1R58
Crystal Structure of MetAP2 complexed with A357300
Summary for 1R58
| Entry DOI | 10.2210/pdb1r58/pdb |
| Related | 1r5g 1r5h |
| Descriptor | Methionine aminopeptidase 2, MANGANESE (II) ION, N'-((2S,3R)-3-AMINO-2-HYDROXY-5-(ISOPROPYLSULFANYL)PENTANOYL)-N-3-CHLOROBENZOYL HYDRAZIDE, ... (4 entities in total) |
| Functional Keywords | hydrolase |
| Biological source | Homo sapiens (human) |
| Total number of polymer chains | 1 |
| Total formula weight | 41839.75 |
| Authors | Sheppard, G.S.,Wang, J.,Kawai, M.,BaMaung, N.Y.,Craig, R.A.,Ericken, S.A.,Lynch, L.,Patel, J.,Yang, F.,Searle, X.B.,Lou, P.,Park, C.,Kim, K.H.,Henkin, J.,Lesniewski, R. (deposition date: 2003-10-09, release date: 2004-10-12, Last modification date: 2024-11-06) |
| Primary citation | Sheppard, G.S.,Wang, J.,Kawai, M.,BaMaung, N.Y.,Craig, R.A.,Erickson, S.A.,Lynch, L.,Patel, J.,Yang, F.,Searle, X.B.,Lou, P.,Park, C.,Kim, K.H.,Henkin, J.,Lesniewski, R. 3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2. Bioorg.Med.Chem.Lett., 14:865-868, 2004 Cited by PubMed Abstract: Substituted 3-amino-2-hydroxyamides and related hydroxyamides and acylhydrazines were identified as inhibitors of human methionine aminopeptidase-2 (MetAP2). Examination of substituents through parallel synthesis and iterative structure-based design allowed the identification of potent inhibitors with good selectivity against MetAP1. Diacylhydrazine 3t (A-357300) was identified as an analogue displaying inhibition of methionine processing and cellular proliferation in human microvascular endothelial cells (HMVEC). PubMed: 15012983DOI: 10.1016/j.bmcl.2003.12.031 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (1.9 Å) |
Structure validation
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