Category: Renal Carcinoma

Abexinostat is an Orally Available Pan-HDAC Inhibitor

HDAC (Histone deacetylases) are a class of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone. To date, There are 18 human HDACs. Besides, HDACs include four classes on the basis of their homology with yeast proteins. Class I HDACs (HDAC1, 2, 3, and...

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...

UC2288 is an Orally Active p21 Attenuator

p21 is a member of the cip/kip family of cyclin-dependent kinase inhibitors, it regulates cell growth in both malignant or non-malignant cells. It possesses diverse physiological functions in vitro, such as vascular smooth muscle cell proliferation, cancer progression, and viral infection. p21 is well-known as a tumor suppressor protein...

PT2977 is an Orally Active and Selective HIF-2α Inhibitor for Solid Tumor Treatment

Previous studies have demonstrated that hypoxia-inducible factor 2α (HIF-2α) is a key oncogenic driver in clear cell renal cell carcinoma (ccRCC). PT2385 was the first reported HIF-2α inhibitor. However, PT2385 was restricted by variable and dose-limited pharmacokinetics. This results from extensive metabolism of PT2385 to its glucuronide metabolite. Herein,...

R916562, a Dual Axl/VEGF-R2 Inhibitor for Cancer Therapy

Axl tyrosine kinase is a putative driver of diverse cellular processes that are critical for the development, growth, and spread of tumors. It is a promising therapeutic target for cancer therapy. VEGFR2 is a primary responder to vascular endothelial growth factor signal, and thereby regulates endothelial migration and proliferation....