at the University of North Carolina at Chapel Hill. She is the author of over 15 peer-reviewed publications and an inventor on over 15 patents.

Discovery of Potent and Selective DNA-PK Inhibitors via Structure-Guided Virtual Screening Strategies

Dr Charlene FALLAN

ASTRAZENECA, Cambridge, United Kingdom
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Dr Charlene FALLAN

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Charlene Fallan joined AstraZeneca in 2016 as a medicinal chemist within the Oncology R&D group, Cambridge, UK. Born in Scotland, Charlene obtained her PhD from the University of Edinburgh, under the supervision of Professor Hon Wai Lam in the field of asymmetric catalysis. Following her PhD she undertook a Post-Doctoral research position in St Andrews with Professor Andrew Smith, developing organocatalysis methodologies. Since joining AstraZeneca, Charlene’s work has focussed on kinase inhibitor programmes as well as projects aiming to target hormone nuclear receptors, to deliver new cancer therapies to patients.

M3541 and M4076: Discovery and Optimization of Potent and Selective ATM Kinase Inhibitors with Strong Anti-tumor Efficacy in Combination Therapies

Dr Thomas FUCHSS

MERCK KGAA - MERCK BIOPHARMA, Darmstadt, Germany
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Dr Thomas FUCHSS

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Thomas Fuchss is a Director within Global Medicinal Chemistry at Merck Biopharma, Merck KGaA, Darmstadt, Germany. Thomas received his diploma in Chemistry from Universität Konstanz, Konstanz, Germany, and his doctorate with honours in 1999 on the synthesis of functionalized carbon and sulfur glycosides of nojirimycin and N-acetyl glucosamine including glycoside hydrolase inhibitors and C-glycopeptides. During his initial industrial research at ALTANA AG, Thomas established a novel, safe and cost-effective synthetic access to the reversible, gastrointestinal proton-pump inhibitor soraprazan.

Thomas joined Merck KGaA in 2007 after having various roles at ALTANA as well as the ALTANA Research Institute in Waltham, Massachusetts, USA, where he worked on inflammation, respiration and oncology. Following assignments in Medicinal Chemistry on topics in metabolic disorders and osteoarthritis, Thomas, as Principal Scientist and Project Leader, identified and promoted several kinase inhibitors of different oncology targets that undergo clinical development in the field of DNA damage and repair, in particular DNA protein kinase inhibitor peposertib (formerly M3814) and ataxia telangiectasia mutated kinase inhibitor M3541. Additionally, Thomas leads the Research Pharmaceutics Processing Group within Discovery and Development Technologies in Biopharma’s Global R&D. He is the author of more than 45 publications and patent applications.

Discovery of DNA Polymerase theta (Polθ) Inhibitors: HTS to in vitro Probes

Dr Robert HEALD

ARTIOS PHARMA LTD, Cambridge, United Kingdom
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Dr Robert HEALD

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Rob Heald obtained a degree in chemistry and PhD with Prof. Malcolm Stevens from the University of Nottingham in the UK before completing post-doctoral studies at the University of Arizona Cancer Center with Prof. Laurence Hurley. Following his return to the UK he held various positions at Argenta Discovery (latterly Charles River) over a 13-year period working on a broad range of drug discovery projects but focussing on respiratory, inflammation and oncology. A highlight over this period was his participation in a 10-year collaboration with Genentech on projects which delivered multiple clinical candidates including the PI3kinase portfolio members GDC-0084, GDC-0032 and GDC-0077. He has now been at Artios Pharma for 3 years where he is Head of Chemistry leading teams and projects targeting the DNA damage response for the treatment of cancer.

Damage Incorporated: Discovery of ATR Inhibitor BAY 1895344 with Favorable PK Properties and Promising Anti-Tumor Efficacy in Monotherapy and Combination in Preclinical Tumor Models

Dr Ulrich LÜCKING

BAYER AG, Berlin, Germany
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Dr Ulrich LÜCKING

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Ulrich Lücking is a project team leader and principal scientist at Bayer AG in Berlin.

He started his industrial career in 2001 at the former Schering AG, working across multiple therapeutic areas, mainly in lead optimization, to successfully deliver multiple clinical candidates. His efforts were e.g. instrumental in the discovery of clinical candidates in the CDK inhibitor projects, the Androgen Receptor Suppressor project, the PTEFb inhibitor projects and the ATR inhibitor project. Moreover, he has a longstanding interest in neglected sulfur (VI) pharmacophores and macrocyclic compounds in drug discovery.

Prior to joining industry, he studied chemistry at the University of Hannover. As an Erasmus student and later for his master thesis, he spent time in the laboratory of Prof. Steven V. Ley. In 1999 he completed his Ph.D. under the direction of Prof. Andreas Pfaltz, and then carried out postdoctoral work in the laboratories of Prof. Julius Rebek.

The Modification of Pyrazolopyrimidinones and their Effect on WEE1 Inhibition and the DNA Damage Response

Prof. Phil REIGAN

UNIVERSITY OF COLORADO, Aurora, United States
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Prof. Phil REIGAN

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Dr Reigan completed his BSc in Chemistry at the University of Manchester in 1997. He then worked as an organic chemist at Oxford Asymmetry International/Evotec and Bayer Pharmaceuticals. He obtained his MSc in Pharmacology in 2000 and PhD developing small molecule inhibitors of thymidine phosphorylase in 2004 with Dr Sally Freeman at the University of Manchester. From 2004 to 2007 Dr Reigan performed post-doctoral research supporting the development of indolequinones as anticancer agents in Professor David Ross’ lab at the University of Colorado. Dr Reigan then worked as a consultant advising mid-to-large client pharmaceutical companies on their drug pipelines. In 2011 Dr Reigan returned to the University of Colorado as an Assistant Professor of Medicinal Chemistry and was promoted to Associate Professor in 2018. Dr Reigan also serves as the Director of Computational Chemistry and Biology core facility that supports drug discovery and development on the Anschutz Medical Campus. Dr Reigan has published over 50 peer-reviewed publications and has 6 patents. His current research focuses on the development of small molecules targeting adaptive proteins in cancer specifically those involved in DNA damage response and metabolic reprogramming which is funded by NIH, foundation, and innovation grants.

Designing and Combining Cancer's Off Switches

Dr Karen AKINSANYA

SCHRODINGER, New York City, United States
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Dr Karen AKINSANYA

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Karen Akinsanya has served as Chief Biomedical Scientist at Schrödinger since 2018. She has more than 25 years of experience spanning academia and pharmaceutical R&D. Prior to joining Schrödinger, Karen held positions of increasing responsibility at Merck Research Labs since 2005 in clinical pharmacology, therapeutic area leadership, and business development. She also served in a number of drug discovery roles in the US and the United Kingdom with Ferring Pharmaceutical starting in 1996. Karen received her Ph.D. from the Royal Postgraduate Medical School at Imperial College in London and completed post-doctoral training at Imperial and the Ludwig Institute for Cancer Research (UCL).

Rational Design of Inhibitors of Protein-Protein Interactions

Prof. Paramjit ARORA

NYU, New York, United States
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Prof. Paramjit ARORA

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Paramjit Arora obtained his B.S. in Chemistry from UC Berkeley and his earliest research experience synthesizing fluorescent dyes for the sequencing of the human genome. He received his Ph.D. degree in Organic Chemistry from UC Irvine and pursued an American Cancer Society Postdoctoral Fellowship at Caltech before joining the faculty of NYU in 2002. He is interested in using the principles of organic chemistry to miniaturize proteins with overall goal of creating a new class of synthetic therapeutics.

Next Generation Drug Discovery

Dr Steve COLLETTI

LODO THERAPEUTICS, New York, United States
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Dr Steve COLLETTI

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Senior Vice President, Research & Development

Dr Steve Colletti joined Lodo Therapeutics in 2018 as SVP and Head of R&D. Prior to Lodo, he was Executive Director and Head of Therapeutic Modalities at Merck, with 24 years of experience and leadership in small molecule, natural products, oligonucleotide, peptide, and fusion protein drug discovery – targeting cardiovascular and respiratory disease, diabetes and obesity, immunological disorders, infectious diseases, neuroscience, and oncology. Dr Colletti built and led the RNA Therapeutics Med Chem Department, and he was a core member of multiple development teams that were responsible for discovering more than a dozen preclinical candidate molecules and advancing them toward clinical development. His responsibilities also included working closely with licensing and business development, evaluating external opportunities, and helping to manage acquisitions. Dr Colletti is an inventor, author and co-author of over 125 publications and patents. He completed his BS degree at Loyola University Chicago, received his PhD in Chemistry from Boston University, and was an NIH Postdoctoral Research Fellow in Chemistry at the Scripps Research Institute.

Optimization of Mycobacterium Tuberculosis (Mtb) Selective Inhibitors of Lipoamide Dehydrogenase (Lpd)

Dr John GINN

TRI-INSTITUTIONAL THERAPEUTICS DISCOVERY INSTITUTE, New York, United States
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Dr John GINN

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Dr Ginn received a Bachelor of Science in Chemistry from Mercer University in Macon, Georgia. Subsequently, he attended Emory University in Atlanta, Georgia where he earned a Master’s degree studying titanocene mediated reductive cyclizations under the supervision of Professor William Crowe. He then completed his doctoral studies with Professor Albert Padwa developing intramolecular Diels-Alder cyclization of amino-thio-furans for generating the tricyclic core structure common to several classes of natural products. In 2001, Dr Ginn joined the Medicinal Chemistry department of Boehringer-Ingelheim Pharmaceuticals in Ridgefield, Connecticut where he focused on projects covering inflammatory, cardiovascular, and renal diseases. In 2017, he joined the Tri-Institutional Therapeutics Discovery Institute, in New York City as a Director of Chemistry where he leads projects as part of Tri-TDI’s mission to support the identification and development of small molecule and biologic therapeutics at its three affiliated academic institutions: Memorial Sloan Kettering, The Rockefeller University and Weill Cornell Medical College.

Therapeutic Potential of the Gut-Brain Axis

Dr Ann WEBER

KALLYOPE, New York, United States
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Dr Ann WEBER

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Ann E. Weber, Ph.D., is Senior Vice President – Drug Discovery at Kallyope Inc., a New York City-based biotechnology company focused on harnessing the potential of the gut-brain axis. In this role she is responsible for translating opportunities arising from the company’s state-of the-art technology platform into drug discovery and development programs. She was formerly Vice President – Lead Optimization Chemistry at Merck Research Laboratories (MRL), responsible for the discovery of innovative therapeutic agents across disease areas. She joined MRL as a Senior Research Chemist in 1987.

Dr Weber’s research interests include the design and synthesis of ligands for G-protein coupled receptors, ion channels and enzymes. Her work has led to over 40 development candidates, including JANUVIA® (sitagliptin), a treatment for patients with Type 2 diabetes (T2DM), JANUMET®, a fixed dose combination of sitagliptin and metformin, and MARIZEV® (omarigliptin), a once-weekly treatment for T2DM approved in Japan. An additional therapeutic agent, BEOVA® (vibegron) for the treatment of overactive bladder, was approved in Japan in September 2018 and is in late stage clinical trials in the US.

Dr Weber is the author or co-author of over 90 publications. She is co-inventor on over 35 issued US patents. Her awards include the Robert M. Scarborough Award for Excellence in Medicinal Chemistry (American Chemistry Society (ACS)), the Heroes of Chemistry Award (ACS), the Discoverer's Award (PhRMA), recognizing scientists whose work has been of special benefit to humankind, and a Directors’ Award, the highest honor that Merck confers on its employees. She is a 2013 Liberty Science Center Women in STEM Honoree and the recipient of the 2015 Gift of Mentoring Award from the Metro Women Chemists Committee. In 2016 she was named to the Medicinal Chemistry Hall of Fame (ACS). She was the 2017 recipient of the Perkin Medal (Society of Chemical Industry American Section), considered the highest honor given in the US chemical industry. She received the 2018 ACS Award for Creativity in Molecular Design and Synthesis. In 2019 she was named a Fellow of the American Chemical Society.

Dr Weber is passionate about advancing women in chemistry and is a member of the ACS Women Chemists Committee. She also serves on the TB Alliance Scientific Advisory Committee and the University of Notre Dame College of Science Advisory Council.

Before joining Merck, Dr Weber obtained her B.S. degree in chemistry summa cum laude from the University of Notre Dame. She earned her PhD degree from Harvard University, studying synthetic organic chemistry in the laboratories of Professor David A. Evans.

The Development of Substrate Competitive and Allosteric Inhibitors of Cysteine Protease ATG4B to Prevent Autophagic Flux

Dr Jason CROSS

MD ANDERSON CANCER CENTER, Houston, United States
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Dr Jason CROSS

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Jason B. Cross is Institute Group Leader for Structural Chemistry in the Institute for Applied Cancer Science (IACS) at the University of Texas MD Anderson Cancer Center. He received his B.Sc. in biochemistry from the University of Windsor and his Ph.D. in physical chemistry from Wayne State University, where he worked with H. Bernhard Schlegel. Following a post-doctoral fellowship under the direction of Lakshmi Narasimhan at Pfizer, which focused on the development surface area-based scoring functions, Dr Cross joined Affinium Pharmaceuticals in 2004 where he served as team leader for a collaborative antibacterial drug discovery project with Pfizer and co-led the implementation of an X-ray crystallography-based fragment screening platform. He joined Wyeth Pharmaceuticals in 2006, where he led a cross-site initiative to standardize virtual screening workflows, deployed ADME models to medicinal chemists’ desktops, and designed a focused compound library for nuclear receptor screening. In 2009, Dr Cross became Head of Molecular Modeling at Cubist Pharmaceuticals, where he managed computational chemistry and structural bioinformatics resources. While at Cubist, he co-led an exploratory research team focused on therapies for acute pain and chemotherapy induced peripheral neuropathy, and co-invented CB-618, a novel, broad spectrum beta-lactamase inhibitor that advanced to the clinic. Since 2015, Dr Cross has coordinated the application of computational chemistry, structural biology, biophysics, and fragment screening techniques to oncology and neurodegeneration drug discovery projects at IACS. Dr Cross has authored or co-authored 23 research papers, 3 book chapters, 14 issued patents, and 2 revisions of the GAUSSIAN quantum chemistry package (GAUSSIAN 03 and GAUSSIAN 09), and is a member of the American Chemical Society.

Title of talk to be confirmed

Dr Peter FULLER

MERCK & CO. INC., Boston, United States

Chemical Activation of Chaperone-Mediated Autophagy for Protection against Neurodegeneration

Prof. Evripidis GAVATHIOTIS

ALBERT EINSTEIN COLLEGE OF MEDICINE, Bronx, United States
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Prof. Evripidis GAVATHIOTIS

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Evripidis (Evris) Gavathiotis, Ph.D. is a Professor of Biochemistry and Medicine at Albert Einstein College of Medicine and faculty member of the Albert Einstein Cancer Center, the Institute for Aging Research, and the Wilf Family Cardiovascular Research Institute. He received his Ph.D. in biological chemistry from the University of Nottingham. He performed postdoctoral research at Rockefeller University and at Dana-Farber Cancer Institute and he was junior faculty at Harvard Medical School. He started his lab at Einstein in 2011 as assistant professor and he was promoted to full professor in 2019. His research focuses on mechanisms and protein interactions in cell death and cell survival signaling and the discovery and optimization of small molecule modulators towards novel chemical tools and therapeutics. His work has pioneered structural and mechanistic insights of BCL-2 family proteins and other key proteins. He has discovered first-in-class small molecules for several “undruggable” targets and demonstrated novel pharmacological strategies. His laboratory’s research has contributed to the founding of three biotechnology companies (Stelexis Therapeutics, Selphagy Therapeutics, Aspida Therapeutics) that are advancing novel therapeutics for cancer and aging-associated diseases. Dr. Gavathiotis has received numerous awards including an Sidney Kimmel Scholar Award, the 2014 Young Chemical Biologist Award, the 2015 Pershing Square Sohn Prize, an AHA Collaborative Science Award, a Irma T. Hirschl Career Scientist Award, an BioAccelerate NYC Prize and the Julius Marmur Mentorship Award. He has served on numerous NIH study sections and review panels in chemical biology and drug discovery. He is a member of the American Chemical Society, the American Society for Biochemistry and Molecular Biology and the American Association for Cancer Research.

Activating PTEN-Induced Kinase 1 (PINK1) for Parkinson’s Disease

Dr Nicholas HERTZ

MITOKININ INC, San Francisco, United States
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Dr Nicholas HERTZ

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Dr Hertz’s graduate research with Kevan Shokat provided the foundation for Mitokinin’s PINK1 program. Dr Hertz leads a team of 12 scientists and research associates, along with 8 FTEs at CRO partners, pushing Mitokinin’s science and therapeutics forward. He has authored over 18 publications in journals such as Cell, Neuron and Nature. Dr Hertz has been an invited speaker at international conferences including the Michael J. Fox Parkinson’s Disease Therapeutics Conference in 2018 and holds several patents.

Dr Hertz received his Ph.D in Chemistry and Chemical Biology from UCSF with a Genentech graduate fellowship in the labs of Kevan Shokat and Al Burlingame. Following his Ph.D, he completed his post-doctoral training in neuroscience as a Helen Hay Whitney fellow in the lab of Marc Tessier-Lavigne at Stanford University. He graduated magna cum laude and Phi Beta Kappa from UCLA with a B.S. in Biochemistry.

Unraveling Autophagy in Cancer Using Chemical Genetics

Prof. Jeff MACKEIGAN

MICHIGAN STATE UNIVERSITY, East Lansing, United States
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Prof. Jeff MACKEIGAN

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Dr Jeff MacKeigan is a Professor of Cancer Biology and Complex Diseases in the College of Human Medicine at Michigan State University. Dr MacKeigan also serves as Assistant Dean for Research in the College of Human Medicine. He earned his B.A. from the University of Colorado and his Ph.D. in Microbiology and Immunology at the University of North Carolina Comprehensive Cancer Center. His postdoctoral research in the Department of Cell Biology at Harvard Medical School was immediately followed by a position as project leader at Novartis Institutes for Biomedical Research in Cambridge, Massachusetts. Dr MacKeigan joined the faculty at the Van Andel Research Institute as an Assistant Professor; he was promoted to Associate Professor; and joined Michigan State University as a Professor in 2017. His lab seeks a systems-level understanding of cancer biology and cell signaling networks that encompass autophagy, the mTOR pathway and cancer metabolism. Their research involves a variety of cutting-edge technologies, and they use their tumor biology expertise and pathway knowledge to study complex diseases. All of their research projects have one common goal – to identify novel therapeutic targets.

Discovery of Highly Potent and Selective Vacuolar Protein Sorting 34 (Vps34) Inhibitors

Dr Jenny VIKLUND

SPRINT BIOSCIENCE AB, Huddinge, Sweden
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Dr Jenny VIKLUND

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Director Protein Science and Drug Design at Sprint Bioscience (Stockholm, Sweden)

Chemistry project leader for the Vps34 project, from fragment hit to in vivo PoC. Responsible for development of the Sprint Bioscience fragment screening platform, as well as enabling and driving drug design and data analysis.

Prior to joining Sprint Bioscience, ten years as a computational chemist at AstraZeneca, Sweden. Contributing to two CNS programs producing candidates that are now in clinical trials.

Education: Master of Science in Molecular Biotechnology, Uppsala, Sweden.

3 Generations of RAF Inhibitors – Learnings and Improvements Based on Clinical Data

Dr Robert AVERSA

NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Cambridge, United States
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Dr Robert AVERSA

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Robert Aversa was born in Philadelphia, PA and did his undergraduate studies at Cornell University, studying biochemistry and chemistry. He obtained a PhD in organic chemistry from The Scripps Research Institute in La Jolla, CA, performing research in natural product synthesis under the tutelage of Prof. K.C. Nicolaou. He has been a Research Investigator in the Global Discovery Chemistry group at the Novartis Institutes for BioMedical Research since 2011, first in Emeryville, CA and currently in Cambridge, MA. During this time, he has worked in the therapeutic areas of oncology, immuno-oncology, hearing loss, chronic kidney diseases, and chronic liver diseases spanning drug discovery phases from target elucidation to optimization and delivery of clinical candidates, including B/CRAF inhibitor NVP-LXH254. He has been recognized with a Roche Excellence in Chemistry award in 2010 from his PhD research and an ACS Young Investigator’s award in 2016.

Discovery of Oral CGRP Receptor Antagonists for the Treatment of Migraine: Learning from (Clinical) Experience

Dr Christopher BURGEY

MERCK & CO., INC., West Point, United States
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Dr Christopher BURGEY

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Christopher Burgey is currently a Director in the Discovery Chemistry department at Merck (West Point, PA). Over the course of a 20+ year career, he has been involved in research programs spanning a range of diseases areas, including: HIV, neuropathic pain, migraine, Alzheimer’s disease, and osteoporosis. Chris has led multiple chemistry, project, and early clinical development teams and several drug candidates have progressed to late-stage clinical development; notably, these include the novel CGRP receptor antagonists telcagepant and ubrogepant, which proceeded to Phase 3 registration studies for the treatment of migraine. Additionally, he has had broad scientific management experience, including leading recruiting efforts for Global Chemistry. Chris earned a B.S. from Bucknell University, a Ph.D. from Duke University (Burroughs Wellcome Fund Fellow) and performed postdoctoral research at Harvard University (American Cancer Society Fellowship).

LPA1 Receptor Antagonists for the Treatment of IPF

Dr Peter CHENG

BRISTOL-MYERS SQUIBB R & D, Hopewell, United States
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Dr Peter CHENG

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Peter Cheng received his B.Sc. and Ph.D. from the University of Toronto (NSERC pre-doctoral fellowship), carried out postdoctoral research at the University of Rochester (NSERC post-doctoral fellowship) and then joined Bristol-Myers Squibb, where he is currently a Director in the Fibrosis Chemistry Department. At BMS, Peter has led multiple medicinal chemistry programs in the Metabolic and Fibrosis Disease therapeutic areas encompassing diverse targets (nuclear hormone receptors, GPCRs and kinases). These efforts have resulted in the discovery of multiple advanced clinical compounds, including the PPARα/γ dual agonists muraglitazar (Pargluva; completed Phase 3 clinical trials) and peliglitazar (completed Phase 2b clinical trials) for the treatment of type 2 diabetes. Most recently, his group’s work in the Fibrosis area has resulted in the discovery of the LPA1 antagonist BMS-986278, which is currently in clinical trials.

Leveraging the Human PK of PF-06882961, an Oral Small Molecule GLP-1R Agonists, in the Discovery of a 2nd Generation Candidate

Dr David GRIFFITH

PFIZER INC., Cambridge, United States
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Dr David GRIFFITH

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David received his undergraduate degree from Harvey Mudd College and his PhD in Chemistry from Yale University in the laboratory of Professor Sam Danishefsky. Following postdoctoral studies at the University of California, Berkeley, with Professor Clayton Heathcock, he joined Pfizer in 1995. There he has led Medicinal Chemistry efforts and broader Project Teams against targets for Obesity, Osteoporosis, and Diabetes resulting in multiple candidates advanced for clinical testing including the Ph3 CB-1 antagonist Otenabant and the Ph2 GLP-1R agonist PF-06882961. He is an author on more than 46 publications and is an inventor on 40 patents.

Discovery of Risdiplam, a Selective SMN2 Gene Splicing Modifier for the Treatment of Spinal Muscular Atrophy

Dr Hasane RATNI

F. HOFFMANN-LA ROCHE LTD, Basel, Switzerland
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Dr Hasane RATNI

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Dr H. Ratni is an Expert Scientist, Medicinal Chemistry, at F. Hoffmann-La Roche Ltd., Basel, Switzerland.

He received his PhD at the University of Geneva and did a post-doc at Tokyo University before joining F. Hoffmann-La Roche Ltd in 2001. His research has mainly been devoted to the areas of neuroscience (e.g. V1a receptor antagonist now in human clinical trials, phase 3, for autism). In 2005, he participated in a secondment within the Roche group at Chugai Pharmaceutical Co. Ltd, Gotemba Japan. He was the chemistry discovery project leader of the SMN program aiming for a treatment for spinal muscular atrophy, which led to the discovery of Risdiplam (awaiting FDA approval). His current focus is on gamma secretase modulator for Alzheimer disease.

He is an author or co-author of more than 115 patents and publications and received the following awards:
- 2014: Roche Leo Sternbach Award for Innovation in Chemistry
- 2016: Gold medal at the Roche Patent Inventor’s recognition event
- 2019: Paper of the year award by the Society of Toxicology (DDTSS)
- 2020: Roche CEO Award for Excellence
- 2020: Senior Industrial Science Award by the Swiss Chemical Society (SCS)

Evolution of Clinical PI3K Inhibitors at Genentech

Dr Steve STABEN

GENENTECH, South San Francisco, United States
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Dr Steve STABEN

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Steve received his BS in Chemistry from Western Washington University in 2002. He joined Dean Toste's lab at UC Berkeley pursuing doctoral research directed at new reaction development and natural product synthesis. He started as a medicinal chemist in the Discovery Chemistry group at Genentech in 2007, where he is currently an Associate Director. At Genentech, Steve has contributed to a number of projects across immunology, cancer immunology and oncology.

Discovery of Novel Drug Regimens for the Treatment of Tuberculosis

Dr Christopher B. COOPER

TB ALLIANCE, GLOBAL ALLIANCE FOR TB DRUG DEVELOPMENT, New York, United States
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Dr Christopher B. COOPER

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Christopher B. (Chris) Cooper joined the TB Alliance in January 2009, as Director of Chemistry. Chris received his BS (magna cum laude) in Chemistry from Clemson University in 1980, and his MS in Organic Chemistry at Stanford University with Professor Carl Djerassi in 1982. Following a two-year industry sabbatical at CIBA-Geigy Pharmaceuticals, he returned to Stanford in 1984 to earn his Ph.D. in Organic Chemistry with Professor Paul A. Wender. From 1988 through 1998, Dr. Cooper was engaged in medicinal chemistry research at Pfizer, Inc., in both their Groton, Connecticut, and Sandwich, England, laboratories. His areas of investigation included veterinary and human drug discovery programs (infectious disease, inflammation, immunology, oncology, and neuroscience), as well as applications of automated synthesis technologies for both lead generation and lead optimization purposes.

Dr Cooper joined Bristol-Myers Squibb, Inc., in Princeton, New Jersey, in 1998 to launch the Lead Synthesis Group directing the design, development, and synthesis of novel, drug-like medicinal chemistry arrays. His research team at BMS was directly responsible for the rapid pharmacological assessment of exploratory biological targets of interest, and the advancement of early- and full-phase discovery programs through hit-to-lead, lead optimization, and pre-development candidate selection medicinal chemistry approaches.

As Senior Director of Chemistry at the TB Alliance, Chris is responsible for all lead identification, lead optimization, preclinical, and clinical candidate chemistry efforts including medicinal chemistry, process chemistry, and cGMP drug substance manufacturing activities across the Alliance’s research and development portfolio. He currently oversees ~60 medicinal chemistry, analytical chemistry, process chemistry, and GMP manufacture FTE’s at 15 combined universities, biopharma, contract research organizations (CRO’s), and contract manufacturing organizations (CMO’s) for the advancement of ~25 discovery/preclinical/clinical programs. Dr. Cooper is the author of over 70 publications and is the inventor on twenty approved US and international (WO) patents.

Discovery of Upadacitinib: a Tricyclic Janus Kinase 1 (JAK1) Inhibitor

Dr Kristine E. FRANK

ABBVIE, North Chicago, United States
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Dr Kristine E. FRANK

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Kristine Frank received a B.S. in pharmacy from The Ohio State University (1993) and a PhD in medicinal chemistry from the University of Kansas (1998) working with Professors Lester A. Mitscher and Jeffrey Aubé. She began her industrial career at Pharmacia & Upjohn (Kalamazoo, MI) working on GPCRs for CNS indications. In 2003, Kristine moved to Abbott Bioresearch Center (Worcester, MA) to work predominantly on kinases in immunology. During this time, she was a co-inventor of Rinvoq® (upadacitinib), a Jak1 inhibitor. Kristine then transferred to the hit-to-lead group in Abbott (Abbott Park, IL) to pursue her passion for working in the early discovery space. Now in AbbVie’s centralized medicinal chemistry group, she balances efforts on early projects along with chemistry leadership for a lead optimization project and mentoring as much as time allows.

DSM265, a Dihydroorotate Dehydrogenase Inhibitor for the Treatment of Malaria

Prof. Meg PHILLIPS

UNIVERSITY OF TEXAS SOUTHWESTERN MED CENTER, Dallas, United States
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Prof. Meg PHILLIPS

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Margaret A. Phillips was born in Cleveland, Ohio in 1959. She received her undergraduate degree in Biochemistry from the University of California, Davis (1981) and her PhD in Pharmaceutical Chemistry from the University of California, San Francisco (1988), where she was also a postdoctoral fellow in the Dept. of Biochemistry (1988-1992).

Dr Phillips is currently Professor and Chair of the Department of Biochemistry at UT Southwestern, where her research focuses on biochemistry and drug discovery in parasitic protozoa.

Discovery of the Selective Allosteric TYK2 Inhibitor BMS-986165 for the Treatment of Autoimmune Diseases

Dr Steve WROBLESKI

BRISTOL-MYERS SQUIBB, Princeton, United States
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Dr Steve WROBLESKI

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After obtaining a doctorate in synthetic organic chemistry from the University of Rochester and completing an NIH postdoctoral fellowship under Prof. Barry Trost at Stanford University, Steve joined Bristol-Myers Squibb in 1999 where he is currently working as a Senior Principal Scientist in the Discovery Chemistry group. While at BMS, he successfully contributed to the advancement of multiple discovery programs and clinical drug candidates while building an expertise in kinase inhibitors and structure-guided drug design.

Delivering Innovative Medicines: Small Changes can have a Large Effect

Dr Wendy YOUNG

GENENTECH, South San Francisco, United States
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Dr Wendy YOUNG

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Wendy B. Young, Ph.D. is Senior Vice President of Small Molecule Drug Discovery at Genentech in San Francisco, CA.

In this role she leads an internal team of over 380 internal scientists that invent, discover and develop new medicines for patients. Wendy is a chemist by training and has over 25 years of experience leading research and drug discovery teams. She led the team and is co-inventor of fenebrutinib, a Bruton tyrosine Kinase (btk) inhibitor, which is currently in clinical trials for several immunology indications. Wendy received a B.A./M.S. degree in chemistry under Huw Davies at Wake Forest University, a Ph.D. from Princeton University in 1993 under the guidance of E.C. Taylor, and thereafter was a postdoctoral fellow at MSKCC with Samuel Danishefsky. Prior to Genentech, Wendy led discovery efforts at Axys/Celera for 10 years. In 2015, Wendy was recognized by the San Francisco Business Times as one of San Francisco Bay Area’s “Most Influential Business Women of 2015.” In 2017, Wendy was elected and served as the Chair of the National ACS Medicinal Chemistry Division, in 2018 was an ACS Fellows Awardee and in 2020 will be awarded the National ACS Earle B. Barnes award for Leadership in Chemical Research Management.

2020 IUPAC-Richter Prize Lecture
How I Spent my Summer Vacation: Insights from a 30-year Career in Drug Discovery (and Molecules that have Broken my Heart)

Dr John E. MACOR

SANOFI, Waltham, United States
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Dr John E. MACOR

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https://www.acsmedchem.org/?nd=Macor

John Macor earned his B.S. degree from the University of Notre Dame in 1982 doing undergraduate research with Professor Marvin Miller, and earned his Ph.D. degree at Princeton University with Professor E. C. Taylor in 1986. John then joined Pfizer where he was engaged in a variety of CNS drug discovery efforts, moved to Astra Arcus in 1994 focusing on cholinergic drug discovery, and then moved to Bristol-Myers Squibb in 1997, starting in cardiovascular and moving to neuroscience in 2001 and immunosciences in 2013. He assumed the role as Executive Director of Neuroscience Discovery Chemistry in 2002 and Executive Director of Immunosciences Discovery Chemistry in 2013. In 2016, he accepted the role as Global Head of Integrated Drug Discovery for Sanofi with groups in Paris, Frankfurt and Waltham, MA.

John is a co-inventor of Relpax® (eletriptan), an anti-migraine agent during his time at Pfizer. At Astra he was co-inventor of AZD0328, an α7 neuronal nicotinic receptor agonist, which advanced to Phase 2 trials for schizophrenia. At BMS, he was a co-inventor of BMS-346567 (sparsentan, a dual AT1/ETA receptor antagonist presently in Phase 3 clinical trials for focal segmental glomerulosclerosis), BMS-708163 (avagecestat, a γ-secretase inhibitor for Alzheimer’s Disease that reached Phase 2), and BMS-927711 (rimegepant), a CGRP receptor antagonist for the treatment of migraine awaiting NDA submission. Dr. Macor is also a co-inventor of LX9211 (AAK1 inhibitor, neuropathic pain) and BHV-3500 (CGRP antagonist, migraine), both presently in Phase 1.

John has authored/co-authored over 190 peer-reviewed publications, is an inventor on more than 115 issued US patents, and given more than 100 invited lectures. Dr. Macor chaired the 2002 Gordon Research Conference on Medicinal Chemistry and the 2006 Gordon Research Conference on Heterocyclic Compounds. Dr. Macor served as Editor-in-Chief of Annual Reports in Medicinal Chemistry for Volumes 42 – 46 (2006 – 2011). John was awarded the 2009 Scarborough Award in Medicinal Chemistry, and was made an American Society Fellow in 2011. Dr. Macor served as Chair of the Medicinal Chemistry Division (MEDI) of the American Chemical Society in 2015 and served a total of ten years on the Executive Committee of MEDI in various roles. Dr. Macor was awarded the 2014 Alfred Burger Award in Medicinal Chemistry (a National Award from the ACS) and was inducted into the Medicinal Chemistry Hall of Fame in 2014. Most recently he was designated as the 2019 Smissman awardee from the MEDI Division of the ACS “given to a living scientist whose research, teaching or service has had a substantial impact on the intellectual and theoretical development of the field of Medicinal Chemistry.”

2020 Division of Medicinal Chemistry Award Lecture
Title of Talk to be confirmed

Prof. Shaomeng WANG

UNIVERSITY OF MICHIGAN, Ann Arbor, United States