Title:
GAIN-OF-FUNCTION MUTANT OF BRANCHED-CHAIN AMINO ACID TRANSAMINASE 1, AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/207545
Kind Code:
A1
Abstract:
The present invention provides an activated gain-of-function mutant of branched-chain amino acid transaminase 1 (BCAT1), and use thereof. In particular, the present invention provides a human BCAT1E61A gain-of-function activated mutant protein (namely BCAT1E61A mutant protein) and a targeting inhibitor for the mutant protein. Compared with a wild-type protein, the targeting inhibitor of the present invention not only has a more remarkable inhibitory effect on the mutant protein, but also has an effective inhibitory concentration (IC50) remarkably lower than that of an existing BCAT1 inhibitor, and the specificity of an action target is stronger.
Inventors:
LEI QUNYING (CN)
Application Number:
PCT/CN2023/086648
Publication Date:
November 02, 2023
Filing Date:
April 06, 2023
Export Citation:
Assignee:
UNIV FUDAN (CN)
International Classes:
C12N9/10; A61K45/00; A61K45/06; A61P3/06; A61P3/10; A61P5/50; A61P13/12; A61P19/02; A61P29/00; A61P35/00; A61P35/02; A61P35/04; C12N15/54; C12Q1/6883; C12Q1/6886
Foreign References:
| EP0613687A1 | 1994-09-07 | |||
| US20100029560A1 | 2010-02-04 | |||
| US20130310545A1 | 2013-11-21 | |||
| US20130072397A1 | 2013-03-21 |
Other References:
LIU YUPING; HE WENWEN; WANG WENYAN; ZHU DAN; DENG MINGFEN: "Suppression Effects of Candesartan on Proliferation, Migration and Invasion of Ovarian Cancer Caov-3 Cells and Its Mechanism", TUMOR, SHANGHAI, CN, vol. 38, no. 11, 30 November 2018 (2018-11-30), CN , pages 1001 - 1010, XP009550017, ISSN: 1000-7431
RONG WU; JUN-TAO ZHANG; WEI-BIN LI; KUN WANG; ZHI-ZHEN LIU: "Losartan Attenuates Angiogenesis in Hepatocellular Carcinoma via Down-Regulation of AT1R/VEGF Signaling Pathway", CHINA JOURNAL OF MODERN MEDICINE, ZHONGNAN DAXUE, CN, vol. 28, no. 26, 30 September 2018 (2018-09-30), CN , pages 7 - 13, XP009550014, ISSN: 1005-8982
SHAFEI MAI AHMED, FORSHAW THOMAS, DAVIS JASMINE, FLEMBAN ARWA, QUALTROUGH DAVID, DEAN SARAH, PERKS CLAIRE, DONG MING, NEWMAN ROBER: "BCATc modulates crosstalk between the PI3K/Akt and the Ras/ERK pathway regulating proliferation in triple negative breast cancer", ONCOTARGET, vol. 11, no. 21, 26 May 2020 (2020-05-26), pages 1971 - 1987, XP093104474, DOI: 10.18632/oncotarget.27607
RONG WU; JUN-TAO ZHANG; WEI-BIN LI; KUN WANG; ZHI-ZHEN LIU: "Losartan Attenuates Angiogenesis in Hepatocellular Carcinoma via Down-Regulation of AT1R/VEGF Signaling Pathway", CHINA JOURNAL OF MODERN MEDICINE, ZHONGNAN DAXUE, CN, vol. 28, no. 26, 30 September 2018 (2018-09-30), CN , pages 7 - 13, XP009550014, ISSN: 1005-8982
SHAFEI MAI AHMED, FORSHAW THOMAS, DAVIS JASMINE, FLEMBAN ARWA, QUALTROUGH DAVID, DEAN SARAH, PERKS CLAIRE, DONG MING, NEWMAN ROBER: "BCATc modulates crosstalk between the PI3K/Akt and the Ras/ERK pathway regulating proliferation in triple negative breast cancer", ONCOTARGET, vol. 11, no. 21, 26 May 2020 (2020-05-26), pages 1971 - 1987, XP093104474, DOI: 10.18632/oncotarget.27607
Attorney, Agent or Firm:
XU & PARTNERS, LLC. et al. (CN)
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