Cambridge Healthtech Institute’s 2nd Annual

Immunology and Oncology: Emerging Drug Targets and Therapeutics

New Approaches for Treating Autoimmunity and Cancer

September 16 - 17, 2020 ALL TIMES EDT

The rapid pace of research in the immunology field and medically relevant signaling pathways highlighted by new biologics on the market are providing a plethora of new drug targets whose modulation are showing promise for treating diseases of the immune system or cancer. Often it’s the same target, modulated in opposite ways, that proves beneficial for both diseases. This conference covers such dual targets. We also focus on molecular targets whose modulation impacts either one or the other (autoimmunity or oncology). All drug modalities will be explored, though an emphasis will be on small molecules because many of the newest drug targets are intra-cellular.

Wednesday, September 16

TARGETING METABOLISM FOR CANCER AND AUTOIMMUNITY

9:30 am

Arginase Inhibition Leads to Increased Immune Cell Infiltration and Anti-Tumor Activity in Various Syngeneic Tumor Models

Alwin Schuller, PhD, Director, Oncology, AstraZeneca Pharmaceuticals

With both T cells and NK cells dependent on arginine, arginase has been recognized as a major immune-suppressive mechanism. We developed a small molecule arginase inhibitor that demonstrates in vivo activity evidenced by an increase in plasma and tumor arginine levels, reactivation of anti-tumor immunity, and single agent anti-tumor activity. Combination with various immune activators, including checkpoint inhibitors, further increases signs of immune activation as well as anti-tumor response.

9:50 am Session Break
10:10 am

A Novel Pharmacological Inhibitor of the Mitochondrial F1Fo-ATPase Which Represses Viability of Cancerous Cells

Michelangelo Campanella, Pharm D, PhD, Professor of Pharmacology, Head of the Mitochondrial Cell Biology and Pharmacology Unit, University of London

Function of the mitochondrial enzyme F1Fo-ATPsynthase is compromised in both acute and chronic pathologies. This makes the enzyme an exploitable target to devise innovative therapeutics for long-term metabolic dysfunctions such as cancer. In my talk, I shall illustrate our progresses on this account by reporting synthesis and in vitro characterisation of the NH-Sulfoximine (NHS) which exploits the bio-energy dependent on mitochondria acting in reverse to deliver cytostatic effect.

Qunsheng Ji, WuXi AppTec, VP, Head of Oncology & Immunology Unit, Oncology & Immunology, WuXi AppTec

Despite clinical progress in a broad range of tumor types with immune checkpoint inhibitors, many patients don’t respond to therapies. The talk will focus on a CRISPR/Cas9 mediated in vivo screen platform enabling identification of genes that control cancer cell sensitivity to T cell-mediated elimination as potential targets or biomarkers.

10:50 am LIVE Q&A:

Session Wrap-Up Panel Discussion

Panel Moderator:
Masha Poyurovsky, PhD, Vice President, Discovery Biology, Kadmon Corporation
Panelists:
Alwin Schuller, PhD, Director, Oncology, AstraZeneca Pharmaceuticals
Michelangelo Campanella, Pharm D, PhD, Professor of Pharmacology, Head of the Mitochondrial Cell Biology and Pharmacology Unit, University of London
Qunsheng Ji, WuXi AppTec, VP, Head of Oncology & Immunology Unit, Oncology & Immunology, WuXi AppTec
11:10 am Coffee Break - View Our Virtual Exhibit Hall

TARGETING METABOLISM FOR CANCER AND AUTOIMMUNITY (CONT.)

11:25 am

The Role of Aryl Hydrocarbon Receptor and the Kyneurin Pathway in Cancer Immuno-Metabolism

David Sherr, Professor, Environmental Health, Boston University
11:45 am

Discovery of Novel IDO/Aryl Hydrocarbon Pathway Inhibitors

Bing Xia, PhD, Investigator, R&D Medicinal Science & Technology, GlaxoSmithKline

Indoleamine 2,3-dioxogenase-1 (IDO1) is induced and activated in response to viral and bacterial infection causing a dysfunctional immune response in clearing pathogens. IDO1 inhibitors (IDO1i) can potentially restore immune function in indications such as cancer and infection. A structurally-unique IDO1i class was discovered through the affinity selection of a novel DNA-encoded library. After additional medicinal chemistry iterations, the compound series was elaborated into potential best in class preclinical molecule.

12:05 pm

Regulation of Inflammatory Cell Death Signaling by RIP Kinases

Domagoj Vucic, PhD, Staff Scientist, Early Discovery Biology, Genentech

RIP1 kinase is a critical mediator of multiple signaling pathways that regulate inflammatory responses and cell death. Using RIP1 kinase inhibitor, GNE684, we show that RIP1 inhibition can efficiently block arthritis, skin and liver inflammation, and colitis in animal disease models. Conversely, RIP1 inhibition had no effect on tumor growth, metastases or viral infections. Together these data emphasize the protective role for RIP1 kinase inhibition in inflammatory disease.

12:25 pm LIVE Q&A:

Session Wrap-Up Panel Discussion

Panel Moderator:
Tatiana Novobrantseva, PhD, Co-Founder & CSO, R&D, Verseau Therapeutics
Panelists:
David Sherr, Professor, Environmental Health, Boston University
Bing Xia, PhD, Investigator, R&D Medicinal Science & Technology, GlaxoSmithKline
Domagoj Vucic, PhD, Staff Scientist, Early Discovery Biology, Genentech
12:45 pm Lunch Break - View Our Virtual Exhibit Hall

NEW IMMUNO AND/OR ONCOLOGY TARGETS

1:15 pm

Inhibitors of Sec61 as Novel Anti-Cancer Therapeutics

Dustin McMinn, PhD, Senior Director, Head of Chemistry, Kezar Life Sciences

Post-translational functionalization of most secreted and transmembrane proteins requires co-translational translocation to the ER through Sec61. Translocation is negotiated by protein interactions between Sec61 and unique signal sequences specific to each translating protein. Disruption of these interactions in specific or multi-signal sequence fashion presents an opportunity to modulate protein homeostasis toward therapeutic benefit. Development of signal and multi-signal sequence selective Sec61 inhibitors as novel anti-cancer agents will be discussed.

1:35 pm

Targeting Novel Macrophage Checkpoints for Modulating Anti-Tumor Responses

Tatiana Novobrantseva, PhD, Co-Founder & CSO, R&D, Verseau Therapeutics

Macrophages can adopt different functional roles in response to signals from their environment, including the ability to direct pro-inflammatory and anti-inflammatory immune responses. Verseau is utilizing its proprietary all human drug discovery and translation platform to develop an expansive pipeline of macrophage checkpoint modulators. At Verseau we have nominated and validated more than two dozen targets that modulate human macrophage biologyThe lead program targeting PSGL-1, reprograms macrophages to a pro-inflammatory state, activates T cells and attracts other immune cells to generate a coordinated and powerful anti-tumor response.

Gaurav Agrawal, PhD, Scientific Development Manager, Research & Development, Eurofins DiscoverX

Covid-19 has been declared a global pandemic by WHO. There are hundreds of active clinical programs focused on developing and repurposing therapeutic drugs for treatment of Covid-19. In this talk, we highlight how our cell-based assays are supporting these programs, particularly in managing proinflammatory cytokines associated with high mortality rate in Covid-19 patients.

2:15 pm LIVE Q&A:

Session Wrap-Up Panel Discussion

Panel Moderator:
Chaohong Sun, PhD, Director, Protein Sciences & FBDD, AbbVie, Inc.
Panelists:
Dustin McMinn, PhD, Senior Director, Head of Chemistry, Kezar Life Sciences
Tatiana Novobrantseva, PhD, Co-Founder & CSO, R&D, Verseau Therapeutics
Gaurav Agrawal, PhD, Scientific Development Manager, Research & Development, Eurofins DiscoverX
2:35 pm Refresh Break - View Our Virtual Exhibit Hall
3:00 pm Interactive Breakout Discussions - View Our Virtual Exhibit Hall

Join a breakout discussion group. These are informal, moderated discussions with brainstorming and interactive problem solving, allowing participants from diverse backgrounds to exchange ideas and experiences and develop future collaborations around a focused topic. Discussion topics and moderators will be listed on the website.

3:35 pm Close of Day

Thursday, September 17

TARGETING AUTOIMMUNITY WITH SMALL MOLECULES

10:15 am

An IL36 Antagonist for Probing Psoriasis

Chaohong Sun, PhD, Director, Protein Sciences & FBDD, AbbVie, Inc.

IL-36 cytokines, pro-inflammatory members of the IL-1 superfamily, are upregulated in inflammatory disorders. Targeting IL-36 signaling has been an attractive approach for several dermatological diseases including psoriasis. I will present our discovery of A-552, a novel first in class small molecule antagonist of the IL-36 signaling pathway. A-552 binds potently and selectively to human IL-36g and was capable of attenuating IL-36g induced responses in mouse and human disease models.

10:35 am

Discovery and Development of BIIB068: A Selective, Potent, Reversible Inhibitor of Bruton’s Tyrosine Kinase (BTK)

Bin Ma, PhD, Senior Scientist, Medicinal Chemistry, Biogen

Covalent modification of BTK has been proven to be beneficial for cancer patients with multiple drugs on market while their safety profiles are concerned for autoimmune disease indications. A reversible non-covalent BTK inhibitor will have the promise to address this unmet need. We will report our discovery of BIIB068, an exquisitely selective, potent, reversible BTK inhibitor, together with the med chem strategy and Phase I clinical results.

10:55 am

An Oral ROR-Gamma Inverse Agonist for the Treatment of Psoriasis

Kavitha Nellore, PhD, Director, Cell & Molecular Biology, Aurigene Discovery Technologies Ltd

This presentation will cover the discovery and development of AUR101, an ROR-gamma inverse agonist. AUR101 is currently in Phase 2 clinical trials for the treatment of psoriasis (ClinicalTrials.gov Identifier: NCT04207801). 

11:15 am Session Break
11:35 am LIVE Q&A:

Session Wrap-Up Panel Discussion

Panel Moderator:
Murali Ramachandra, PhD, CEO, Aurigene Discovery Technologies, Ltd.
Panelists:
Chaohong Sun, PhD, Director, Protein Sciences & FBDD, AbbVie, Inc.
Bin Ma, PhD, Senior Scientist, Medicinal Chemistry, Biogen
Kavitha Nellore, PhD, Director, Cell & Molecular Biology, Aurigene Discovery Technologies Ltd
11:55 am Coffee Break - View Our Virtual Exhibit Hall

PLENARY KEYNOTE PROGRAM

12:20 pm

PLENARY KEYNOTE: Tackling Undruggable Oncoproteins: Lessons from the VHL Tumor Suppressor Protein

William G. Kaelin, Jr., MD, 2019 Nobel Laureate; Professor, Medical Oncology, Dana-Farber Cancer Institute; Investigator, Howard Hughes Medical Institute; Co-Founder, Cedilla and Tango Therapeutics

VHL tumor suppressor protein (pVHL) inactivation is common in kidney cancer and upregulates the HIF2 transcription factor. PT2977/MK-6482 is an allosteric HIF2 inhibitor now in Phase 3 testing. Thalidomide-like drugs (IMiDs) bind to cereblon which, like pVHL, is the substrate-binding unit of a ubiquitin ligase. IMiDs redirect cereblon to destroy the myeloma oncoproteins, IKZF1 and IKZF3. We have developed new assays for identifying drugs that can destabilize oncoproteins of interest.

12:45 pm LIVE Q&A:

Plenary Keynote Discussion

Panel Moderator:
Stewart Fisher, PhD, CSO, C4 Therapeutics, Inc.
Panelist:
William G. Kaelin, Jr., MD, 2019 Nobel Laureate; Professor, Medical Oncology, Dana-Farber Cancer Institute; Investigator, Howard Hughes Medical Institute; Co-Founder, Cedilla and Tango Therapeutics
12:55 pm LIVE PANEL AND Q&A:

Plenary Keynote Discussion: De-Risking Early Drug Discovery

Panel Moderator:
Nadeem Sarwar, PhD, Founder & President, Eisai Center for Genetics Guided Dementia Discovery, Eisai, Inc.
  • Data Sciences
  • ​Novel Chemical Modalities
  • Investment and Partnering Models
  • COVID-19 Progress as Examples of Successful Partnerships
Panelists:
Anthony A. Philippakis, PhD, Chief Data Officer, Data Sciences & Data Engineering, Broad Institute; Venture Partner, GV
Stephen A. Hitchcock, PhD, Head, Research, Takeda Pharmaceuticals, Inc.
1:35 pm Lunch Break - View Our Virtual Exhibit Hall
2:05 pm Close of Immunology and Oncology: Emerging Drug Targets and Therapeutics Conference
9:50 am Session Break





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