Pre-Conference Day
Tuesday May 10, 2022

WORKSHOP A

Leveraging the Structure-Based Design of Proximity Inducing Molecules
9:30 – 12:00

Key Discussion Topics include:

  • How to do this in an unbiased and scalable way
  • What tools are available to help achieve this?
  • What are they key challenges associated with this and can they be overcome?
  • How to improve the diversity of scaffolds/modules
  • How successful has virtual screening been to identify hits for both biologics and small molecules?
  • Understanding the structure-based design will elaborate on the medicinal chemistry and will help predict effect
  • What biophysical assays are necessary to validate the structure-based design of molecules?
  • What is the optimal distance between 2 proteins of interest?
  • Understanding the complex formation between proteins

More details will be revealed soon

Workshop Leader

Will

William Pomerantz
Associate Professor
University of Minnesota

Networking Break

12:00 - 13:00

WORKSHOP B

Better Understanding Emerging Extracellular Antigen-based Induced Proximity Therapeutics
13:00 – 15:30

  • Emerging methods to target cell-surface antigens and proteins towards degradation
  • What are the benefits of leveraging extracellular induced proximity between proteins?
  • What are characteristics of the current antibody conjugate formats?
  • How do we improve the initial tool/probes towards a therapeutic index?
  • Can we develop a rule-set for designing antibody-based proximity drugs?
  • Discuss the pros/cons of antibodies vs. small molecule-based antigen recognition

Examples of formats to be discussed:

A) AbTACs: Antibody-Based PROTACs for the Degradation of the Cell-Surface
Immune Checkpoint Protein PD-L1.

B) Antibody-enzyme conjugates:

  • Antibody mediated induced proximity for enhancing tumor cell susceptibility
    to antibody dependent cell-mediated cytotoxicity (ADCC)

C) Antibody-tri-GalNAC Conjugates (LYTACs):

  • LYTACs engage the asialoglycoprotein receptor (ASGPR), a liver-specific
    lysosome-targeting receptor, to degrade extracellular proteins in a celltype-
    specific manner

D) Antibody-degrader conjugates:

  • Case study 1: Genentech’s antibody-chimeric BET degrader approach and in
    vivo activity in blood cancers.
  • Case study 2: Antibody-PROTAC conjugates for HER2-Dependent Targeted
    Protein Degradation of BRD4

Workshop Leaders

Ed Ha 1

Ed Ha
Head of Chemistry & Bioconjugation
Angiex

Manish Hudlikar

Manish Hudlikar
Scientist, Chemistry & Bioconjugates
Angiex