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Novel Strategies for Kinase Inhibitors


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The use of Kinase Inhibitors is moving beyond the cancer field. The newest developments show lots of promise, especially in areas such as inflammation and autoimmune diseases. Novel applications for existing inhibitors are being researched and new targets to develop cancer therapeutics are being explored. With over 40% of the projects of large pharma companies in non-oncology areas, there is clearly a need to address the arising challenges such as resistance, specificity, off-target effects and efficacy.


7:00 am Conference Registration and Morning Coffee

Novel (Non-Oncology) Applications

8:30 Chairperson’s Opening Remarks

Andy Whitlock, Ph.D., Director, Pre-Clinical Development, Ora, Inc.

8:40 Novel Opportunities for Kinases in Ophthalmology

Andy Whitlock, Ph.D., Director, Pre-Clinical Development, Ora, Inc.

Ocular anterior segment diseases, such as allergic conjunctivitis, dry eye and post-operative inflammation need new potent treatments with efficacy comparable to steroids but very limited side effects. Recently, a number of new kinase inhibitors have been studied in more detail for conditions such as cancer and rheumatoid arthritis. The mechanisms of action of these novel therapies are very applicable to a number of ophthalmic diseases that are underserved with current treatments.

9:10 Targeting the Malaria Kinome

Andrew Tobin, Ph.D., Professor of Cell Biology, Cell Physiology and Pharmacology, MRC Toxicology Unit, University of Leicester

We have just published in Nature Communications a paper describing the essential protein kinases in the human malaria parasite Plasmodium falciparum. In collaboration with Monash University, the structural genomics consortium in Toronto and a major pharmaceutical company we are now developing novel protein kinase inhibitors that selectively target the malaria kinome.

9:40 RC Kinase: A Novel Target Implicated in COPD and Idiopathic Pulmonary Fibrosis

Stefen Boehme, Ph.D., Director, Immunology, Axikin Pharmaceuticals

We have characterized a novel serine/threonine protein kinase, called RC kinase. Inhibition of RC kinase by siRNA or novel small molecule inhibitors reduces pulmonary inflammation and cellular and biochemical markers of disease in murine models of both COPD and IPF. We will discuss our ongoing preclinical development of antagonists against this novel kinase and their utility as a possible treatment for COPD and IPF.

10:10 Grand Opening Coffee Break in the Exhibit Hall with Poster Viewing

Targeting Kinases from Different Vantages

10:40 Chemoproteomic Approaches to Target Deconvolution and Selectivity Profiling of Kinase Inhibitors

Markus Schirle, Senior Investigator I, Developmental and Molecular Pathways, Novartis Institutes for BioMedical Research, Inc.

Quantitative chemoproteomics allows the determination of protein interaction profiles of drug candidates in a disease-relevant cell line or tissue. In contrast to standard biochemical and biophysical kinase assays, application of this method to kinase inhibitors determines compound binding to endogenously expressed kinases under conditions approximating the physiological situation with regard to the molecular state of the kinase and presence of required cofactors and regulatory proteins. Different experimental variants and applications of this approach will be presented.

Zalicus 11:10 Use of cHTS for Identification of Synergistic Drug Combinations that are Selective and Kill Cancer CellsRichard Rickles, Ph.D., Senior Research Fellow Oncology & Director, Discovery Partnerships, Zalicus Inc.Monotherapies are rarely effective cancer treatments as tumor cells have a tremendous capacity to overcome the activity of single drugs. Understanding the multi-target mechanisms for selective killing is required for oncology drug discovery.  We have developed a cHTS platform for the rapid screening of thousands of drug combinations in hundreds of cell lines to identify potent drug combinations that selectively kill tumor cells. The platform is a powerful tool for both discovery and translational research.    

11:40 The Nanocyclix Platform: Applications on Novel Kinase Targets in Cancer, CNS and Epigenetics

Jan Hoflack, Ph.D., CSO, Drug Discovery, Oncodesign Biotechnology

Oncodesign's Nanocyclix platform gives access to potent and selective inhibitors for known and unexplored kinases. Broad profiling and phenotypic screening approaches will be described that have led to advanced programs in cancer, CNS, inflammation and epigenetics fields. The compounds display unique properties as related to ADME profiles and CNS penetration.

12:10 pm Biophysical and Mechanistic Insights into a Novel Allosteric Inhibitor of Spleen Tyrosin Kinase

Justin Hall, Ph.D., Senior Scientist, Structural Biology and Biophysics, Pfizer

Kinases play essential roles in cell signal amplification and transduction and are important targets in oncology and inflammation. Due to the conservation and prevalence of the kinase domain motif (ca. 520 different proteins), it is a substantial challenge to develop ATP competitive inhibitors against a specific target while also simultaneously out-competing physiological concentrations of ATP. Recourse to this challenge is the development of allosteric kinase inhibitors that are noncompetitive against ATP; we show here a novel allosteric inhibitor of spleen tyrosine kinase (Syk) that may help the development of human therapeutics.

A Novel Approach for the Study of Kinase Signal Transduction – Comparative Measurement of in vitro and in vivo Expression of MAPK Pathway Kinases

W. Matthew Dickerson, Ph.D., Senior Scientist , Assay Development, BioScale, Inc.The ability to measure the activation states and molecular interactions of the kinases comprising the MAPK and PI3K-AKT pathways are crucial in the efficient and effective discovery and development of anti-cancer pharmaceuticals and therapeutics.  Results of the assessment and quantification of EGFR, MEK, ERK, p38, JNK and AKT in several tumor cell lines with or without stimulation of surface ligand receptors, and compared with lysates prepared from xenograft tumors derived from the same cell lines will be discussed.

Emerging Therapeutic Targets

2:20 Chairperson’s Remarks

Denis Drygin, Ph.D., Vice President, Biology, Cylene Pharma

2:25 Protein Kinase CK2, a Logical Therapeutic Target for Drug Combinations

Denis Drygin, Ph.D., Vice President, Biology, Cylene Pharma

Protein kinase CK2 controls multiple biological pathways that are necessary for the maintenance of malignant phenotype. Increased expression levels and/or activity of CK2, which are commonly found in cancers, have been linked to poor prognosis and drug resistance, highlighting the potential of CK2 as a therapeutic target in drug combinations. I will discuss known mechanisms that underlie the regulation of drug resistance by CK2, present examples of the enhancement of therapeutic outcome by modulation of CK2 expression and/or activity, and provide a perspective on the potential use of CK2 inhibitors for the clinical development in combination with other therapeutics. 

2:55 Repurposing Kinase Medicinal Chemistry for Neglected Diseases Caused by Protozoan Parasites

Michael Pollastri, Ph.D., Associate Professor, Chemistry & Chemical Biology, Northeastern University

3:25 Refreshment Break in the Exhibit Hall with Poster Viewing

4:05 A Synthetic Lethal and Survival RNAi Screen Accompanied by Cancer Drug Neratinib Identifies Novel Oncology Targets Leading to Neratinib and Paclitaxel Combination Treatments and Markers of Drug Resistance

Attila Seyhan, Ph.D., MIT Research Affiliate, The Chemical Engineering Department, Massachusetts Institute of Technology

We undertook a genome-wide pooled lentiviral RNAi screen in comibantion with neratinib, a tyrosine kinase inhibitor of the ErbB receptor family currently in Phase III clinical trials, and discovered a panel of genes whose inhibition selectively impaired or enhanced the viability of cancer cells in the presence of subeffective or lethal concentrations of neratinib.

4:35 The Discovery of Potent and Selective Inhibitors of CK2 Kinase Identified through Focused Subset Screening and Structure Based Design

Claudio Chuaqui, Ph.D., Principle Scientist II, Astrazeneca R&D

In this talk I will describe the discovery of potent and selective CK2 inhibitors identified via  kinase-focused subset screening as starting points for structure-based design. The synthesis, SAR, and effects of this novel series on Akt signaling and cell proliferation in vitro are described.

5:05 Interactive Breakout Discussion Groups

The Challenge of Drug Resistance

Moderator: David Proia, Ph.D., Associate Director, Cancer Biology, Synta Pharmaceuticals

• Establishing drug resistance using in vitro models
• Identifying the mechanisms of resistance and ways to bypass
• Translation in vivo and in the clinic

Drug Combination Therapies – Pro’s and Con’s to Consider

Moderator: Denis Drygin, Ph.D., Vice President, Biology, Cylene Pharma

• Challenges in the identification of clinically significant “Synthetic Lethality”
• Multi-targeted agents vs combination of selective agents
• Minimizing side-effects and toxicity of drug combinations

ATP Non-Competitive Inhibitors

Moderator: Justin Hall, Ph.D., Senior Scientist, Structural Biology and Biophysics, Pfizer

• Kinase active site anatomy; which residues are broadly conserved and how is inhibitor selectivity built?
• The kinase domain in contexts; why do we usually study isolated the kinase domains and what can we gain from looking at larger constructs?

6:15 – 7:30 Welcoming Reception in the Exhibit Hall with Poster Viewing


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Next-Generation Histone Deacetylase Inhibitors

Strategies for Tackling Rare Genetic Diseases

Understanding CRISPR: Mechanisms and Applications

Autoimmunity – Small Molecule Approaches

NK Cell-Based Cancer Immunotherapy

Medical Dermatology Therapeutic R&D and Technical Innovation



Targeting Histone Methyltransferases and Demethylases

Targeting the Ubiquitin Proteasome System

Targeting the Microbiome
– Part 1

GPCR-Based Drug Discovery - Part 1

Advances in Gene Editing and Gene Silencing – Part 1

Gene Therapy Breakthroughs

Antibodies Against Membrane Protein Targets – Part 1

Targeting Cardio-Metabolic Diseases

Targeting Ocular Disorders


Targeting Epigenetic Readers and Chromatin Remodelers

Kinase Inhibitor Discovery

Targeting the Microbiome
– Part 2

GPCR-Based Drug Discovery - Part 2

Advances in Gene Editing and Gene Silencing – Part 2

Translating Cancer Genomics

Antibodies Against Membrane Protein Targets – Part 2

Metabolomics in Drug Discovery

TRAINING SEMINAR: Data Visualization


Monday, September 19
8:00 - 11:00 am

(SC1) Immunology Basics for Chemists

(SC2) Designing Peptide Therapeutics for Specific PPIs

(SC3) Phenotypic Screening and Chemical Probe Development

(SC4) Medical Dermatology Therapeutic R&D and Technical Innovation - Part 1

Monday, September 19
2:00 - 3:00 pm

(SC5) GPCR Structure-Based Drug Discovery

(SC6) RNA as a Small Molecule Drug Target

(SC7) Using IP Landscape Studies to Improve Your Confidence

(SC8) Medical Dermatology Therapeutic R&D and Technical Innovation - Part 2

Monday, September 19
3:30 - 6:30 pm

(SC9) Targeting of GPCRs with Monoclonal Antibodies

(SC10) Introduction to Targeted Covalent Inhibitors

(SC11) Contact Lens Drug Delivery Systems

(SC12) Introduction to Gene Editing

Monday, September 19
7:00 - 9:30 pm

(SC13) Convergence of Immunotherapy and Epigenetics for Cancer Treatment

Wednesday, September 21
7:00 - 9:30 pm

(SC14) Cancer Metabolism: Pathways, Targets and Clinical Updates

(SC15) Introduction to Allosteric Modulators and Biased Ligands of GPCRs

(SC16) Functional Screening Strategies Using CRISPR and RNAi

(SC17) Challenges and Opportunities in DNA Methyl Transferase (DNMT) Inhibitors as Therapeutics