2GA2

h-MetAP2 complexed with A193400

Summary for 2GA2

• Entry DOI: 10.2210/pdb2ga2/pdb
• Descriptor: Methionine aminopeptidase 2, MANGANESE (II) ION, 5-BROMO-2-{[(4-CHLOROPHENYL)SULFONYL]AMINO}BENZOIC ACID, ... (4 entities in total)
• Functional Keywords: complex, hydrolase
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 1
• Total formula weight: 41870.52

Authors

Park, C. (deposition date: 2006-03-07, release date: 2007-03-13, Last modification date: 2024-10-30)

Primary citation

Kawai, M.,BaMaung, N.Y.,Fidanze, S.D.,Erickson, S.A.,Tedrow, J.S.,Sanders, W.J.,Vasudevan, A.,Park, C.,Hutchins, C.,Comess, K.M.,Kalvin, D.,Wang, J.,Zhang, Q.,Lou, P.,Tucker-Garcia, L.,Bouska, J.,Bell, R.L.,Lesniewski, R.,Henkin, J.,Sheppard, G.S.
Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.
Bioorg.Med.Chem.Lett., 16:3574-3577, 2006

PubMed Abstract: We have screened molecules for inhibition of MetAP2 as a novel approach toward antiangiogenesis and anticancer therapy using affinity selection/mass spectrometry (ASMS) employing MetAP2 loaded with Mn(2+) as the active site metal. After a series of anthranilic acid sulfonamides with micromolar affinities was identified, chemistry efforts were initiated. The micromolar hits were quickly improved to potent nanomolar inhibitors by chemical modifications guided by insights from X-ray crystallography.

PubMed: 16632353
DOI: 10.1016/j.bmcl.2006.03.085

Experimental method

X-RAY DIFFRACTION (1.95 Å)