Menu
×
West Ashley Library
9 a.m. - 7 p.m.
Phone: (843) 766-6635
Folly Beach Library
Closed
Phone: (843) 588-2001
Edgar Allan Poe/Sullivan's Island Library
Closed for renovations
Phone: (843) 883-3914
Wando Mount Pleasant Library
9 a.m. - 8 p.m.
Phone: (843) 805-6888
Village Library
9 a.m. - 1 p.m.
Phone: (843) 884-9741
St. Paul's/Hollywood Library
9 a.m. - 8 p.m.
Phone: (843) 889-3300
Otranto Road Library
9 a.m. - 8 p.m.
Phone: (843) 572-4094
Mt. Pleasant Library
9 a.m. - 8 p.m.
Phone: (843) 849-6161
McClellanville Library
9 a.m. - 6 p.m.
Phone: (843) 887-3699
Keith Summey North Charleston Library
9 a.m. - 8 p.m.
Phone: (843) 744-2489
John's Island Library
9 a.m. - 8 p.m.
Phone: (843) 559-1945
Hurd/St. Andrews Library
9 a.m. - 8 p.m.
Phone: (843) 766-2546
Miss Jane's Building (Edisto Library Temporary Location)
2 p.m. – 6 p.m.
Phone: (843) 869-2355
Dorchester Road Library
9 a.m. - 8 p.m.
Phone: (843) 552-6466
John L. Dart Library
9 a.m. - 7 p.m.
Phone: (843) 722-7550
Baxter-Patrick James Island
9 a.m. - 8 p.m.
Phone: (843) 795-6679
Main Library
9 a.m. - 8 p.m.
Phone: (843) 805-6930
Bees Ferry West Ashley Library
9 a.m. - 8 p.m.
Phone: (843) 805-6892
Mobile Library
9 a.m. - 5 p.m.
Phone: (843) 805-6909
Today's Hours
West Ashley Library
9 a.m. - 7 p.m.
Phone: (843) 766-6635
Folly Beach Library
Closed
Phone: (843) 588-2001
Edgar Allan Poe/Sullivan's Island Library
Closed for renovations
Phone: (843) 883-3914
Wando Mount Pleasant Library
9 a.m. - 8 p.m.
Phone: (843) 805-6888
Village Library
9 a.m. - 1 p.m.
Phone: (843) 884-9741
St. Paul's/Hollywood Library
9 a.m. - 8 p.m.
Phone: (843) 889-3300
Otranto Road Library
9 a.m. - 8 p.m.
Phone: (843) 572-4094
Mt. Pleasant Library
9 a.m. - 8 p.m.
Phone: (843) 849-6161
McClellanville Library
9 a.m. - 6 p.m.
Phone: (843) 887-3699
Keith Summey North Charleston Library
9 a.m. - 8 p.m.
Phone: (843) 744-2489
John's Island Library
9 a.m. - 8 p.m.
Phone: (843) 559-1945
Hurd/St. Andrews Library
9 a.m. - 8 p.m.
Phone: (843) 766-2546
Miss Jane's Building (Edisto Library Temporary Location)
2 p.m. – 6 p.m.
Phone: (843) 869-2355
Dorchester Road Library
9 a.m. - 8 p.m.
Phone: (843) 552-6466
John L. Dart Library
9 a.m. - 7 p.m.
Phone: (843) 722-7550
Baxter-Patrick James Island
9 a.m. - 8 p.m.
Phone: (843) 795-6679
Main Library
9 a.m. - 8 p.m.
Phone: (843) 805-6930
Bees Ferry West Ashley Library
9 a.m. - 8 p.m.
Phone: (843) 805-6892
Mobile Library
9 a.m. - 5 p.m.
Phone: (843) 805-6909
Patron Login
menu
Item request has been placed!
×
Item request cannot be made.
×
![loading](/sites/all/modules/hf_eds/images/loading.gif)
Design, synthesis and biological evaluation of PEGylated Xenopus glucagon-like peptide-1 derivatives as long-acting hypoglycemic agents.
Item request has been placed!
×
Item request cannot be made.
×
![loading](/sites/all/modules/hf_eds/images/loading.gif)
- Author(s): Han J;Han J; Wang Y; Wang Y; Meng Q; Meng Q; Li G; Li G; Huang F; Huang F; Wu S; Wu S; Fei Y; Fei Y; Zhou F; Zhou F; Fu J; Fu J
- Source:
European journal of medicinal chemistry [Eur J Med Chem] 2017 May 26; Vol. 132, pp. 81-89. Date of Electronic Publication: 2017 Mar 18.- Publication Type:
Journal Article- Language:
English - Source:
- Additional Information
- Source: Publisher: Editions Scientifiques Elsevier Country of Publication: France NLM ID: 0420510 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1768-3254 (Electronic) Linking ISSN: 02235234 NLM ISO Abbreviation: Eur J Med Chem Subsets: MEDLINE
- Publication Information: Publication: Paris : Editions Scientifiques Elsevier
Original Publication: Paris, S.E.C.T. [etc.] - Subject Terms: Diabetes Mellitus, Type 2/*drug therapy ; Glucagon-Like Peptide 1/*chemistry ; Hypoglycemic Agents/*chemical synthesis ; Hypoglycemic Agents/*pharmacokinetics ; Polyethylene Glycols/*chemistry; Animals ; Blood Glucose/drug effects ; Cysteine/genetics ; Drug Design ; Glucagon-Like Peptide 1/pharmacology ; Half-Life ; Humans ; Hypoglycemic Agents/pharmacology ; Insulin/blood ; Mice, Inbred Strains ; Mutagenesis, Site-Directed ; Mutant Chimeric Proteins/pharmacology ; Polyethylene Glycols/pharmacology ; Xenopus
- Abstract: In order to develop novel long-acting GLP-1 derivatives, a peptide hybrid (1a) from human GLP-1 and Xenopus GLP-1 discovered in our previous research was selected as the lead compound. Exendin-4 inspired modification resulted in peptide 1b with enhanced glucose-lowering activity. Cysteine mutated 1b derivatives with reserved bioactivity were further site-specifically connected with mPEG
2000 -MAL to provide conjugates 3a-h, among which 3d and 3e were found to have significantly improved hypoglycemic activity and insulinotropic ability than GLP-1. The hypoglycemic durations of 3d and 3e were remarkably prolonged to ∼20 h in type 2 diabetic db/db mice, compared with the 5.3 h of exendin-4 in the same test. Finally, chronic in vivo studies revealed that a once-daily treatment of 3d or 3e for five weeks resulted in recovered glucose-controlling ability of type 2 diabetic db/db mice, along with other benefits, such as reduced body weight gains, food intake amounts and HbA1c values. Collectively, our results suggest 3d and 3e as potential long-acting glucose-lowering agents for treating type 2 diabetes.
(Copyright © 2017 Elsevier Masson SAS. All rights reserved.) - Contributed Indexing: Keywords: Glucagon-like peptide-1; PEGylation; Type 2 diabetes
- Accession Number: 0 (Blood Glucose)
0 (Hypoglycemic Agents)
0 (Insulin)
0 (Mutant Chimeric Proteins)
3WJQ0SDW1A (Polyethylene Glycols)
89750-14-1 (Glucagon-Like Peptide 1)
K848JZ4886 (Cysteine) - Publication Date: Date Created: 20170326 Date Completed: 20170605 Latest Revision: 20181202
- Publication Date: 20240628
- Accession Number: 10.1016/j.ejmech.2017.03.032
- Accession Number: 28342399
- Source:
Contact CCPL
Copyright 2022 Charleston County Public Library Powered By EBSCO Stacks 3.3.0 [350.3] | Staff Login
No Comments.