The human kinome is a very large and druggable class of targets with many disease indications. Thus, the kinome targets account for a significant portion of drug discovery efforts. Kinase inhibitor discovery is a very active area as developers explore more deeply into designing immune-modulatory agents as single or combination therapies, tackling chronic disease indications such as inflammation and CNS disorders as well as effectively harnessing allosteric modulators and covalently binding compounds. This year we'll also be discussing PROTACS and the role of artificial intelligence in kinase inhibitor discovery.
EMERGING CHALLENGES AND OPPORTUNITIES
KEYNOTE PRESENTATION: Kinase Inhibitor Drug Discovery – Challenges and Opportunities for the Next Decade
Bayard R. Huck, PhD, Vice President, Global Head of Medicinal Chemistry, Discovery Technologies, Global Research & Development, Merck
Targeting Human Pseudokinases with Kinase Inhibitors
Patrick Eyers, PhD, Professor, Cell Signaling, Biochemistry, University of Liverpool
Targeted Therapy in Patients with PIK3CA-Related Overgrowth Syndrome
Guillaume Canaud, MD, PhD, Professor of Medicine, Hôpital Necker Enfants Malades, Paris
APPROVED, IN-CLINIC AND ADVANCED INHIBITORS
Medicinal Chemistry Discovery of BLU-667, a Potent RET Inhibitor
Chris De Savi, PhD, Head of Chemistry, Blueprint Medicines
Targeting PI3K-gamma with IPI-549, a Tumor Macrophage-Reprogramming Small Molecule, in Patients with Advanced Solid Tumors
Jeffery L. Kutok, MD, PhD, CSO, Infinity Pharmaceuticals, Inc.
Acalabrutinib – Case Study of a Discovery of a Covalent BTK Inhibitor
Allard Kaptein, PhD, Executive Vice President – Discovery, Acerta Pharma
PROTACs AND PROTEIN DEGRADERS
Orally Active IRAK4 Degraders for Oncology and Autoimmune Diseases
Nello Mainolfi, PhD, Founder and CSO, Kymera Therapeutics, Inc.
Targeted Protein Degradation for Treatment of Cancer
Michael Plewe, PhD, Vice President, Medicinal Chemistry, Cullgen Inc.
Structure-Based Design of Degraders
Radoslaw Novak, PhD, Scientist, Laboratory of Dr. Eric Fischer, Department of Cancer Biology, Dana-Farber Cancer Institute, Harvard Medical School
* The program is subject to change without notice, due to unforeseen reason.