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Binding and structural analyses of potent inhibitors of the human Ca²⁺/calmodulin dependent protein kinase kinase 2 (CAMKK2) identified from a collection of commercially-available kinase inhibitors.

ABSTRACT: Calcium/Calmodulin-dependent Protein Kinase Kinase 2 (CAMKK2) acts as a signaling hub, receiving signals from various regulatory pathways and decoding them via phosphorylation of downstream protein kinases - such as AMPK (AMP-activated protein kinase) and CAMK types I and IV. CAMKK2 relevance is highlighted by its constitutive activity being implicated in several human pathologies. However, at present, there are no selective small-molecule inhibitors available for this protein kinase. Moreover, CAMKK2 and its closest human homolog, CAMKK1, are thought to have overlapping biological roles. Here we present six new co-structures of potent ligands bound to CAMKK2 identified from a library of commercially-available kinase inhibitors. Enzyme assays confirmed that most of these compounds are equi

SUBMITTER: Profeta GS

PROVIDER: S-EPMC6848146 | biostudies-literature | 2019 Nov

REPOSITORIES: biostudies-literature

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Dataset Information

Binding and structural analyses of potent inhibitors of the human Ca²⁺/calmodulin dependent protein kinase kinase 2 (CAMKK2) identified from a collection of commercially-available kinase inhibitors.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Dataset Information

Binding and structural analyses of potent inhibitors of the human Ca2+/calmodulin dependent protein kinase kinase 2 (CAMKK2) identified from a collection of commercially-available kinase inhibitors.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Binding and structural analyses of potent inhibitors of the human Ca²⁺/calmodulin dependent protein kinase kinase 2 (CAMKK2) identified from a collection of commercially-available kinase inhibitors.