Archived Content

Advances in Targeting the PI3K Pathway


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Targeting the PI3K Pathway offers opportunities for therapeutic developments, in a large number of human diseases, such as cancer, metabolic diseases and inflammation, to name a few. A variety of PI3K inhibitors have been tested in pre-clinical studies and several have now entered clinical trials. This meeting provides input and updates on the current status of PI3K targeting drugs and it discusses progress made in drug discovery and in exploring novel applications for those drugs. Experts share their lessons learned and their knowledge gained.


PI3K Pathway Perspectives

1:30 pm Chairperson’s Remarks

Joseph R. Garlich, Ph.D., Cancer Research Consultant, Stemica LLC


PTEN and PI-3 Kinase the Yin and Yang of Oncogenic Signaling

Donald Durden, M.D., Ph.D.,Vice Chair for Research, Department of Pediatrics, University of California San Diego; Associate Director, Pediatric Oncology, Moores UCSD Cancer Center

2:10 Discovery and Development of Novel, Isoform-Selective PI3K Inhibitors for the Treatment of Immune-Inflammatory Diseases and Cancer

Stephen J. Shuttleworth, Ph.D., FRSC CChem, CSO, Karus Therapeutics Ltd.

Our R&D programs at Karus are centered on the design and development of subtype-selective small molecule inhibitors of PI3K and of HDAC. This talk will outline our approaches to PI3K isoformspecific inhibitor discovery and development for the treatment of Th17 cell-mediated immune-inflammatory diseases, and of specific tumour types.

2:40 The mTORs New Clothes-Questioning Dogma and Dispelling Myths Surrounding PI3K Pathway Inhibition

Joseph R. Garlich, Ph.D., Cancer Research Consultant, Stemica LLC

Previously it was thought that many tumor types would be sensitive to PI3K pathway inhibitors but emerging biology has shown complex interactions including alternate pathway activation/resistance mechanisms exist to blunt the effects of these inhibitors. These new developments argue for inhibiting more kinase targets for best efficacy. PI3K isoform selective inhibition represents the "less is more" approach but several examples are now available to refute this line of attack demonstrating it to be less efficaceous. This and other ramifications of new pathway biology will be discussed.

3:10 Refreshment Break in the Exhibit Hall with Poster Viewing

Progress in Targeting the PI3K Pathway

3:45 Targeting the PDK1/Akt Signaling Pathway

Jacques Ermolieff, Ph.D., Senior Principal Scientist, External Research Solutions (ERS), Pfizer Worldwide Research and Development

4:15 Mutation Status is a Key Determinant of In Vitro Response to COTI-2, a Highly Effective Third Generation Thiosemicarbazone for the Treatment of Susceptible Cancers

Wayne Danter, Ph.D., President & CEO, Critical Outcome Technologies, Inc.

4:45 Role of Phosphoinositide 3-Kinase P110 Gamma in Pancreatic and Liver Cancer

Marco Falasca, Ph.D., Professor in Molecular Pharmacology, Blizard Institute, Queen Mary University of London

The PI3K subunit p110alpha has a well established role in cancer and gain of function of this isoform, due to mutation is common in several human cancers. A role has been suggested for p110 gamma in tumour angiogenesis and drug resistance of chronic myeloid leukemia cells. Interestingly, overexpression of wild-type p110alpha does not appear to have transforming potential while overexpression of the wild-type catalytic subunits p110beta, gamma or delta is sufficient to induce an oncogenic phenotype in cultured cells. Accumulating evidence from our lab clearly indicate that p110 gamma plays a key and specific role in pancreatic and liver cancer.

5:15 Targeting Specific Class I PI3K Isoforms for the Treatment of B and T-Cell Malignances

Brian Lannutti, Ph.D., Associate Director, Cancer Research, Gilead Sciences, Inc.

5:45 End of Day


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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