Science. 1989 Mar 10;243(4896):1346-51.

Structure of recombinant human renin, a target for cardiovascular-active drugs, at 2.5 A resolution.

Sielecki AR, Hayakawa K, Fujinaga M, Murphy ME, Fraser M, Muir AK, Carilli CT, Lewicki JA, Baxter JD, James MN.

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Department of Biochemistry, University of Alberta, Edmonton, Canada.

Abstract

The x-ray crystal structure of recombinant human renin has been determined. Molecular dynamics techniques that included crystallographic data as a restraint were used to improve an initial model based on porcine pepsinogen. The present agreement factor for data from 8.0 to 2.5 angstroms (A) is 0.236. Some of the surface loops are poorly determined, and these disordered regions border a 30 A wide solvent channel. Comparison of renin with other aspartyl proteinases shows that, although the structural cores and active sites are highly conserved, surface residues, some of which are critical for specificity, vary greatly (up to 10A). Knowledge of the actual structure, as opposed to the use of models based on related enzymes, should facilitate the design of renin inhibitors.

PMID:: 2493678; [PubMed - indexed for MEDLINE]

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X-ray analyses of aspartic proteinases. II. Three-dimensional structure of the hexagonal crystal form of porcine pepsin at 2.3 A resolution. [J Mol Biol. 1990]
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Review [Various aspects of structural studies of aspartate proteinases].
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Cited by 14 PubMed Central articles

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Structures reported by this article

Structure Of Recombinant Human Renin, A Target For Cardiovascular-Active Drugs, At 2.5 Angstroms Resolution

PDB: 2REN

Source: Homo sapiens

Method: X-Ray Diffraction

Resolution: 2.5 Å

See all 2 structures...

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