RAS TDD Resource Page
Welcome to our resource page for the 2nd RAS Targeted Drug Development (TDD) Summit. Because we won’t be able to meet you in person, explore this page for information and resources about kinase biology, target engagement, protein degradation and more. Learn how we can support your research with our products and technologies.
A Comprehensive Live-Cell Target Engagement Approach for the RAS-RAF-MEK-ERK Pathway
Presented by Matt Robers, Senior Research Scientist, Promega Corporation
As a driver of tumorigenesis in a variety of cell types, the RAS-mapk pathway has been the subject of concerted drug discovery efforts for decades. Here we will present the use of NanoBRET™-TE to quantify live cell target engagement to all of the described drug binding sites within the RAS-RAF-MEK-ERK pathway. With this method, we can observe the impact of oncogenic KRAS (G12C) on engagement potency on downstream effectors including BRAF. We have also developed a pan-KRAS NanoBRET™ tracer that has the capacity to detect a variety of orthosteric and allosteric engagement mechanisms at this challenging target, previously deemed “undruggable”.
- Development of a pan-RAS target engagement assay for querying multiple inhibitory mechanisms
- Real-time analysis of engagement and protein-protein interactions at RAS and its effector proteins
- The landscape of engagement selectivity and drug residence time for the mapk pathway in the presence of active KRAS
Resources for Drug Discovery
Small-Molecule Drug Discovery
Our comprehensive collection of products and services for small-molecule drug discovery will help to accelerate your workflow.
Assay Development and Services
Let our team of experts guide you through customized solutions for your drug discovery workflow, with application-specific designs and and automation options.
Study protein degradation in live cells from compound cell permeability and E3 ligase engagement to target degradation. Learn about the comprehensive selection of CRISPR-edited cell line pools and clones to facilitate studying popular protein degradation targets that Promega has to offer.
Promega offers biochemical assays for inhibitor screening, kinase-ligand binding assays in live cells and custom kinase assay services. Our bioluminescent assays are available to query the ability of compounds to bind or inhibit kinases in biochemical and cellular formats.
CRISPR Cas9 Knock-in Tagging
CRISPR/Cas9 knock-in tagging offers a convenient method to study endogenous biology, without the drawbacks of overexpression methods. Promega offers a comprehensive selection of CRISPR-edited cell line pools and clones for popular drug targets and cell backgrounds.
Measure compound-target residence time and screen inhibitor panels with sensitive, live-cell binding assays that use an energy transfer technique to measure molecular proximity.
Using high-throughput assays from Promega, you can perform comparative analysis by multiplexing assays with other measures of cell health, such as apoptosis and autophagy. Check out our complete offering of cell health screening assays.