Distortion of a cellobio-derived isofagomine highlights the potential conformational itinerary of inverting beta-glucosidases

A  Varrot; J  Macdonald; R V  Stick; G  Pell; H J  Gilbert; G J  Davies

doi:10.1039/b301592k

Distortion of a cellobio-derived isofagomine highlights the potential conformational itinerary of inverting beta-glucosidases

A Varrot, J Macdonald, R V Stick, G Pell, H J Gilbert, G J Davies

Chemistry

Research output: Contribution to journal › Article › peer-review

Abstract

A cellobio-derived isofagomine glycosidase inhibitor (K-i similar to 400 nM) displays an unusual distorted B-2,B-5 (boat) conformation upon binding to cellobiohydrolase Cel6A from Humicola insolens, highlighting the different conformational itineraries used by various glycosidases, with consequences for the design of therapeutic agents.

Original language	English
Pages (from-to)	946-947
Number of pages	2
Journal	Chemical Communications
Issue number	8
DOIs	https://doi.org/10.1039/b301592k
Publication status	Published - 2003

Keywords

HUMICOLA-INSOLENS CELLOBIOHYDROLASE
B-2,B-5 CONFORMATION
TRICHODERMA-REESEI
ACTIVE-SITE
SUBSTRATE
CEL6A
HYDROLYSIS
CATALYSIS
ANGSTROM
COMPLEX

Access to Document

10.1039/b301592k

Cite this

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title = "Distortion of a cellobio-derived isofagomine highlights the potential conformational itinerary of inverting beta-glucosidases",

abstract = "A cellobio-derived isofagomine glycosidase inhibitor (K-i similar to 400 nM) displays an unusual distorted B-2,B-5 (boat) conformation upon binding to cellobiohydrolase Cel6A from Humicola insolens, highlighting the different conformational itineraries used by various glycosidases, with consequences for the design of therapeutic agents.",

keywords = "HUMICOLA-INSOLENS CELLOBIOHYDROLASE, B-2,B-5 CONFORMATION, TRICHODERMA-REESEI, ACTIVE-SITE, SUBSTRATE, CEL6A, HYDROLYSIS, CATALYSIS, ANGSTROM, COMPLEX",

author = "A Varrot and J Macdonald and Stick, {R V} and G Pell and Gilbert, {H J} and Davies, {G J}",

year = "2003",

doi = "10.1039/b301592k",

language = "English",

pages = "946--947",

journal = "Chemical Communications",

issn = "1359-7345",

publisher = "The Royal Society of Chemistry",

number = "8",

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T1 - Distortion of a cellobio-derived isofagomine highlights the potential conformational itinerary of inverting beta-glucosidases

AU - Varrot, A

AU - Macdonald, J

AU - Stick, R V

AU - Pell, G

AU - Gilbert, H J

AU - Davies, G J

PY - 2003

Y1 - 2003

N2 - A cellobio-derived isofagomine glycosidase inhibitor (K-i similar to 400 nM) displays an unusual distorted B-2,B-5 (boat) conformation upon binding to cellobiohydrolase Cel6A from Humicola insolens, highlighting the different conformational itineraries used by various glycosidases, with consequences for the design of therapeutic agents.

AB - A cellobio-derived isofagomine glycosidase inhibitor (K-i similar to 400 nM) displays an unusual distorted B-2,B-5 (boat) conformation upon binding to cellobiohydrolase Cel6A from Humicola insolens, highlighting the different conformational itineraries used by various glycosidases, with consequences for the design of therapeutic agents.

KW - HUMICOLA-INSOLENS CELLOBIOHYDROLASE

KW - B-2,B-5 CONFORMATION

KW - TRICHODERMA-REESEI

KW - ACTIVE-SITE

KW - SUBSTRATE

KW - CEL6A

KW - HYDROLYSIS

KW - CATALYSIS

KW - ANGSTROM

KW - COMPLEX

U2 - 10.1039/b301592k

DO - 10.1039/b301592k

M3 - Article

SN - 1359-7345

SP - 946

EP - 947

JO - Chemical Communications

JF - Chemical Communications

IS - 8

ER -