title: BRAF inhibitors: From the laboratory to clinical trials.
abstract: BRAF is one of the most commonly mutated proto-oncogenes and plays a significant role in the development of numerous cancers of high clinical impact. Due to the commonality of BRAF mutations, a number of BRAF inhibitors have been developed as tools in the management of patients with cancers dependent on the action of mutant BRAF to drive cellular proliferation. In this review, we examine the current state of clinical trials and laboratory research concerning BRAF inhibitors in development and available for clinical use. We contrast the effectiveness of type-I and type-II BRAF inhibitors, the former typically showing much more restricted inhibitory selectivity and greater patient response rates.
authors.affiliation: Cancer Molecular Pathology Group, Griffith Health Institute, Griffith University, Gold Coast, Australia.
authors.forename: M A
authors.initials: MA
authors.lastname: Rahman
authors.affiliation: Cancer Molecular Pathology Group, Griffith Health Institute, Griffith University, Gold Coast, Australia.
authors.forename: A
authors.initials: A
authors.lastname: Salajegheh
authors.affiliation: Cancer Molecular Pathology Group, Griffith Health Institute, Griffith University, Gold Coast, Australia.
authors.forename: R A
authors.initials: RA
authors.lastname: Smith
authors.affiliation: Cancer Molecular Pathology Group, Griffith Health Institute, Griffith University, Gold Coast, Australia. Electronic address: a.lam@griffith.edu.au.
authors.forename: A K-Y
authors.initials: AK
authors.lastname: Lam
mesh_terms: D000970:Antineoplastic Agents / Q000145:classification / Q000494:pharmacology* / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D004353:Drug Evaluation, Preclinical; D006801:Humans; D058990:Molecular Targeted Therapy; D009369:Neoplasms / Q000188:drug therapy*; D047428:Protein Kinase Inhibitors / Q000145:classification / Q000494:pharmacology* / Q000627:therapeutic use*; D048493:Proto-Oncogene Proteins B-raf / Q000037:antagonists & inhibitors*
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D048493:Proto-Oncogene Proteins B-raf
keywords: BRAF; Clinical trial; Kinase inhibitors; Multi-kinase inhibitor