78P Small molecule compounds targeting the p53 mutants

Targeting p53 by small molecule p53 activators in multiple myeloma

For the past three decades of research, p53 has been identified as one of the most targetable molecules for developing anticancer treatments. This tumor suppressor protein is involved in apoptosis, cell cycle arrest and senescence. Impairment of p53 function in tumors occurs either as a result of mutations in the TP53 gene itself or the abrogation of signaling pathways regulating p53 that are r...

Identification of Novel p53 Pathway Activating Small-Molecule Compounds Reveals Unexpected Similarities with Known Therapeutic Agents

Manipulation of the activity of the p53 tumor suppressor pathway has demonstrated potential benefit in preclinical mouse tumor models and has entered human clinical trials. We describe here an improved, extensive small-molecule chemical compound library screen for p53 pathway activation in a human cancer cell line devised to identify hits with potent antitumor activity. We uncover six novel sma...

Small molecule toxins targeting tumor receptors.

Targeting toxic therapeutics to tumors through receptors over expressed on the surface of cancer cells can reduce systemic toxicity and increase the effectiveness of the targeted compounds. Small molecule targeted therapeutics have a number of advantages over toxic immunoconjugates including better tumor penetration, lack of neutralizing host immune response and superior flexibility in selectio...

A Novel Small-molecule Inhibitor Targeting

Targeting Protein Stability with a Small Molecule

Both genetic approaches and small-molecule inhibitors can be used to perturb protein function. Banaszynski et al. (2006) now describe a strategy to regulate the stability of a target protein, in which specificity is provided by a genetically encoded tag and temporal control is imparted by a small molecule.