apcin and Neoplasms

The anaphase promoting complex/ cyclosome (APC/C), is an evolutionarily conserved protein complex essential for cellular division due to its role in regulating the mitotic transition from metaphase to anaphase. In this review, we highlight recent work that has shed light on our understanding of the role of APC/C coactivators, Cdh1 and Cdc20, in cancer initiation and development. We summarize the current state of knowledge regarding APC/C structure and function, as well as the distinct ways Cdh1 and Cdc20 are dysregulated in human cancer. We also discuss APC/C inhibitors, novel approaches for targeting the APC/C as a cancer therapy, and areas for future work.

Topics: Anaphase-Promoting Complex-Cyclosome; Antigens, CD; Antineoplastic Agents; Carbamates; Cdc20 Proteins; Cdh1 Proteins; Diamines; Genomic Instability; Humans; Molecular Targeted Therapy; Neoplasms

Target-based screening and cell-based screening are major approaches to identify anticancer drug candidates. Cell-based screening often contributes to the discovery of first-in-class drugs, but identification of the cellular targets of obtained compounds is a time-consuming step. To overcome this problem, affinity purification with small-molecule probes, which is a classic, but still the most common approach, has become more sophisticated and diversified. In addition, recent advances in omics studies and imaging analyses have allowed us to profile the biological effects of small molecules globally and quantitatively. Consequently, new therapeutic targets/drug leads involved in cancer cell cycle, transcription and redox regulation have been discovered.

Topics: Aminoquinolines; Antineoplastic Agents; Carbamates; Cell Cycle; Coumarins; Diamines; Diterpenes, Kaurane; Drug Discovery; Humans; Molecular Targeted Therapy; Neoplasms; Pyrazoles; Quinolines