Conference Day One

Tuesday, February 11

8:00 am Check-In, Coffee & Light Breakfast

8:45 am Chair’s Opening Remarks

Unraveling Kinase Biology to Determine Structural Specificity & Accelerate Drug Discovery

9:00 am De-Risking Kinase Preclinical Studies: Translating Biochemical Data Into Cellular Selectivity

Synopsis

  • Shifting away from isolated kinases to comprehend their larger complexes and their interactions
  • Depicting how structural changes within kinase complexes influence target activation and modulation
  • Evaluating the impact of post-translational modifications on assembly, stability, and functionality

9:30 am Enabling Discovery with AI: Using Structural Predictions to Influence Next Generation Kinase Inhibitors

  • Rayees Rahman Co-founder & Chief Executive Office, Harmonic Discovery

Synopsis

  • Reimagining the industry’s approach to structure-guided design to reveal how compounds can acquire on-target selectivity
  • Harnessing AI to detect conformational changes that can shed light on kinase transition states in the context of drug binding
  • Diving into key structural features of the active kinase domain to discover potential sites of intervention

10:00 am Session Reserved for AssayQuant

10:30 am Morning Refreshments & Speed Networking

Synopsis

Speed Networking will take place in small groups of 4 or 6 within the first 20 minutes of the Morning Break to provide all attendees the chance to maximize their engagement.

Overcoming Mutation-Driven Resistance to Combat Tumor Resilience & Enhance Drug Design

11:30 am Optimizing Kinase Selectivity & Predicting Resistance Using Physics-Based Modeling

  • Aleksey Gerasyuto Vice President & Head of Drug Discovery & Chemistry, Schrodinger Inc

Synopsis

  • Unlocking kinome-wide selectivity of WEE1 inhibitors through free energy calculations
  • Optimizing selectivity of DLK inhibitors through off-target free energy perturbation (FEP)
  • Predicting clinical resistance with protein-residue-mutation FEP

12:00 pm Streamlining Kinase drug discovery with Lumit Immunoassays: Monitoring Protein Phosphorylation, Degradation and HTS Applications

  • Hicham Zegzouti Senior Scientist & Group Leader - Research, Promega Corporation

Synopsis

  • The Lumit Immunoassay Cellular System is a homogeneous bioluminescent immunoassay that combines immunodetection with enzyme subunit complementation to measure target analytes directly in cell lysates.
  • Protein Phosphorylation Detection: Lumit immunoassays enable rapid and wash-free detection of phosphorylation in kinase signaling pathways, such as RAS-MAPK/ERK, for inhibitor evaluation and profiling.
  • Targeted Protein Degradation (TPD): Lumit immunoassays enable efficient profiling of PROTAC-mediated protein degradation across multiple cell lines, supporting targeted kinase degradation.
  • High-Throughput Screening (HTS): Lumit immunoassays are optimized for scalable HTS, enabling efficient screening of kinase pathway modulators in 384- and 1536-well formats.

12:30 pm Lunch & Networking

1:30 pm Breaking Industry Barriers: Discovering BAY2927088, Novel Inhibitor of ERBB2 Mutants in NSCLC

  • Matthew L. Meyerson Director & Professor - Pathology, Medical Oncology & Center Cancer Genome Discovery, Dana-Farber / Harvard Cancer Center

Synopsis

  • Unpacking challenges of mutant-selective kinase inhibition: targeting EGFR/ERBB2 exon 20 insertion mutants
  • Evaluating biochemical and cellular approaches to developing inhibitors for untargetable mutant TYK
  • Revealing clinical data on selectivity for ERBB2 exon 20 insertion mutants in NSCLC

Maximizing Kinase Selectivity to Prevent Off-Target Binding & Increase Drug Efficacy

2:00 pm Session Reserved for Oncolines

2:30 pm Afternoon Refreshments & Poster Session

3:15 pm Panel Discussion: The Kinome Kit – Augmenting Selectivity Profiling Through Assays to Achieve On-Target Specificity

Synopsis

  • Evaluating compounds against other kinases to identify potential off-target effects in early development
  • Employing continuous assay systems to access full enzymatic activity over time and monitor various mechanisms of action
  • Uncovering strategies for detecting kinase selectivity to facilitate effective target engagement and improve drug efficacy

4:00 pm AB801 Potently & Selectively Inhibits AXL to Overcome Therapeutic Resistance

Synopsis

  • Inhibiting both ligand-dependent and ligand-independent AXL signaling
  • Attaining high selectivity and potency for optimal AXL inhibition
  • Overcoming AXL-mediated resistance to standard-of-care therapies

4:30 pm Chair’s Closing Remarks

4:45 pm End of Conference Day One

SPEAKERS
DAY TWO