Identification of novel ASK1 inhibitors using virtual screening.

Bioorg Med Chem

Drug Discovery Department, Research & Development Division, PharmaDesign, Inc., 2-19-8 Hatchobori, Chuo-ku, Tokyo 104-0032, Japan.

Published: January 2011

Apoptosis signal-regulating kinase 1 (ASK1, also called MAP3K5) is a mitogen-activated protein kinase kinase kinase (MAP3K) that plays important roles in stress-induced cell death and inflammation, and is expected as a new therapeutic target for cancer, cardiovascular diseases, and neurodegenerative diseases. We identified novel ASK1 inhibitors by virtual screening from the public chemical library collected by Chemical Biology Research Initiative (CBRI) at the University of Tokyo.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmc.2010.11.004DOI Listing

Publication Analysis

Top Keywords

novel ask1
8
ask1 inhibitors
8
inhibitors virtual
8
virtual screening
8
kinase kinase
8
identification novel
4
screening apoptosis
4
apoptosis signal-regulating
4
kinase
4
signal-regulating kinase
4

Similar Publications

Article Synopsis
  • Cardiac remodelling is a key factor in cardiovascular diseases, and this study investigates the role of TRAF7, a protein linked to heart defects, in promoting pathological cardiac hypertrophy.
  • Researchers utilized mouse models and various experimental techniques to examine how TRAF7 affects heart cell growth and dysfunction, revealing that higher levels of TRAF7 worsen heart enlargement, while reducing TRAF7 has a protective effect.
  • The study found that TRAF7 influences heart hypertrophy by interacting with another protein, ASK1, which leads to its activation and contributes to the disease process, suggesting that TRAF7 could be a potential target for new treatments.
View Article and Find Full Text PDF

Ovarian cancer, the second most leading cause of gynecologic cancer mortality worldwide, is challenged by chemotherapy resistance, presenting a significant hurdle. Pyroptosis, an inflammation-linked programmed cell death mediated by gasdermins, has been shown to impact chemoresistance when dysregulated. However, the mechanisms connecting pyroptosis to chemotherapy resistance in ovarian cancer are unclear.

View Article and Find Full Text PDF

OLFM4 modulates intestinal inflammation by promoting IL-22ILC3 in the gut.

Commun Biol

July 2024

Pediatric Intensive Care Unit, Guangdong Provincial People's Hospital (Guangdong Academy of Medical Sciences); Department of Immunology, School of Basic Medical Sciences; Department of Clinical Laboratory, the Third Affiliated Hospital of Southern Medical University, Southern Medical University, Guangzhou, China.

Group 3 innate lymphoid cells (ILC3s) play key roles in intestinal inflammation. Olfactomedin 4 (OLFM4) is highly expressed in the colon and has a potential role in dextran sodium sulfate-induced colitis. However, the detailed mechanisms underlying the effects of OLFM4 on ILC3-mediated colitis remain unclear.

View Article and Find Full Text PDF

Ovarian cancer is a gynecological malignant tumor with the highest mortality rate, and chemotherapy resistance seriously affects patient therapeutic outcomes. It has been shown that the high expression of anti‑apoptotic proteins Bcl‑2 and Bcl‑xL is closely related to ovarian cancer chemotherapy resistance. Therefore, reducing Bcl‑2 and Bcl‑xL expression levels may be essential for reversing drug resistance in ovarian cancer.

View Article and Find Full Text PDF

Vagal-α7 nicotinic acetylcholine receptor signaling exacerbates influenza severity by promoting lung epithelial cell infection.

J Med Virol

July 2024

Unit of Respiratory Infection and Immunity, Shanghai Institute of Immunity and Infection, Chinese Academy of Sciences, University of Chinese Academy of Sciences, Shanghai, China.

Article Synopsis
  • The vagus nerve and a special receptor (α7 nAChR) help control how our body reacts to infections, like inflammation.
  • Researchers found that the α7 nAChR has different roles in lung cells and immune cells when it comes to the influenza virus.
  • When they blocked this receptor in certain lung cells, it actually helped reduce flu infections and protected mice from getting seriously ill.
View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!