PMID- 36672221
OWN - NLM
STAT- PubMed-not-MEDLINE
DCOM- 20230124
LR  - 20240131
IS  - 2073-4409 (Electronic)
IS  - 2073-4409 (Linking)
VI  - 12
IP  - 2
DP  - 2023 Jan 11
TI  - SGC-CAMKK2-1: A Chemical Probe for CAMKK2.
LID - 10.3390/cells12020287 [doi]
LID - 287
AB  - 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.
FAU - Wells, Carrow
AU  - Wells C
AUID- ORCID: 0000-0003-4799-6792
AD  - Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of 
      North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
FAU - Liang, Yi
AU  - Liang Y
AD  - Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of 
      North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
FAU - Pulliam, Thomas L
AU  - Pulliam TL
AD  - Department of Cancer Systems Imaging, The University of Texas MD Anderson Cancer 
      Center, Houston, TX 77054, USA.
FAU - Lin, Chenchu
AU  - Lin C
AD  - Department of Cancer Systems Imaging, The University of Texas MD Anderson Cancer 
      Center, Houston, TX 77054, USA.
FAU - Awad, Dominik
AU  - Awad D
AD  - Department of Cancer Systems Imaging, The University of Texas MD Anderson Cancer 
      Center, Houston, TX 77054, USA.
FAU - Eduful, Benjamin
AU  - Eduful B
AUID- ORCID: 0000-0002-7923-9975
AD  - Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of 
      North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
FAU - O'Byrne, Sean
AU  - O'Byrne S
AUID- ORCID: 0000-0002-1880-0239
AD  - Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of 
      North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
FAU - Hossain, Mohammad Anwar
AU  - Hossain MA
AUID- ORCID: 0000-0001-8684-8755
AD  - Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of 
      North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
FAU - Catta-Preta, Carolina Moura Costa
AU  - Catta-Preta CMC
AUID- ORCID: 0000-0001-8983-3487
AD  - Centro de Quimica Medicinal (CQMED), Centro de Biologia Molecular e Engenharia 
      Genetica (CBMEG), Universidade Estadual de Campinas (UNICAMP), Campinas 
      13083-886, Brazil.
FAU - Ramos, Priscila Zonzini
AU  - Ramos PZ
AUID- ORCID: 0000-0001-6716-2504
AD  - Centro de Quimica Medicinal (CQMED), Centro de Biologia Molecular e Engenharia 
      Genetica (CBMEG), Universidade Estadual de Campinas (UNICAMP), Campinas 
      13083-886, Brazil.
FAU - Gileadi, Opher
AU  - Gileadi O
AUID- ORCID: 0000-0001-6886-898X
AD  - Centro de Quimica Medicinal (CQMED), Centro de Biologia Molecular e Engenharia 
      Genetica (CBMEG), Universidade Estadual de Campinas (UNICAMP), Campinas 
      13083-886, Brazil.
FAU - Gileadi, Carina
AU  - Gileadi C
AD  - Centro de Quimica Medicinal (CQMED), Centro de Biologia Molecular e Engenharia 
      Genetica (CBMEG), Universidade Estadual de Campinas (UNICAMP), Campinas 
      13083-886, Brazil.
FAU - Counago, Rafael M
AU  - Counago RM
AUID- ORCID: 0000-0003-1847-5090
AD  - Centro de Quimica Medicinal (CQMED), Centro de Biologia Molecular e Engenharia 
      Genetica (CBMEG), Universidade Estadual de Campinas (UNICAMP), Campinas 
      13083-886, Brazil.
FAU - Stork, Brittany
AU  - Stork B
AD  - Department of Molecular and Cellular Biology, Baylor College of Medicine, 
      Houston, TX 77030, USA.
FAU - Langendorf, Christopher G
AU  - Langendorf CG
AD  - St Vincent's Institute of Medical Research, Fitzroy, VIC 3065, Australia.
FAU - Nay, Kevin
AU  - Nay K
AD  - St Vincent's Institute of Medical Research, Fitzroy, VIC 3065, Australia.
AD  - Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Parkville, 
      VIC 3052, Australia.
FAU - Oakhill, Jonathan S
AU  - Oakhill JS
AUID- ORCID: 0000-0002-9475-1440
AD  - St Vincent's Institute of Medical Research, Fitzroy, VIC 3065, Australia.
FAU - Mukherjee, Debarati
AU  - Mukherjee D
AD  - Department of Pharmacology and Cancer Biology, Duke University School of 
      Medicine, Durham, NC 27705, USA.
FAU - Racioppi, Luigi
AU  - Racioppi L
AD  - Department of Medicine, Division of Hematological Malignancies and Cellular 
      Therapy, Duke University School of Medicine, Durham, NC 27710, USA.
AD  - Department of Molecular Medicine and Medical Biotechnology, University of Naples 
      Federico II, 80131 Naples, Italy.
FAU - Means, Anthony R
AU  - Means AR
AD  - Department of Molecular and Cellular Biology, Baylor College of Medicine, 
      Houston, TX 77030, USA.
FAU - York, Brian
AU  - York B
AD  - Department of Molecular and Cellular Biology, Baylor College of Medicine, 
      Houston, TX 77030, USA.
FAU - McDonnell, Donald P
AU  - McDonnell DP
AUID- ORCID: 0000-0002-7331-4700
AD  - Department of Pharmacology and Cancer Biology, Duke University School of 
      Medicine, Durham, NC 27705, USA.
FAU - Scott, John W
AU  - Scott JW
AD  - St Vincent's Institute of Medical Research, Fitzroy, VIC 3065, Australia.
AD  - Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Parkville, 
      VIC 3052, Australia.
AD  - The Florey Institute of Neuroscience and Mental Health, Parkville, VIC 3052, 
      Australia.
FAU - Frigo, Daniel E
AU  - Frigo DE
AUID- ORCID: 0000-0002-0713-471X
AD  - Department of Cancer Systems Imaging, The University of Texas MD Anderson Cancer 
      Center, Houston, TX 77054, USA.
AD  - Department of Genitourinary Medical Oncology, The University of Texas MD Anderson 
      Cancer Center, Houston, TX 77030, USA.
AD  - Center for Nuclear Receptors and Cell Signaling, University of Houston, Houston, 
      TX 77204, USA.
AD  - Department of Biology and Biochemistry, University of Houston, Houston, TX 77204, 
      USA.
FAU - Drewry, David H
AU  - Drewry DH
AUID- ORCID: 0000-0001-5973-5798
AD  - Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of 
      North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
AD  - Lineberger Comprehensive Cancer Center, Department of Medicine, School of 
      Medicine, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, 
      USA.
LA  - eng
GR  - R01CA218442/NH/NIH HHS/United States
GR  - 1U24DK116204-01/NH/NIH HHS/United States
GR  - NIH R01CA184208/NH/NIH HHS/United States
GR  - 106169/ZZ14/Z/WT_/Wellcome Trust/United Kingdom
PT  - Journal Article
PT  - Research Support, N.I.H., Extramural
PT  - Research Support, Non-U.S. Gov't
DEP - 20230111
PL  - Switzerland
TA  - Cells
JT  - Cells
JID - 101600052
SB  - IM
PMC - PMC9856672
OTO - NOTNLM
OT  - CAMKK2
OT  - NanoBRET
OT  - chemical probe
OT  - kinase
OT  - kinase selectivity
COIS- D.E.F. has received research funding from GTx, Inc. and has familial 
      relationships with Hummingbird Bioscience, Maia Biotechnology, Alms Therapeutics, 
      Hinova Pharmaceuticals, and Barricade Therapeutics. The funders had no role in 
      the conceptualization of the study or writing of the manuscript, or in the 
      decision to publish this article. The authors declare no conflict of interest.
EDAT- 2023/01/22 06:00
MHDA- 2023/01/22 06:01
PMCR- 2023/01/11
CRDT- 2023/01/21 01:11
PHST- 2022/11/04 00:00 [received]
PHST- 2022/12/31 00:00 [revised]
PHST- 2023/01/05 00:00 [accepted]
PHST- 2023/01/21 01:11 [entrez]
PHST- 2023/01/22 06:00 [pubmed]
PHST- 2023/01/22 06:01 [medline]
PHST- 2023/01/11 00:00 [pmc-release]
AID - cells12020287 [pii]
AID - cells-12-00287 [pii]
AID - 10.3390/cells12020287 [doi]
PST - epublish
SO  - Cells. 2023 Jan 11;12(2):287. doi: 10.3390/cells12020287.