title: Identification of direct protein targets of small molecules.
abstract: Small-molecule target identification is a vital and daunting task for the chemical biology community as well as for researchers interested in applying the power of chemical genetics to impact biology and medicine. To overcome this "target ID" bottleneck, new technologies are being developed that analyze protein-drug interactions, such as drug affinity responsive target stability (DARTS), which aims to discover the direct binding targets (and off targets) of small molecules on a proteome scale without requiring chemical modification of the compound. Here, we review the DARTS method, discuss why it works, and provide new perspectives for future development in this area.
authors.affiliation: Department of Molecular and Medical Pharmacology, University of California, Los Angeles, 90095, United States.
authors.forename: Brett
authors.initials: B
authors.lastname: Lomenick
authors.forename: Richard W
authors.initials: RW
authors.lastname: Olsen
authors.forename: Jing
authors.initials: J
authors.lastname: Huang
mesh_terms: D002846:Chromatography, Affinity; D016503:Drug Delivery Systems; D015195:Drug Design; D058990:Molecular Targeted Therapy / Q000379:methods*; D004364:Pharmaceutical Preparations; D011485:Protein Binding / Q000502:physiology*; D020543:Proteome / Q000737:chemistry*; D040901:Proteomics; D054852:Small Molecule Libraries / Q000737:chemistry*
chemical_list: D004364:Pharmaceutical Preparations; D020543:Proteome; D054852:Small Molecule Libraries