Proteolysis targeting chimeras (PROTACs), heterobifunctional protein degraders, have emerged as an {exciting|thrilling|fascinating} and transformative {technology|technologies} in chemical biology and drug discovery to degrade disease-causing proteins {through|via|by means of|by way of} co-opting {of the|from the|in the|on the|with the|of your} ubiquitin-proteosome {system|method|program|technique} (UPS). {Here|Right here} we {develop|create} a mechanistic mathematical model for {the use of|the usage of} irreversible covalent chemistry in targeted protein degradation (TPD), either {to the|towards the|for the} target protein of interest (POI) or E3 ligase ligand, {considering|contemplating|thinking about|taking into consideration|thinking of} the thermodynamic and kinetic {factors|elements|aspects|variables|components|things} governing ternary {complex|complicated} formation, ubiquitination, and degradation {through|via|by means of|by way of} the UPS. We highlight {key|important|crucial|essential} {advantages|benefits|positive aspects} of covalency to POI and E3 ligase, {and the|and also the|as well as the|along with the|plus the} underlying theoretical basis {in the|within the|inside the} TPD reaction framework. We {further|additional} {identify|determine|recognize} regimes {where|exactly where} covalency can serve to overcome weak binary binding affinities and {improve|enhance|boost|increase|strengthen} kinetics of ternary {complex|complicated} formation and degradation. Our {results|outcomes|final results|benefits} highlight the enhanced catalytic efficiency of covalent E3 PROTACs and {thus|therefore|hence|as a result} their {potential|possible|prospective} {to improve|to enhance} the degradation of {fast|quick|quickly|rapidly|rapid|speedy} turnover targets. 885588-14-7 site 1,2-Cyclopentanedicarboxylic acid Data Sheet PMID:24275718
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