37th National Medicinal Chemistry Symposium

American Chemical Society
Division of Medicinal Chemistry

 New York City, NY, United States    June 28-July 1, 2020

Session 1: Integrating Novel Chemical Modalities in Hit-to-lead: a New Paradigm for Early Drug Discovery

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

Dr Susan ASHWELL
Dr Susan ASHWELL
RA PHARMA, Cambridge, United States
Read more

Impact of Structure Based Drug Design in GPCR Lead Optimisation Strategies

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

Translating RNA Sequence into Lead Small Molecule Medicines

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

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

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

Title of talk to be confirmed

Dr Nello MAINOLFI
Dr Nello MAINOLFI
KYMERA THERAPEUTICS, Cambridge, United States

Integrating DNA-Encoded Library Technologies in Lead Discovery

Dr Lisa MARCAURELLE
Dr Lisa MARCAURELLE
GSK, Cambridge, United States
Read more

Session 2: New Directions in Targeting DNA Damage Repair (DDR)

Discovery and Optimization of Novel PARG Inhibitors

Dr Hilary BECK
Dr Hilary BECK
IDEAYA BIOSCIENCES, South San Francisco, United States
Read more

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

Dr Charlene FALLAN
Dr Charlene FALLAN
ASTRAZENECA, Cambridge, United Kingdom
Read more

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

Dr Robert HEALD
Dr Robert HEALD
ARTIOS PHARMA LTD, Cambridge, United Kingdom
Read more

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
Dr Ulrich LÜCKING
BAYER HEALTHCARE, Berlin, Germany
Read more

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

Assoc. Prof. Phil REIGAN
Assoc. Prof. Phil REIGAN
UNIVERSITY OF COLORADO, Aurora, United States
Read more

Session 3: Hot Targets from NYC Academic and Biotech Scene

Designing and Combining Cancer's Off Switches

Dr Karen AKINSANYA
Dr Karen AKINSANYA
SCHRODINGER, New York City, United States
Read more

Rational Design of Inhibitors of Protein-Protein Interactions

Prof. Paramjit ARORA
Prof. Paramjit ARORA
NYU, New York, United States
Read more

Next Generation Drug Discovery

Dr Steve COLLETTI
Dr Steve COLLETTI
LODO THERAPEUTICS, New York, United States
Read more

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

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

Therapeutic Potential of the Gut-Brain Axis

Dr Ann WEBER
Dr Ann WEBER
KALLYOPE, New York, United States
Read more

Session 4: Targeting Autophagy for Cancer, Neurodegeneration, or Autoimmune Disease

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

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

Chemical Activation of Chaperone-Mediated Autophagy for Protection against Neurodegeneration

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

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

Dr Nicholas HERTZ
Dr Nicholas HERTZ
MITOKININ, New York, United States
Read more

Bcl-2 Regulation of Beclin 1-Dependent Autophagy in Health and Disease

Prof. Beth LEVINE
Prof. Beth LEVINE
UT SOUTHWESTERN MEDICAL CENTER, Dallas, United States
Read more

Unraveling Autophagy in Cancer Using Chemical Genetics

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

Title of talk to be confirmed

Dr Jenny VIKLUND
Dr Jenny VIKLUND
SPRINT BIOSCIENCE, Huddinge, Sweden

Session 5: “If At First You Don’t Succeed, Try, Try, Try Again”:
How Clinical Failures Propelled Next Generation Candidates

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

Dr Robert AVERSA
Dr Robert AVERSA
NOVARTIS, Cambridge, United States
Read more

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

Dr Chris BURGEY
Dr Chris BURGEY
MERCK & CO., INC., Rahway, United States
Read more

LPA1 Receptor Antagonists for the Treatment of IPF

Dr Peter CHENG
Dr Peter CHENG
BRISTOL-MYERS SQUIBB, New York, United States

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
Dr David GRIFFITH
PFIZER, New York, United States
Read more

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

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

Evolution of Clinical PI3K Inhibitors at Genentech

Dr Steve STABEN
Dr Steve STABEN
GENENTECH, South San Francisco, United States
Read more

Session 6: Lessons from Drug Hunters across Academia, NPOs and the Pharmaceutical Industry

Discovery of Novel Drug Regimens for the Treatment of Tuberculosis

Dr Christopher B. COOPER
Dr Christopher B. COOPER
TB ALLIANCE, New York, United States
Read more

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

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

Discovery of mGlu4 PAMs for the Treatment of Neurological Diseases

Prof. Craig LINDSLEY
Prof. Craig LINDSLEY
VANDERBILT UNIVERSITY, Nashville, United States

DSM265, a Dihydroorotate Dehydrogenase Inhibitor for the Treatment of Malaria

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

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

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

Delivering Innovative Medicines: Small Changes can have a Large Effect

Dr Wendy YOUNG
Dr Wendy YOUNG
GENENTECH, South San Francisco, United States
Read more