The Kinase Chemogenomic Set (KCGS)
- Institute The University of North Carolina at Chapel Hill ; Structural Genomics Consortium (SGC)
Tool name: The Kinase Chemogenomic Set (KCGS)
Tool type: Small molecules
Description: Designed to study the biology of dark kinases from the human genome.
Background and Research Application
The Kinase Chemogenomic Set (KCGS) is the most diverse and highly annotated, publicly-available collection of kinase inhibitors. Version 1.0 of the set contains 187 kinase inhibitors sourced from eight pharma companies and academic laboratories with potent activity on 215 human kinases. Sets like KCGS can help identify medically important kinases and allow the synthesis of high-quality chemical probes for high priority dark kinases of therapeutic interest.
Dark kinases are those which are difficult to characterise, have little biological information gathered and their medical potential is unreached/untested. The goal of the KCGS is to generate, systematize and disseminate knowledge about dark kinases, biological networks in which they function and connections to cellular phenotypes and human disease. There is a vast array of small molecule drugs, including at least 38 cancer therapies, which function by inhibiting the action of protein kinases, or similar lipid kinases. An enhanced understanding of signalling networks, particularly those which control the immune system, should eventually lead to drug discoveries.
The KCGS aims to: (i) establish a knowledgebase covering the approximately 160 poorly understood dark kinases, (ii) distil primary data into functional biochemical and biological information and promote further research using genetic and chemical tools, which they are also developing and making available, (iii) place dark kinases within a new and emerging network-level understanding of cell signalling and physiology and (iv) identify those dark kinases whose mutation or mis-regulation is associated with human disease, making them possible therapeutic targets. The KCGS, is a collection of narrow spectrum, small molecule kinase inhibitors that has been assembled by the SGC-UNC to study the biology of dark kinases.
Research area: Cancer
- For Research Use Only
- • KCGS FAQs
- • The Kinase Chemogenomic Set (KCGS): An open science resource for kinase vulnerability identification
- • Burdova et al. 2019. EMBO J. 38(20):e101443. PMID: 31424118.
- • Wells et al. 2018. Medchemcomm. 9(1):44-66. PMID: 30108900.
- • Drewry et al. 2017. PLoS One. 12(8):e0181585. PMID: 28767711.