1ocq

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 4: Line 4:
==Overview==
==Overview==
-
Glycosidases are some of the most ubiquitous enzyme in nature. Their, biological significance, coupled to their enormous catalytic prowess, derived from tight binding of the transition state, is reflected in their, importance as therapeutic targets. Many glycosidase inhibitors are known., Imino sugars are often potent inhibitors, yet many facets of their mode of, action, such as their degree, if any, of transition-state "mimicry" and, their protonation state when bound to the target glycosidase remain, unclear. Atomic resolution analysis of the endoglucanase, Cel5A, in, complex with a cellobio-derived isofagomine in conjunction with the pH, dependence of Ki and kcat/KM reveals that this compound binds as a, protonated sugar. Surprisingly, both the enzymatic nucleophile and the, acid/base are unprotonated in the complex.
+
Glycosidases are some of the most ubiquitous enzyme in nature. Their biological significance, coupled to their enormous catalytic prowess derived from tight binding of the transition state, is reflected in their importance as therapeutic targets. Many glycosidase inhibitors are known. Imino sugars are often potent inhibitors, yet many facets of their mode of action, such as their degree, if any, of transition-state "mimicry" and their protonation state when bound to the target glycosidase remain unclear. Atomic resolution analysis of the endoglucanase, Cel5A, in complex with a cellobio-derived isofagomine in conjunction with the pH dependence of Ki and kcat/KM reveals that this compound binds as a protonated sugar. Surprisingly, both the enzymatic nucleophile and the acid/base are unprotonated in the complex.
==About this Structure==
==About this Structure==
Line 14: Line 14:
[[Category: Cellulase]]
[[Category: Cellulase]]
[[Category: Single protein]]
[[Category: Single protein]]
-
[[Category: Davies, G.J.]]
+
[[Category: Davies, G J.]]
[[Category: Macdonald, J.]]
[[Category: Macdonald, J.]]
-
[[Category: Stick, R.V.]]
+
[[Category: Stick, R V.]]
[[Category: Varrot, A.]]
[[Category: Varrot, A.]]
-
[[Category: Withers, S.G.]]
+
[[Category: Withers, S G.]]
[[Category: BGC]]
[[Category: BGC]]
[[Category: GOL]]
[[Category: GOL]]
Line 28: Line 28:
[[Category: hydrolase]]
[[Category: hydrolase]]
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Feb 3 09:56:13 2008''
+
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:16:14 2008''

Revision as of 12:16, 21 February 2008


1ocq, resolution 1.08Å

Drag the structure with the mouse to rotate

COMPLEX OF THE ENDOGLUCANASE CEL5A FROM BACILLUS AGARADHEARANS AT 1.08 ANGSTROM RESOLUTION WITH CELLOBIO-DERIVED ISOFAGOMINE

Overview

Glycosidases are some of the most ubiquitous enzyme in nature. Their biological significance, coupled to their enormous catalytic prowess derived from tight binding of the transition state, is reflected in their importance as therapeutic targets. Many glycosidase inhibitors are known. Imino sugars are often potent inhibitors, yet many facets of their mode of action, such as their degree, if any, of transition-state "mimicry" and their protonation state when bound to the target glycosidase remain unclear. Atomic resolution analysis of the endoglucanase, Cel5A, in complex with a cellobio-derived isofagomine in conjunction with the pH dependence of Ki and kcat/KM reveals that this compound binds as a protonated sugar. Surprisingly, both the enzymatic nucleophile and the acid/base are unprotonated in the complex.

About this Structure

1OCQ is a Single protein structure of sequence from Bacillus agaradhaerens with , , and as ligands. Active as Cellulase, with EC number 3.2.1.4 Known structural/functional Site: . Full crystallographic information is available from OCA.

Reference

Direct observation of the protonation state of an imino sugar glycosidase inhibitor upon binding., Varrot A, Tarling CA, Macdonald JM, Stick RV, Zechel DL, Withers SG, Davies GJ, J Am Chem Soc. 2003 Jun 25;125(25):7496-7. PMID:12812472

Page seeded by OCA on Thu Feb 21 14:16:14 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Personal tools