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Title: Synthesis of montbretin A analogues yields potent competitive inhibitors of human pancreatic α-amylase

Journal Article · · Chemical Science
DOI: https://doi.org/10.1039/C9SC02610J · OSTI ID:1572100
 [1];  [2];  [1];  [1];  [2]; ORCiD logo [1]
  1. Department of Chemistry, University of British Columbia, Vancouver BC, Canada V6T 1Z1
  2. Department of Biochemistry and Molecular Biology, University of British Columbia, Vancouver BC, Canada V6T 1Z3
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Simplified analogues of montbretin A bind similarly to human alpha amylase and with nanomolar affinity.

Sponsoring Organization:
USDOE
OSTI ID:
1572100
Alternate ID(s):
OSTI ID: 1624978
Journal Information:
Chemical Science, Journal Name: Chemical Science Journal Issue: 48 Vol. 10; ISSN 2041-6520; ISSN CSHCBM
Publisher:
Royal Society of Chemistry (RSC)Copyright Statement
Country of Publication:
United Kingdom
Language:
English

References (21)

Inhibition of .ALPHA.-Glucosidase and .ALPHA.-Amylase by Flavonoids journal January 2006
An Update on the Etiology and Epidemiology of Diabetes Mellitus journal November 2006
The amylase inhibitor montbretin A reveals a new glycosidase inhibition motif journal July 2015
Flavonoids for Controlling Starch Digestion: Structural Requirements for Inhibiting Human α-Amylase journal June 2008
The Search for Novel Human Pancreatic α-Amylase Inhibitors: High-Throughput Screening of Terrestrial and Marine Natural Product Extracts journal February 2008
Cloning, mutagenesis, and structural analysis of human pancreatic α-amylase expressed in pichia pastoris journal January 1999
Glucose lowering effect of montbretin A in Zucker Diabetic Fatty rats journal November 2015
Miglitol: A Review of its Therapeutic Potential in Type 2 Diabetes Mellitus journal January 2000
The Role of Acarbose in the Treatment of Non–Insulin-Dependent Diabetes Mellitus journal July 1998
Subsite Mapping of the Human Pancreatic α-Amylase Active Site through Structural, Kinetic, and Mutagenesis Techniques † , ‡ journal April 2000
Acarbose-associated hepatotoxicity journal November 1998
The structure of human pancreatic α -amylase at 1.8 Å resolution and comparisons with related enzymes journal September 1995
The clinical consequences of sucrase-isomaltase deficiency journal February 2016
In Situ Extension as an Approach for Identifying Novel α-Amylase Inhibitors journal August 2004
Efficacy of voglibose in type 2 diabetes journal April 2014
Postprandial hyperglycaemia and α-glucosidase inhibitors journal July 1998
Acarbose Improves Glycemic Control in Overweight Type 2 Diabetic Patients Insufficiently Treated With Metformin journal February 2003
Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors journal May 2009
Preparation of pentafluorophenyl esters of FMOC protected amino acids with pentafluorophenyl trifluoroacetate journal January 1990
Iminosugars past, present and future: medicines for tomorrow journal February 2011
Definition, diagnosis and classification of diabetes mellitus and its complications. Part 1: diagnosis and classification of diabetes mellitus. Provisional report of a WHO Consultation journal July 1998

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