Crystal Structure-Guided Design of Bisubstrate Inhibitors and Photoluminescent Probes for Protein Kinases of the PIM Family.


Journal

Molecules (Basel, Switzerland)
ISSN: 1420-3049
Titre abrégé: Molecules
Pays: Switzerland
ID NLM: 100964009

Informations de publication

Date de publication:
19 Jul 2021
Historique:
received: 01 06 2021
revised: 09 07 2021
accepted: 14 07 2021
entrez: 24 7 2021
pubmed: 25 7 2021
medline: 18 9 2021
Statut: epublish

Résumé

We performed an X-ray crystallographic study of complexes of protein kinase PIM-1 with three inhibitors comprising an adenosine mimetic moiety, a linker, and a peptide-mimetic (d-Arg)

Identifiants

pubmed: 34299628
pii: molecules26144353
doi: 10.3390/molecules26144353
pmc: PMC8307404
pii:
doi:

Substances chimiques

Carbocyanines 0
Fluorescent Dyes 0
Peptidomimetics 0
Protein Kinase Inhibitors 0
cyanine dye 5 0
PIM1 protein, human EC 2.7.11.1
Proto-Oncogene Proteins c-pim-1 EC 2.7.11.1

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Subventions

Organisme : Eesti Teadusagentuur
ID : PRG454
Organisme : Eesti Teadusagentuur
ID : PSG230
Organisme : Medical Research Council and the Nuffield Department of Medicine, University of Oxford
ID : NDM Prize Studentship
Organisme : German translational cancer network
ID : (DKTK)
Organisme : Frankfurt Cancer Institute
ID : (FCI)
Organisme : Genome Canada through Ontario Genomics Institute
ID : OGI-196
Organisme : EU/EFPIA/OICR/McGill/KTH/Diamond
ID : SGC no. 1097737
Organisme : Innovative Medicines Initiative 2 Joint Undertaking EUbOPEN
ID : 875510
Organisme : Wellcome Trust
ID : 106169/ZZ14/Z
Pays : United Kingdom

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Auteurs

Olivier E Nonga (OE)

Institute of Chemistry, University of Tartu, 14A Ravila St., 50411 Tartu, Estonia.

Darja Lavogina (D)

Institute of Chemistry, University of Tartu, 14A Ravila St., 50411 Tartu, Estonia.

Erki Enkvist (E)

Institute of Chemistry, University of Tartu, 14A Ravila St., 50411 Tartu, Estonia.

Katrin Kestav (K)

Institute of Chemistry, University of Tartu, 14A Ravila St., 50411 Tartu, Estonia.

Apirat Chaikuad (A)

Institut für Pharmazeutische Chemie, Goethe University Frankfurt am Main, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.
Structural Genomics Consortium (SGC), Buchmann Institute for Life Sciences, Goethe University Frankfurt, Max-von-Laue-Str. 15, 60438 Frankfurt am Main, Germany.

Sarah E Dixon-Clarke (SE)

Centre for Medicines Discovery, Old Road Campus, University of Oxford, Roosevelt Drive, Oxford OX3 7DQ, UK.
Department of Cancer Biology, Dana-Farber Cancer Institute, 450 Brookline Avenue, Boston, MA 02215, USA.

Alex N Bullock (AN)

Centre for Medicines Discovery, Old Road Campus, University of Oxford, Roosevelt Drive, Oxford OX3 7DQ, UK.

Sergei Kopanchuk (S)

Institute of Chemistry, University of Tartu, 14A Ravila St., 50411 Tartu, Estonia.

Taavi Ivan (T)

Institute of Chemistry, University of Tartu, 14A Ravila St., 50411 Tartu, Estonia.

Ramesh Ekambaram (R)

Institute of Chemistry, University of Tartu, 14A Ravila St., 50411 Tartu, Estonia.

Kaido Viht (K)

Institute of Chemistry, University of Tartu, 14A Ravila St., 50411 Tartu, Estonia.

Stefan Knapp (S)

Institut für Pharmazeutische Chemie, Goethe University Frankfurt am Main, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.
Structural Genomics Consortium (SGC), Buchmann Institute for Life Sciences, Goethe University Frankfurt, Max-von-Laue-Str. 15, 60438 Frankfurt am Main, Germany.

Asko Uri (A)

Institute of Chemistry, University of Tartu, 14A Ravila St., 50411 Tartu, Estonia.

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Classifications MeSH