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Title:
NONAPEPTIDE OF FORMULA I, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR PREPARATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2019/229771
Kind Code:
A3
Abstract:
The present invention relates to a nonapeptide of Formula (I), designed from the taxol binding cavity of β-tubulin. The nonapeptide has the ability to bind at taxol pocket of β-tubulin with a significant binding affinity and promotes microtubule polymerization. More particularly, the nonapeptide of the present invention binds to the 17-21 region of amyloid beta, inhibits acetylcholinesterase (AChE) induced amyloid beta (Aβ) aggregation by interacting at the peripheral anionic site (PAS) of AChE, enters into the derived neurons, promotes neurite growth, provides microtubule stabilization and shows significant neuroprotection against nerve growth factor (NGF) deprived neurons. Furthermore, the nonapeptide doesn't show any toxicity to both rat pheochromocytoma (PC12) derived neurons as well as primary cortical neurons.

Inventors:
GHOSH SURAJIT (IN)
MONDAL PRASENJIT (IN)
DAS GAURAV (IN)
KHAN JUHEE (IN)
PRADHAN KRISHNANGSU (IN)
Application Number:
PCT/IN2019/050418
Publication Date:
February 27, 2020
Filing Date:
May 29, 2019
Export Citation:
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Assignee:
COUNCIL SCIENT IND RES (IN)
International Classes:
C07K7/06; A61K38/08
Domestic Patent References:
WO2016083809A12016-06-02
WO2008070586A22008-06-12
Foreign References:
US20170253631A12017-09-07
Other References:
PRASENJIT MONDAL ET AL: "Crafting of Neuroprotective Octapeptide from Taxol-Binding Pocket of [beta]-Tubulin", ACS CHEMICAL NEUROSCIENCE, vol. 9, no. 3, 21 March 2018 (2018-03-21), US, pages 615 - 625, XP055646280, ISSN: 1948-7193, DOI: 10.1021/acschemneuro.7b00457
PRASENJIT MONDAL ET AL: "Potential Neuroprotective Peptide Emerged from Dual Neurotherapeutic Targets: A Fusion Approach for the Development of Anti-Alzheimer's Lead", ACS CHEMICAL NEUROSCIENCE, vol. 10, no. 5, 15 May 2019 (2019-05-15), US, pages 2609 - 2620, XP055645343, ISSN: 1948-7193, DOI: 10.1021/acschemneuro.9b00115
Attorney, Agent or Firm:
SINGH, Manisha (IN)
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