2. Academic Validation
  3. SGC-CAMKK2-1: A Chemical Probe for CAMKK2

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

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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