1R5G

Crystal Structure of MetAP2 complexed with A311263

Summary for 1R5G

• Entry DOI: 10.2210/pdb1r5g/pdb
• Related: 1R58 1R5H
• Descriptor: Methionine aminopeptidase 2, MANGANESE (II) ION, (2S,3R)-3-AMINO-2-HYDROXY-5-(ETHYLSULFANYL)PENTANOYL-((S)-(-)-(1-NAPHTHYL)ETHYL)AMIDE, ... (4 entities in total)
• Functional Keywords: hydrolase
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 1
• Total formula weight: 41826.37

Authors

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. (deposition date: 2003-10-10, release date: 2004-10-12, Last modification date: 2024-10-16)

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

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: 15012983
DOI: 10.1016/j.bmcl.2003.12.031

Experimental method

X-RAY DIFFRACTION (2 Å)