PROTAC: targeted drug strategy. Principles and limitations
O. A. Koroleva, Yu. V. Dutikova, A.V. Trubnikov, Fedor A. Zenov, E. V. Manasova, Аlexander А. Shtil, Aleksander V. Kurkin
Abstract
) technology is a method of targeting intracellular proteins previously considered undruggable. This technology utilizes the ubiquitin-proteasome system in cells to specifically degrade target proteins, thereby offering significant advantages over conventional small-molecule inhibitors of the enzymatic function. Preclinical and preliminary clinical trials of PROTAC-based compounds (degraders) are presented. The review considers the general principles of the design of degraders. Advances and challenges of the PROTAC technology are discussed.
Topics & Concepts
ChemistryProteasomeComputational biologyProteolysisDrugDrug discoveryUbiquitinNanotechnologyBiochemistryPharmacologyEnzymeBiologyMaterials scienceGeneProtein Degradation and InhibitorsUbiquitin and proteasome pathwaysMultiple Myeloma Research and Treatments