The University of Michigan has disclosed pyrrolo[1,2-a]-azocine analogues acting as as inhibitor of apoptosis proteins (IAP) inhibitors. As such, they are reported to be potentially useful for the treatment of AIDS, cancer, infections, psoriasis, multiple sclerosis, vascular disorders, inflammatory disorders and autoimmune diseases.
GAS41, the chromatin-associated protein encoded by YEATS4, is frequently overexpressed in non-small-cell lung cancer (NSCLC). Beyond its association with epigenetic dysregulation, GAS41 plays an active role in modulating transcriptional programs that are essential for NSCLC pathogenesis, underscoring its suitability as a mechanistically well-supported therapeutic target.
Cancer of the uterus is the most common gynecological malignancy in the U.S., with over 60,000 diagnoses per year, where incidence and mortality have increased through the years. About 30%-40% of patients with high-grade disease harbor mutations in the PPP2R1A gene, which encodes the primary subunit of protein phosphatase 2A, with hotspots being P179R and S256F.
Shanghai Institute of Organic Chemistry and the University of Michigan have prepared and tested new cyclin-dependent kinase 12 (CDK12) and 13 (CDK13) inhibitors reported to be useful for the treatment of cancer.
University of Michigan has disclosed prodrugs of stimulator of interferon genes protein (STING; TMEM173) agonists reported to be useful for the treatment of cancer, autoimmune disease, inflammatory disorder and infections.
Researchers at the University of Michigan designed an optimized viral protein able to boost the antitumor function of T cells. The project stemmed from observations on the particular system employed by Herpesvirus saimiri to infect T cells and hijack cellular pathways by activating them.
A metabolic vulnerability of pancreatic ductal adenocarcinoma (PDAC) could be used to address this type of cancer that often resists treatments. Scientists at the University of Michigan have discovered that inhibiting the PIKfyve enzyme prevented tumor development and reduced tumor growth by altering the lipid synthesis these cells rely on. The KRAS-MAPK pathway is involved in this process, leading the researchers to suggest that dual inhibitors of PIKfyve and KRAS-MAPK could be an effective therapeutic strategy.
The University of Michigan has divulged lysine-specific histone demethylase 1A (KDM1A; LSD1) inhibitors reported to be useful for the treatment of cancer, autism, myocardial fibrosis and more.
High-grade serous ovarian cancer (HGSC) is among the most lethal gynecologic malignancies, with up to 90% of patients eventually becoming resistant to platinum-based chemotherapy. The limited availability of effective targeted therapies for platinum-resistant HGSC presents a significant clinical challenge.
The absent, small or homeotic-like 1 (ASH1L) protein regulates the expression of HOXA genes, which are critical for the development of MLL1 translocations frequently found in leukemia patients. Knockdown of ASH1L leads to growth arrest and apoptosis of leukemia cells, thereby inhibiting leukemia progression suggesting that ASH1L can be considered as a therapeutic target in this setting.
