TD1092 is a pan-IAP degrader, degrades cIAP1, cIAP2, and XIAP
Apoptosis inhibitor proteins (IAP) represent a group of caspases and negative regulators of cell death. Particularly, the IAP protein family prevents cell death by binding to and inhibiting active caspases and is negatively regulated by IAP-binding proteins. In addition to cell death, IAP also acts as an innate immune...
Zingerone, an Orally Active Nontoxic Methoxyphenol, Possesses Anti-Inflammatory and Anti-Tumor Properties
Humans have been using natural products for medicinal use for ages. Ginger (Zingiber officinale) is used as a condiment worldwide from times immemorial. Ginger has many health benefits in traditional medicine. It is due to diverse phytochemical constituents present in ginger which lead to promising health benefits. It is...
Deguelin, a Naturally Occurring Rotenoid, Acts as a Chemopreventive Agent
Head and neck squamous cell carcinoma (HNSCC) represents more than 5% of all cancers each year. In addition, breast cancer is a heterogeneous group of diseases. Approximately 60-70% of breast cancers express estrogen receptors (ER) and/or progesterone receptors (PR). About 20-30% of breast cancers have amplified levels of the...
CBL0137 is an Histone Chaperone FACT Inhibitor
Cancer harbors several characteristics, including high heterogeneity, diverse gene mutation, or rapid progression; consequently, treating cancer is difficult, and it easily relapses. Surgery, radiotherapy, chemotherapy, immunotherapy, and targeted therapy show remarkable achievements. In particular, targeted therapies promote treatment. However, we have failed to treat cancer. Chemotherapy with or without...
IMD-0354 is a Selective IKKβ Inhibitor
IKKβ is an enzyme that is part of an intracellular signaling pathway activated by cytokines involved in triggering an immune response. Particularly, Phosphorylated IκB degrades and releases NF-κB through the ubiquitination pathway. Importantly, it enters the nucleus and participates in a variety of genes in inflammation and other immune...
PS315, an Allosteric PKC Inhibitor Binding to the PIF-Pocket
Members of the protein kinase C (PKC) family are regulated by phosphorylation and by an N-terminal extension of the catalytic domain. In addition, AGC kinases are a group of protein kinases comprising PKA, protein kinase G, and PKC families. They typically have three conserved phosphorylation sites. Besides, all PKCs...
E3330, an APE1 Redox Inhibitor, Modulates Cell Migration and Invasion in Metastatic Cancer
AP endonuclease 1 (APE1; also known as REF-1) is a dual-function protein. It contains a redox domain and a DNA repair domain. Several human cancers overexpress APE1. Disruption of APE1 function has detrimental effects on cancer cell viability. Furthermore, APE1 implicates in the transactivation of numerous seminal transcription factors involved...