Title:
IDENTIFICATION OF CYCLIC PEPTIDE AGONISTS OF GALANIN RECEPTOR 2 AND 3 GUIDED BY SPEXIN SOLUTION STRUCTURE
Document Type and Number:
WIPO Patent Application WO/2018/184477
Kind Code:
A1
Abstract:
Cyclic peptide agonists toward human galanin receptor 2 (GalR2) and galanin receptor 3 (GalR3) based on hidden conformation of spexin solution structure for GalR2 and GalR3-related and spexin-deficient disorders are designed and synthesized. LH101, LH102, and LH101 (Ac) are potent spexin analogs with prolonged action, which can be used in the treatment of GalR2 and GalR3-related diseases and spexin-deficient disorders, such as obesity.
Inventors:
BIAN ZHAOXIANG (CN)
HUANG TAO (CN)
LIN CHENGYUAN (CN)
HUANG TAO (CN)
LIN CHENGYUAN (CN)
Application Number:
PCT/CN2018/080353
Publication Date:
October 11, 2018
Filing Date:
March 23, 2018
Export Citation:
Assignee:
UNIV HONG KONG BAPTIST UNIV (CN)
International Classes:
C07K14/575; A61K38/00; C07K14/72; G01N33/566
Domestic Patent References:
| WO2016146513A1 | 2016-09-22 |
Foreign References:
| US20130196348A1 | 2013-08-01 | |||
| US20040234537A1 | 2004-11-25 | |||
| CN101448513A | 2009-06-03 | |||
| CN103391784A | 2013-11-13 |
Other References:
HUANG, T.: "Toward novel therapeutics for functional constipation:from traditional Chinese medicine herbal formula MaZiRenWan to cyclic spexin analogues", HONG KONG BU INSTITUTIONAL REPOSITORY, 12 November 2017 (2017-11-12), XP055542114
GREEN, B.R. ET AL.: "Cyclic analogs of galanin and neuropeptide Y by hydrocarbon stapling", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 21, 30 October 2012 (2012-10-30), pages 303 - 310, XP028961382
LAND, T. ET AL.: "Linear and cyclic N-terminal galanin fragments and analogs as ligands at the hypothalamic galanin receptor", INT. J. PEPTIDE PROTEIN RES., vol. 38, no. 3, September 1991 (1991-09-01), pages 267 - 272, XP055542128
REYES-ALCARAZ, A. ET AL.: "Development of Spexin-based Human Galanin Receptor Type II -Specific Agonists with Increased Stability in Serum and Anxiolytic Effect in Mice", SCIENTIFIC REPORTS, vol. 6, 24 February 2016 (2016-02-24), XP055542142
See also references of EP 3606948A4
GREEN, B.R. ET AL.: "Cyclic analogs of galanin and neuropeptide Y by hydrocarbon stapling", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 21, 30 October 2012 (2012-10-30), pages 303 - 310, XP028961382
LAND, T. ET AL.: "Linear and cyclic N-terminal galanin fragments and analogs as ligands at the hypothalamic galanin receptor", INT. J. PEPTIDE PROTEIN RES., vol. 38, no. 3, September 1991 (1991-09-01), pages 267 - 272, XP055542128
REYES-ALCARAZ, A. ET AL.: "Development of Spexin-based Human Galanin Receptor Type II -Specific Agonists with Increased Stability in Serum and Anxiolytic Effect in Mice", SCIENTIFIC REPORTS, vol. 6, 24 February 2016 (2016-02-24), XP055542142
See also references of EP 3606948A4
Attorney, Agent or Firm:
CHINA PAT INTELLECTUAL PROPERTY OFFICE (CN)
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