2boa
From Proteopedia
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==Overview== | ==Overview== | ||
| - | Treatment of advanced stages of prostate carcinoma with | + | Treatment of advanced stages of prostate carcinoma with histone-deacetylase inhibitors entails expression of human procarboxypeptidase-A4 (hPCPA4). The three-dimensional structure of hPCPA4 has been solved and shows the features of related metallocarboxypeptidase zymogens, with a preformed alpha/beta/-hydrolase active-enzyme moiety (hCPA4) and an inhibiting pro-domain (PD). The protease moiety recalls a sphere, out of which a spherical cone has been cut. This results in a funnel-like structure, at the bottom of which the active-site cleft resides. The border of this funnel is shaped by loops, which are responsible for the interaction with the PD, characterised by a large interface area and relatively few contacts. Such an inhibitory mode is evocative of the recently reported structure of the human inhibitor latexin in its complex with hCPA4. The main contacting structure of latexin is similar to the one employed for PD inhibition. In both cases, active-site blocking relies mainly on a loop provided by the central part of a beta sheet. |
==About this Structure== | ==About this Structure== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Aviles, F | + | [[Category: Aviles, F X.]] |
[[Category: Bonet-Figueredo, R.]] | [[Category: Bonet-Figueredo, R.]] | ||
[[Category: Garcia-Castellanos, R.]] | [[Category: Garcia-Castellanos, R.]] | ||
| - | [[Category: Gomis-Ruth, F | + | [[Category: Gomis-Ruth, F X.]] |
[[Category: Pallares, I.]] | [[Category: Pallares, I.]] | ||
[[Category: Vendrell, J.]] | [[Category: Vendrell, J.]] | ||
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[[Category: zymogen]] | [[Category: zymogen]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:39:52 2008'' |
Revision as of 14:39, 21 February 2008
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HUMAN PROCARBOXYPEPTIDASE A4.
Overview
Treatment of advanced stages of prostate carcinoma with histone-deacetylase inhibitors entails expression of human procarboxypeptidase-A4 (hPCPA4). The three-dimensional structure of hPCPA4 has been solved and shows the features of related metallocarboxypeptidase zymogens, with a preformed alpha/beta/-hydrolase active-enzyme moiety (hCPA4) and an inhibiting pro-domain (PD). The protease moiety recalls a sphere, out of which a spherical cone has been cut. This results in a funnel-like structure, at the bottom of which the active-site cleft resides. The border of this funnel is shaped by loops, which are responsible for the interaction with the PD, characterised by a large interface area and relatively few contacts. Such an inhibitory mode is evocative of the recently reported structure of the human inhibitor latexin in its complex with hCPA4. The main contacting structure of latexin is similar to the one employed for PD inhibition. In both cases, active-site blocking relies mainly on a loop provided by the central part of a beta sheet.
About this Structure
2BOA is a Single protein structure of sequence from Homo sapiens with , and as ligands. Known structural/functional Site: . Full crystallographic information is available from OCA.
Reference
Detailed molecular comparison between the inhibition mode of A/B-type carboxypeptidases in the zymogen state and by the endogenous inhibitor latexin., Garcia-Castellanos R, Bonet-Figueredo R, Pallares I, Ventura S, Aviles FX, Vendrell J, Gomis-Rutha FX, Cell Mol Life Sci. 2005 Sep;62(17):1996-2014. PMID:16091843
Page seeded by OCA on Thu Feb 21 16:39:52 2008
Categories: Homo sapiens | Single protein | Aviles, F X. | Bonet-Figueredo, R. | Garcia-Castellanos, R. | Gomis-Ruth, F X. | Pallares, I. | Vendrell, J. | Ventura, S. | GOL | NAG | ZN | Carboxypeptidase | Exopropeptidase | Hydrolase | Metalloprocarboxypeptidase | Metalloprotease | X-ray crystal structure | Zymogen
