SGC-CAMKK2-1: A Chemical Probe for CAMKK2

  • Cells. 2023 Jan 11;12(2):287. doi: 10.3390/cells12020287.
Carrow Wells  1 ,  Yi Liang  1 ,  Thomas L Pulliam  2 ,  Chenchu Lin  2 ,  Dominik Awad  2 ,  Benjamin Eduful  1 ,  Sean O'Byrne  1 ,  Mohammad Anwar Hossain  1 ,  Carolina Moura Costa Catta-Preta  3 ,  Priscila Zonzini Ramos  3 ,  Opher Gileadi  3 ,  Carina Gileadi  3 ,  Rafael M Couñago  3 ,  Brittany Stork  4 ,  Christopher G Langendorf  5 ,  Kevin Nay  5  6 ,  Jonathan S Oakhill  5 ,  Debarati Mukherjee  7 ,  Luigi Racioppi  8  9 ,  Anthony R Means  4 ,  Brian York  4 ,  Donald P McDonnell  7 ,  John W Scott  5  6  10 ,  Daniel E Frigo  2  11  12  13 ,  David H Drewry  1  14
Affiliations
  • 1. Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
  • 2. Department of Cancer Systems Imaging, The University of Texas MD Anderson Cancer Center, Houston, TX 77054, USA.
  • 3. Centro de Química Medicinal (CQMED), Centro de Biologia Molecular e Engenharia Genética (CBMEG), Universidade Estadual de Campinas (UNICAMP), Campinas 13083-886, Brazil.
  • 4. Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, TX 77030, USA.
  • 5. St Vincent's Institute of Medical Research, Fitzroy, VIC 3065, Australia.
  • 6. Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Parkville, VIC 3052, Australia.
  • 7. Department of Pharmacology and Cancer Biology, Duke University School of Medicine, Durham, NC 27705, USA.
  • 8. Department of Medicine, Division of Hematological Malignancies and Cellular Therapy, Duke University School of Medicine, Durham, NC 27710, USA.
  • 9. Department of Molecular Medicine and Medical Biotechnology, University of Naples Federico II, 80131 Naples, Italy.
  • 10. The Florey Institute of Neuroscience and Mental Health, Parkville, VIC 3052, Australia.
  • 11. Department of Genitourinary Medical Oncology, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA.
  • 12. Center for Nuclear Receptors and Cell Signaling, University of Houston, Houston, TX 77204, USA.
  • 13. Department of Biology and Biochemistry, University of Houston, Houston, TX 77204, USA.
  • 14. Lineberger Comprehensive Cancer Center, Department of Medicine, School of Medicine, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
PMID: 36672221 DOI: 10.3390/cells12020287
Abstract

The serine/threonine protein kinase calcium/calmodulin-dependent protein kinase kinase 2 (CaMKK2) plays critical roles in a range of biological processes. Despite its importance, only a handful of inhibitors of CaMKK2 have been disclosed. Having a selective small molecule tool to interrogate this kinase will help demonstrate that CaMKK2 inhibition can be therapeutically beneficial. Herein, we disclose SGC-CAMKK2-1, a selective chemical probe that targets CaMKK2.

Keywords
CAMKK2; NanoBRET; chemical probe; kinase; kinase selectivity.
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