Discovery on Target
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Targeting the P13K Pathway

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Phosphoinositide 3-kinases  (PI3K) are major therapeutic targets  in developing tumor treatments, due to their influence of  various signaling pathways and cell functions such as cell growth.  In the last few years, new applications for non-tumor related diseases are slowly emerging, such as inflammatory diseases, autoimmune diseases or diabetes. This conference is focusing on the challenges and also on lessons learned when developing targets for PI3K, Akt and mTOR and also on current new developments.


7:00 am Conference Registration and Morning Coffee


Identifying and developing novel inhibitors

8:30 Chairperson’s Opening Remarks

Kevin Liu, Ph.D., Senior Principle Scientist, Pfizer, Inc.

8:40 Design 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 isoform-specific inhibitor discovery and development for the treatment of Th17 cell-mediated immune-inflammatory diseases, and of specific tumour types.

9:10 From PI3K/mTOR Dual Inhibitors to PI3K and mTOR Selective Inhibitors

Kevin Liu, Ph.D., Senior Principle Scientist, Pfizer, Inc.

Drug discovery program that aiming to find small molecules that target the PI3K pathway with different selectivity profile between PI3K and mTOR will be discussed in this talk.

9:40 Genome-Wide RNAi Screening Identifies New Components of the mTOR Signaling Pathway in Pancreatic Cancer Cells

Angela Papageorgiou, Ph.D., Research Fellow, Massachusetts General Hospital and Harvard Medical School

Design and development of the genome-wide RNAi screen, Bioinformatic analysis, secondary assays.

10:10 Grand Opening Coffee Break in the Exhibit Hall

10:40 mTOR as a Therapeutic Target in Multiple Myeloma

Noopur Raje, M.D., M.B., Associate Professor, Medicine, Massachusetts General Hospital, Harvard Medical School

The PI3kinase/Akt/mTOR pathway is important in the development of growth, survial and drug resistance in multiple myeloma. Here we will first highlight the biology of this pathway followed by preclinical and clinical data highlighting targeting the mTOR pathway. We will focus specifically on combination startegies and hoghlight novel mTOR inhibitors with thegoal of overcoming drug resistance.

Sponsored by
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11:10 PI3K (PIK3CA) Mutation Analysis: Challenges in Companion Diagnostic Development
David M. Jackson, Ph.D., Senior Director, Pharma Business Development, QIAGEN
Mutations in the PIK3CA oncogene may result in dysfunctional cell signaling and ultimately tumorigenesis. Numerous targeting therapies are in pre- and clinical development that attack PI3K in general and mutated PI3K in particular.  Designing, developing and validating a PI3K mutation analysis test as a companion diagnostic has proven challenging. This talk will focus on technical, regulatory and clinical issues that influence development of regulated mutation-based companion diagnostic tests using challenges faced during development of a real-time PCR test kit for the PIKCA gene.

11:40 Preclinical Evaluation of the Novel PI3K/mTor Inhibitor GDC-0980 and Prediction of its Human

Laurent Salphati, Pharm.D., Ph.D., Scientist, Drug Metabolism and Pharmacokinetics, Genentech

The PI3K/mTor inhibitor GDC-0980 was evaluated in vitro and in vivo in preclinical studies. The results that guided its development and its predicted human pharmacokinetics will be presented, along with comparisons to observed clinical pharmacokinetic data.

12:10 pm Expert Panel Discussion: Targeting the PI3K Pathway - Which are Promising Approaches?

12:40 Luncheon Presentation (Sponsorship Opportunity Available) or Lunch on your own


From pre-clinical to clinical success

2:20 Chairperson’s Remarks

David Sherris, Ph.D., President and CEO, Paloma Pharmaceuticals

2:25 Development of the Clinical Stage Dual mTOR-PI3K Inhibitor SF1126

Joseph R. Garlich, Ph.D., CSO, Semafore Pharmaceuticals

SF1126 is the first small molecule dual PI3K-mTOR inhibitor in clinical development that is designed to localize selectively in the tumor by incorporating a peptide inhibitor of αvβ3- and αvβ5-integrins, which are transmembrane cell adhesion proteins expressed in new tumor vasculature and within the tumor compartment. SF1126 inhibits all four I PI3K isoforms along with other cancer targets such as mTOR, DNA-PK, PIM1, and PLK1. The development of SF1126 from idea to bench to bedside along with future plans will be discussed.

2:55 Pre-Clinical Characterization of Novel mTORC1 and mTORC2 Inhibitors

Shripad Bhagwat, Ph.D., Research Investigator, Biochemical and Cellular Pharmacology, OSI Pharmaceuticals, Inc.

In this presentation, I will be discussing OSI’s efforts in discovery of two selective and potent mTORC1/mTORC2 inhibitors, OSI-027 and
OXA-01. I will discuss (a) structures, in vitro potency and selectivity profile of OSI-027 and OXA-01 (b) in vitro and in vivo anti-tumor effects of OSI-027 and OXA-01 in various cell and tumor models and their differentiation from rapamycin, (c) anti-angiogenic effects of OXA-01 in vivo and (d) in vitro combination studies of OSI-027 and OXA-01 with MTTs and SOC agents.

3:25 Networking Refreshment Break in the Exhibit Hall

4:05 Palomid 529, a dual TORC1/TORC2 Allosteric Inhibitor of the PI3K/Akt/mTOR Pathway

David Sherris, Ph.D., President and CEO, Paloma Pharmaceuticals, Inc.

Palomid 529 is an allosteric inhibitor of the PI3K/Akt/mTOR pathway causing the dissociation of the TORC1 and TORC2 complexes. Other
dual inhibitors function by competitive inhibition of mTOR kinase via a semi-selective tyrosine kinase inhibitor and hence do not cause dissociation (complex component inhibition outside of mTOR kinase) of the complexes. As Palomid 529 dissociates the complexes via an allosteric mechanism, it would be expected to exert greater control of PI3K/Akt/mTOR pathway as compared to mTOR kinase tyrosine kinase inhibition.

4:35 Discovery of Novel Multiplex PI3 Kinase Inhibitors for the Treatment of Cancer

Dapeng Qian, M.D., Ph.D., Senior Director, Drug Discovery, Progenics Pharmaceuticals, Inc.

5:05 Interactive Breakout Discussion Groups

Developing Novel PI3K  Inhibitors - Challenges and Experiences

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

What Criteria Should One Consider in Bringing a PI3K/Akt/mTOR Inhibitor into the Clinic?

Moderator: David Sherris, Ph.D., President and CEO, Paloma Pharmaceuticals

6:15 – 7:15 Happy Hour in the Exhibit HallSponsored by
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Final Agenda Now Available









The exhibit hall was sold out in 2015, so please contact us early to reserve your place. To customize your sponsorship or exhibit package for 2016, contact:

Jon Stroup
Sr. Business Development Manager






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