Structural highlights
2xhm is a 1 chain structure with sequence from Drosophila melanogaster. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
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| Ligands: | , , , , , |
| Related: | 1j38, 2x94, 2x8z, 1j36, 2x8y, 2x91, 2x95, 2x96, 2x92, 2x93, 2x97, 2x90, 1j37 |
| Activity: | Peptidyl-dipeptidase A, with EC number 3.4.15.1 |
| Resources: | FirstGlance, OCA, RCSB, PDBsum |
Function
[ACE_DROME] May be involved in the specific maturation or degradation of a number of bioactive peptides. May play a role in the contractions of the heart, gut and testes, and in spermatid differentiation.[1]
Evolutionary Conservation
Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.
Publication Abstract from PubMed
Angiotensin-I converting enzyme (ACE, a zinc dependent dipeptidyl carboxypeptidase) is a major target of drugs due to its role in the modulation of blood pressure and cardiovascular disorders. Here we present a crystal structure of AnCE (an ACE homologue from Drosophila melanogaster with a single enzymatic domain) in complex with a natural product-phosphonotripeptide, K-26 at 1.96A resolution. The inhibitor binds exclusively in the S(1) and S(2) binding pockets of AnCE (coordinating the zinc ion) through ionic and hydrogen bond interactions. A detailed structural comparison of AnCE.K-26 complex with individual domains of human somatic ACE provides useful information for further exploration of ACE inhibitor pharmacophores involving phosphonic acids.
Crystal structure of a phosphonotripeptide K-26 in complex with angiotensin converting enzyme homologue (AnCE) from Drosophila melanogaster.,Akif M, Ntai I, Sturrock ED, Isaac RE, Bachmann BO, Acharya KR Biochem Biophys Res Commun. 2010 Jul 30;398(3):532-6. Epub 2010 Jul 1. PMID:20599761[2]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Hurst D, Rylett CM, Isaac RE, Shirras AD. The drosophila angiotensin-converting enzyme homologue Ance is required for spermiogenesis. Dev Biol. 2003 Feb 15;254(2):238-47. PMID:12591244
- ↑ Akif M, Ntai I, Sturrock ED, Isaac RE, Bachmann BO, Acharya KR. Crystal structure of a phosphonotripeptide K-26 in complex with angiotensin converting enzyme homologue (AnCE) from Drosophila melanogaster. Biochem Biophys Res Commun. 2010 Jul 30;398(3):532-6. Epub 2010 Jul 1. PMID:20599761 doi:10.1016/j.bbrc.2010.06.113
