Title:
NEW APPLICATION OF HUWE1 INHIBITOR BI8622
Document Type and Number:
WIPO Patent Application WO/2021/179396
Kind Code:
A1
Abstract:
A new application of an HUWE1 inhibitor BI8622 to inhibition of inflammasome activation. Researches discover that the HUWE1 inhibitor BI8622 can remarkably reduce activation of cysteine protease-1 (Caspase-1) and expression of interleukin 1β (IL-1β) in bone marrow derived macrophages (BMDM) of a mouse, and cell death is reduced; and meanwhile, it is proved that the BI8622 can remarkably reduce activation of the Caspase-1 and expression of the IL-1β in a human mononuclear macrophage line THP1 and human primary peripheral blood mononuclear cells (PBMC), and cell death is also remarkably reduced, so that the BI8622 can remarkably inhibit inflammasome activation.
Inventors:
QI XIAOPENG (CN)
XU TAO (CN)
LI YIHUI (CN)
GUO XIAOMIN (CN)
XU TAO (CN)
LI YIHUI (CN)
GUO XIAOMIN (CN)
Application Number:
PCT/CN2020/085013
Publication Date:
September 16, 2021
Filing Date:
April 16, 2020
Export Citation:
Assignee:
KUNMING INST ZOOLOGY CAS (CN)
International Classes:
A61K31/506; A61P3/10; A61P17/00; A61P19/06; A61P29/00
Foreign References:
| CN108938697A | 2018-12-07 | |||
| CN110251657A | 2019-09-20 | |||
| CN104140954A | 2014-11-12 |
Other References:
ZHANG ZI-YANG; GUO ZHEN; LI HU-LING; HE YONG-TAO; DUAN XING-LIAN; SUO ZHAN-WEI; YANG XIAN; HU XIAO-DONG: "Ubiquitination and inhibition of glycine receptor by HUWE1 in spinal cord dorsal horn", NEUROPHARMACOLOGY, vol. 148, 1 January 1900 (1900-01-01), pages 358 - 365, XP085640800, ISSN: 0028-3908, DOI: 10.1016/j.neuropharm.2019.02.002
PETER STEFANIE, BULTINCK JENNYFER, MYANT KEVIN, JAENICKE LAURA A, WALZ SUSANNE, MÜLLER JUDITH, GMACHL MICHAEL, TREU MATTHIAS, BOEH: "Tumor cell-specific inhibition of MYC function using small molecule inhibitors of the HUWE1 ubiquitin ligase", EMBO MOLECULAR MEDICINE, vol. 6, no. 12, 1 December 2014 (2014-12-01), pages 1525 - 1541, XP055846201, ISSN: 1757-4676, DOI: 10.15252/emmm.201403927
LIN, JIE ET AL.: "The Role of Ubiquitin Ligase HUWE1 in Related Diseases", CHINESE BULLETIN OF LIFE SCIENCES, vol. 30, no. 5, 20 June 2018 (2018-06-20), pages 539 - 544, XP055846198, ISSN: 1004-0374, DOI: 10.13376/j.cbls/2018064
PETER STEFANIE, BULTINCK JENNYFER, MYANT KEVIN, JAENICKE LAURA A, WALZ SUSANNE, MÜLLER JUDITH, GMACHL MICHAEL, TREU MATTHIAS, BOEH: "Tumor cell-specific inhibition of MYC function using small molecule inhibitors of the HUWE1 ubiquitin ligase", EMBO MOLECULAR MEDICINE, vol. 6, no. 12, 1 December 2014 (2014-12-01), pages 1525 - 1541, XP055846201, ISSN: 1757-4676, DOI: 10.15252/emmm.201403927
LIN, JIE ET AL.: "The Role of Ubiquitin Ligase HUWE1 in Related Diseases", CHINESE BULLETIN OF LIFE SCIENCES, vol. 30, no. 5, 20 June 2018 (2018-06-20), pages 539 - 544, XP055846198, ISSN: 1004-0374, DOI: 10.13376/j.cbls/2018064
Attorney, Agent or Firm:
BEIJING GAOWO LAW FIRM (CN)
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