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KIT 09

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Recommended Short Course*

12:00 pm - 3:00 pm Targeting GPCRs and Ion Channels with Antibodies (SC2)

*Separate Registration Required



12:30 pm Registration

2:00 Chairperson’s Opening Remarks


2:10 Keynote Presentation

Stauber_ASafety and Toxicology Challenges on the Way to a Kinase Inhibitor Drug Development

Anja J. Stauber, Ph.D., DABT, Research Advisor, Cancer/Endocrine Safety Assessment, Eli Lilly and Company

A decade ago, kinase inhibitors held great promise for treating unmet medical needs by specifically targeting key regulators of pathways involved in disease while avoiding unwanted side effects.  While targeting kinase pathways still hold great promise, challenges exist in developing kinase inhibitors with toxicity profiles that support clinical trials.  The focus of this discussion will be on safety and toxicology challenges experienced in kinase inhibitor drug development.

Development – Lessons Learned

2:40 Developing a Novel Checkpoint Kinase Inhibitor

Sonya Zabludoff, Ph.D. Associate Director, Cancer Bioscience, AstraZeneca R&D

3:10 Aurora A Inhibitor MLN8237: From Discovery to Development

Jeff Ecsedy, Ph.D., Senior Scientist, Moleculor and Cellular Oncology, Millennium, The Takeda Oncology Corporation

3:40 Networking Refreshment Break in the Exhibit Hall

4:20 Title to be Announced

Peter A. Petillo, Ph.D., Senior Vice President, Deciphera Pharmaceuticals, LLC

Improving Efficacy

ProQinase4:50 Comparison of in vitro and Cellular IC50 Inhibitory Profiles of 7 Clinical Kinase Inhibitors on 16 Oncologically Relevant Kinases

Jan E. Ehlert, Ph.D., Group Leader, Drug Development, ProQinase

For efficient development of kinase inhibitors, cellular phosphorylation assays are becoming increasingly important. Although these assays have the drawback of relatively low throughput and high complexity, they are considered to be less artificial and to reflect the in vivo situation more closely. To evaluate the informative value of cellular phosphorylation assays, we have determined cellular IC50 values for clinical kinase inhibitors Lapatinib, Tozasertib (VX-680), Sorafenib, Sunitinib, Erlotinib, Gefitinib and Vatalanib in parallel on 16 oncologically relevant kinases involved in proliferation, angiogenesis, survival or metastasis. Comparison of cellular IC50 values with in vitro IC50 values determined at different ATP concentrations reveals striking differences for some but not all compounds, supporting the necessity of cellular analyses. Data will be discussed and compared with cellular and in vitro data from literature.

5:20 Identifying Allosteric Modulators of Pyruvate Kinase Orthologs with Quantitative High-throughput Screening

Douglas Auld, Ph.D., Group Leader, NIH Chemical Genomics, National Institute of Health/NHGRI

This talk will illustrate how we identified allosteric modulators of pyruvate kinase orthologs from human, parasitic and bacterial species. The NIH Chemical Genomics Center (NCGC) employs a process called “quantitative HTS” (qHTS) which greatly improves the quality of information that can be derived from HTS by experimentally determining pharmacological parameters such as potency and efficacy on collections of compounds as large as 300K in size. The use of qHTS to define the SAR of both activators and inhibitors of pyruvate kinases will be shown. The compounds identified have given insights into the allosteric regulation of pyruvate kinase and have provided both anti-cancer and anti-parasitic leads.

5:50 Radiosensitize Human Cancer Cells by an scFv against the DNA-Dependent Protein Kinase

Shuyi Li, M.D., Ph.D., Research Scientist, Program in Cancer Biology and Gene Regulation, Institute of Molecular Medicine and Genetics, Medical College of Georgia

We report the development of a therapeutic inhibitor, single chain antibody variable fragment (scFv) against DNA-dependent protein kinase catalytic subunit (DNA-PKcs), a key enzyme in DNA double strand break repair non-homologous end joining pathway. We demonstrate an ability to endow scFv with drug-like properties that allow it to internalize by nondestructive receptor-mediated endocytosis and escape the endocytic compartment to enter the nucleus. The modified scFv inhibited DNA double-strand break repair by binding a regulatory site in DNA-PKcs and sensitized human cancer cells to a clinically relevant dose of ionizing radiation. Results suggest a potentially general approach for targeting intracellular proteins using systemically administered single-chain antibodies.

6:20 Close of Day

Day 1  |  Day 2 |  Short Courses 


Suggested Event Package (November 1 – 4):

November 1

Pre-Conference Short Courses:

Targeting GPCRs and Ion Channels with Antibodies (SC2)

November 2 - 3


HDAC Inhibitors – Developing Molecules for Targeting Oncology and More 

November 3 - 4


Kinase Inhibitors – Moving from Discovery to Development 

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 Short Courses

2015 Discovery on Target Brochure  





Molecular Sensing

Rosa Drug Development Advisors






The exhibit hall was sold out in 2014, so please contact us early to reserve your place. To customize your sponsorship or exhibit package for 2015, contact:

Jon Stroup
Sr. Business Development Manager


September 21 

Next-Generation Histone Deacetylase Inhibitors Symposia 

Strategies for Rare Diseases Symposia 

September 22 

Developing CRISPR-Based Therapies Symposia 

September 22 - 23 

Targeting Epigenetic Readers and Chromatin Remodelers 

Targeting the Ubiquitin Proteasome System 

Targeting the Microbiome 

GPCR - Based Drug Discovery - Part 1 

Antibodies Against Membrane Protein Targets - Part 1 

RNAi for Functional Genomics Screening 

Gene Therapy Breakthroughs 

Targeting Ocular Disorders 

September 23 - 24 

Targeting Histone Methyltransferases and Demethylases 

Targeting the Unfolded Protein Response 

Kinase Inhibitor Discovery 

GPCR-Based Drug Discovery - Part 2 

Antibodies Against Membrane Protein Targets - Part 2 

New Frontiers in Gene Editing 

Quantitative Systems Pharmacology 

Short Courses 

SC1: Cancer Metabolism: Pathways, Targets and Clinical Updates 

SC2: Leveraging Data and Analytics for Drug DiSCovery 

SC3: Setting Up Effective Rnai SCreens: From Design to Data to Validation 

SC4: Phenotypic SCreening and Chemical Probe Development 

SC5: GPCR Structure-based Drug Discovery 

SC6: Targeting of GPCRs with Monoclonal Antibodies 

SC7: Setting Up Effective Functional SCreens Using 3D Cell Cultures 

SC8: Targeting Protein-protein Interactions: Biophysical Approaches 

SC9: Preclinical Animal Models for Ocular Indications 

SC10: Introduction to Allosteric Modulators and Biased Ligands of GPCRs 

SC11: Introduction to Targeted Covalent Inhibitors 

SC12: Assays and High-throughput SCreening for Novel Epigenetic Inhibitors 

SC13: Gamification and Drug Target Challenges 

SC14: A Primer to Gene Editing: Tools and Applications 

SC15: Using Mechanistic Physiological Models In Drug Development