Conference Day One
7:30 am Check-In, Coffee & Light Breakfast
8:15 am Chair’s Opening Remarks
Unraveling Kinase Biology to Determine Structural Specificity & Accelerate Drug Discovery
8:30 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
9:00 am Enabling Discovery with AI: Using Structural Predictions to Influence NextGeneration Kinase Inhibitors
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
9:30 am Session Reserved for AssayQuant
Synopsis
10:00 am Morning Refreshments & Speed Networking
Overcoming Mutation-Driven Resistance to Combat Tumor Resilience & Enhance Drug Design
11:00 am Optimizing Kinase Selectivity & Predicting Resistance Using Physics- Based Modeling
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
11:30 am Breaking Industry Barriers: Discovering BAY2927088, Novel Inhibitor of ERBB2 Mutants in NSCLC
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
12:00 pm Session Reserved for Promega
Synopsis
12:30 pm Lunch & Networking
1:30 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
2:00 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
2:45 pm Session Reserved for DeepKinase
Synopsis
2:55 pm Afternoon Refreshments & Poster Session
Tackling Toxicity Profiles to Optimize Therapeutic Windows & Enable Kinase Inhibition
3:40 pm Shedding Light on a Novel PI3K Inhibitor: Enabling Isoform-Specific Inhibition to Establish Clinical Success
Synopsis
- Examining the mode of action of a novel, non-ATP competitive PI3Kd inhibitor and its pharmacological activity
- Dissecting isoform-dependent toxicity profiles for an improved assessment of therapeutic index
- Highlighting the importance of a selectivity-matched PK profile to optimize the therapeutic potential for clinical development
4:10 pm Leveraging Selective Inhibition of CDK12/13 Through Degradation of Cyclin K
Synopsis
- Outlining how targeted protein degradation of cyclin K enables discovery of highly selective kinase inhibitors
- Presenting how event-driven pharmacology drives potency and selectivity
- Exploiting the PK/PD disconnect for use to further enhance selectivity window in vivo