Crystal structure of human proto-oncogene serine threonine kinase (PIM1) in complex with a consensus peptide and a pyrrolo[2,3-a]carbazole ligand
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Crystal structure of human proto-oncogene serine threonine kinase (PIM1) in complex with a consensus peptide and a pyrrolo[2,3-a]carbazole ligand Descriptor: 1,10-dihydropyrrolo[2,3-a]carbazole-3-carbaldehyde, Peptide (PIMTIDE) ARKRRRHPSGPPTA, Proto-oncogene serine/threonine-protein kinase Pim-1 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) Deposit date: 2009-09-04 Release date: 2009-10-27 Last modified: 2023-09-06 Method: X-RAY DIFFRACTION (2.35 Å) Cite: Synthesis, kinase inhibitory potencies, and in vitro antiproliferative evaluation of new pim kinase inhibitors. J.Med.Chem., 52, 2009
人原癌基因丝氨酸/苏氨酸激酶(PIM1)与共有肽段及吡咯并[2,3-a]咔唑类配体结合的共晶结构
描述:1,10-二氢吡咯并[2,3-a]咔唑-3-甲醛、肽段(PIMTIDE)ARKRRRHPSGPPTA与原癌基因丝氨酸/苏氨酸蛋白激酶Pim-1
作者: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,结构基因组学联盟(Structural Genomics Consortium, SGC)
提交日期:2009-09-04;发布日期:2009-10-27;最后修改日期:2023-09-06
实验方法:X射线衍射(分辨率2.35 Å)
引用文献:《新型PIM激酶抑制剂的合成、激酶抑制活性及体外抗增殖评价》,《药物化学杂志》(J.Med.Chem.),52卷,2009年
创建时间:
2009-09-04



