3JPV

Crystal structure of human proto-oncogene serine threonine kinase (PIM1) in complex with a consensus peptide and a pyrrolo[2,3-a]carbazole ligand

Summary for 3JPV

• Entry DOI: 10.2210/pdb3jpv/pdb
• Descriptor: Proto-oncogene serine/threonine-protein kinase Pim-1, Peptide (PIMTIDE) ARKRRRHPSGPPTA, 1,10-dihydropyrrolo[2,3-a]carbazole-3-carbaldehyde, ... (4 entities in total)
• Functional Keywords: oncogene, kinase, serine-threonine, pim1, pyrrolo[2, 3-a]carbazole, structural genomics consortium, sgc, alternative initiation, atp-binding, cell membrane, manganese, membrane, metal-binding, nucleotide-binding, nucleus, phosphoprotein, proto-oncogene, serine/threonine-protein kinase, transferase, transferase - transferase inhibitor complex, transferase / transferase inhibitor
• Biological source: Homo sapiens (human)
• Cellular location: Isoform 2: Cytoplasm. Isoform 1: Cell membrane: P11309
• Total number of polymer chains: 2
• Total formula weight: 37417.60

Authors

Filippakopoulos, P.,Bullock, A.N.,Fedorov, O.,Akue-Gedu, R.,Rossignol, E.,Azzaro, S.,Bain, J.,Cohen, P.,Prudhomme, M.,Moreau, P.,Amizon, F.,von Delft, F.,Arrowsmith, C.H.,Weigelt, J.,Edwards, A.,Bountra, C.,Knapp, S.,Structural Genomics Consortium (SGC) (deposition date: 2009-09-04, release date: 2009-10-27, Last modification date: 2023-09-06)

• Primary citation: Akue-Gedu, R.,Rossignol, E.,Azzaro, S.,Knapp, S.,Filippakopoulos, P.,Bullock, A.N.,Bain, J.,Cohen, P.,Prudhomme, M.,Anizon, F.,Moreau, P.; Synthesis, kinase inhibitory potencies, and in vitro antiproliferative evaluation of new pim kinase inhibitors.; J.Med.Chem., 52:6369-6381, 2009; PubMed: 19788246; DOI: 10.1021/jm901018f

Experimental method

X-RAY DIFFRACTION (2.35 Å)