2vmf: Difference between revisions

From Proteopedia
Jump to navigation Jump to search
No edit summary
No edit summary
Line 1: Line 1:
[[Image:2vmf.jpg|left|200px]]
{{Seed}}
[[Image:2vmf.png|left|200px]]


<!--
<!--
Line 9: Line 10:
{{STRUCTURE_2vmf|  PDB=2vmf  |  SCENE=  }}  
{{STRUCTURE_2vmf|  PDB=2vmf  |  SCENE=  }}  


'''STRUCTURAL AND BIOCHEMICAL EVIDENCE FOR A BOAT-LIKE TRANSITION STATE IN BETA-MANNOSIDASES'''
===STRUCTURAL AND BIOCHEMICAL EVIDENCE FOR A BOAT-LIKE TRANSITION STATE IN BETA-MANNOSIDASES===




==Overview==
<!--  
Enzyme inhibition through mimicry of the transition state is a major area for the design of new therapeutic agents. Emerging evidence suggests that many retaining glycosidases that are active on alpha- or beta-mannosides harness unusual B2,5 (boat) transition states. Here we present the analysis of 25 putative beta-mannosidase inhibitors, whose Ki values range from nanomolar to millimolar, on the Bacteroides thetaiotaomicron beta-mannosidase BtMan2A. B2,5 or closely related conformations were observed for all tightly binding compounds. Subsequent linear free energy relationships that correlate log Ki with log Km/kcat for a series of active center variants highlight aryl-substituted mannoimidazoles as powerful transition state mimics in which the binding energy of the aryl group enhances both binding and the degree of transition state mimicry. Support for a B2,5 transition state during enzymatic beta-mannosidase hydrolysis should also facilitate the design and exploitation of transition state mimics for the inhibition of retaining alpha-mannosidases--an area that is emerging for anticancer therapeutics.
The line below this paragraph, {{ABSTRACT_PUBMED_18408714}}, adds the Publication Abstract to the page
(as it appears on PubMed at http://www.pubmed.gov), where 18408714 is the PubMed ID number.
-->
{{ABSTRACT_PUBMED_18408714}}


==About this Structure==
==About this Structure==
Line 40: Line 44:
[[Category: Mannosidase]]
[[Category: Mannosidase]]
[[Category: Transition state mimic]]
[[Category: Transition state mimic]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Apr 24 09:30:49 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 02:16:43 2008''

Revision as of 02:16, 29 July 2008

File:2vmf.png

Template:STRUCTURE 2vmf

STRUCTURAL AND BIOCHEMICAL EVIDENCE FOR A BOAT-LIKE TRANSITION STATE IN BETA-MANNOSIDASESSTRUCTURAL AND BIOCHEMICAL EVIDENCE FOR A BOAT-LIKE TRANSITION STATE IN BETA-MANNOSIDASES

Template:ABSTRACT PUBMED 18408714

About this StructureAbout this Structure

2VMF is a Single protein structure of sequence from Bacteroides thetaiotaomicron. Full crystallographic information is available from OCA.

ReferenceReference

Structural and biochemical evidence for a boat-like transition state in beta-mannosidases., Tailford LE, Offen WA, Smith NL, Dumon C, Morland C, Gratien J, Heck MP, Stick RV, Bleriot Y, Vasella A, Gilbert HJ, Davies GJ, Nat Chem Biol. 2008 May;4(5):306-12. PMID:18408714

Page seeded by OCA on Tue Jul 29 02:16:43 2008

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

OCA