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Kinase Selectivity 

Selective Small Molecule Kinase Inhibitors

Eli Wallace, Ph.D., Director, Medicinal Chemistry, Array BioPharma

Challenges and Opportunities with Kinase Inhibitor Selectivity

Peter Brandt, Ph.D., Senior Scientist, Beactica AB

14-3-3 Proteins Capture the Signaling Signatures of Hormones and Kinase Inhibitors

Carol MacKintosh, Ph.D., MRC Protein Phosphorylation Unit, College of Life Sciences, James Black Center, University of Dundee


From Allosteric & Covalent Inhibitors
to Targeting Inactive Kinases

Exploiting Activation-State Dependent Conformational Differences
in Protein Kinases for Inhibitor Design and Optimization

Mark Ashwell, Ph.D., Vice President, Medicinal Chemistry, ArQule, Inc.



Selectivity & Kinases Today

  • How much selectivity is enough? 
  • How is selectivity being assessed? 
  • Differing results from in vitro and in cells-based screens 
  • Novel screening formats to assess selectivity 


Neil Wishart, Ph.D., Associate Director, Abbott 

KINASE BIO: Over 10 years of experience leading multiple kinase programs from early hit-to-lead through to candidate status.  Successfully navigated a number of kinase-related pitfalls on multiple classes of kinase targets (serine/threonine, tyrosine, pseudo and PI3 kinases) for Oncology and Immunology indications. 

Daniel Goldberg, Ph.D., Senior Principal Scientist, Boehringer-Ingelheim Pharmaceuticals 

KINASE BIO: Over 12 years of drug discovery experience, many spent in the field of kinase research.  My focus has been on both autoimmune and cardiovascular disease targets from hit-to-lead through candidate selection.  I have worked to balance the desired kinase selectivity through structure-based approaches while being vigilant on maintaining desired drug like properties.  

Isabelle Dussault, Ph.D., Director, Oncology Research, Amgen 

KINASE BIO: Cancer Biologist, Team Leader and Director of multiple kinase programs. Experience spans from target identification to clinical candidate identification and early clinical development. 


Structure-Based Kinase Inhibitor
Design & Kinase Selectivity

*Shared session with Structure-Based Drug Design Conference 

Discovery of Crizotinib (PF-02341066): A c-Met/ALK Dual Inhibitor for Oncology Applications

Jean Cui, Ph.D., Associate Research Fellow, Oncology Medicinal Chemistry, Pfizer, Inc.

A Role for Hydration in Interleukin-2 Inducible T Cell Kinase Selectivity

Ronald Knegtel, Ph.D., Research Fellow I, Molecular Modeling, Vertex Pharmaceuticals (Europe) Ltd.

How Molecular Dynamics Simulation May be Applied in Structural Based Design of Kinase Drugs

Yibing Shan, Ph.D., Senior Scientist, Chemistry and Biology, D. E. Shaw Research

Overcoming Drug-Resistant Mutations in Kinase Drug Discovery: Applying Lessons from Ponatinib (AP24534)

David C. Dalgarno, Ph.D., Vice President, Research Technologies, ARIAD Pharmaceuticals Inc.



Structure-Based Kinase Inhibitor Design

Andrew C. Good, Ph.D., Scientific Director, Medicinal Chemistry, Genzyme Corp. 

KINASE BIO: Highly experienced computational chemist involved in 3 projects that have brought compounds to the clinic. Exposure to multiple kinase projects at GlaxoWellcome, Bristol-Myers Squibb and Genzyme. Currently leading primary Genzyme kinase oncology project, shepherding the program from hit id through to late stage lead optimization. 

Ravi G. Kurumbail, Ph.D., Research Fellow and Structural Biology Laboratory Head, Pfizer, Inc. 

KINASE BIO: Experience in structure-based drug design in over half a dozen kinase projects in the pharmaceutical industry; contributed to the development of clinical candidates; experience in evaluation of kinase inhibitors for CNS indications; championed a kinase project for Alzheimer’s disease; trained as a protein X-ray crystallographer; currently leading a structural biology lab at Pfizer. 

Dirksen Bussiere, Ph.D., M.B.A., Director, Structural Chemistry, Novartis Institutes for BioMedical Research 

KINASE BIO:  Fifteen years experience in structure-based drug design, including more than ten projects targeting kinases for diabetes and cancer, several of which led to compounds currently in development; trained in protein biochemistry, biophysics, structural biology, and computational chemistry/biology; currently leading a structural biology group at Novartis. 

John D. Haley, Ph.D., Senior Research Director, Translational Research,OSI Pharmaceuticals 


Resistance in Next Gen Kinase Inhibitors 

Resistance to Kinase Inhibitors: Mechanisms, Challenges and Opportunities

Isabelle Dussault, Ph.D., Director, Oncology Research, Amgen


Novel Targets 

The Published Kinase Inhibitor Set: A Pre-competitive Strategy to Develop Probes for the Untargeted KinomeDavid H. Drewry, Ph.D., Director, Department of Chemical Biology, GlaxoSmithKline 


Kinases in Oncology – Hot Targets 

Targeting Kinases Outside the ATP Pocket

Doriano M. Fabbro, Ph.D., Senior Unit Head Expertise Platform
Kinases, Novartis Institutes for BioMedical Research

Next Generation ALK Inhibitors and Personalized Medicine - The Next Frontier of Kinase Drug Discovery

Chris Liang, Ph.D., CSO & Executive Vice President, Xcovery, LLC

Bone Morphogenetic Protein Receptor Kinase Inhibitors

Paul Yu, M.D., Ph.D., Assistant Professor, Medicine, Massachusetts General Hospital


Kinase Inhibitors in Inflammation & Autoimmune 

Bruton’s Tyrosine Kinase from Bench to Bedside: Covalently Silencing B Cells with AVL-292

Juswinder Singh, Ph.D., Founder and CSO, Avila Therapeutics, Inc.

Application of Functional Screening Using Cultured Human Mast Cells for the Discovery and Optimization of SYK Kinase Inhibitors Leading to Fostamatinib

Rajinder Singh, Ph.D., Head, Medicinal Chemistry, Rigel Pharmaceuticals, Inc.


Kinases for CNS Indications 

Highly Selective Brain-Penetrant Inhibitors of Glycogen Synthase Kinase 3-β for Alzheimer’s Disease

Ravi G. Kurumbail, Ph.D., Research Fellow and Structural Biology Laboratory Head, Pfizer, Inc.

Elucidating the Role of LRRK2 in Parkinson’s Disease

Greg Cuny, Ph.D., Assistant Professor, Neurology, Brigham & Women’s Hospital


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