An all-in-one targeted protein degradation platform guided by ...
WEBMar 5, 2024 · Targeted protein degradation (TPD) has emerged as a breakthrough strategy in revolutionizing drug discovery for the currently undruggable targets.
Targeted protein degradation: from mechanisms to clinic
WEBApr 29, 2024 · In its most common form, this degradation is achieved through ligand-mediated neo-interactions between ubiquitin E3 ligases — the principal waste disposal machines of a cell — and the protein...
Protein degradation on the global scale - Cell Press
WEBApr 21, 2022 · Protein degradation occurs through proteasomal, endosomal, and lysosomal pathways. Technological advancements have allowed for the determination of protein copy numbers and turnover rates on a global scale, which has provided an overview of trends and rules governing protein degradation.
Targeted protein degradation using chimeric human E2 ubiquitin …
WEB6 days ago · Proteins can be targeted for degradation by engineering biomolecules that direct them to the eukaryotic ubiquitination machinery. For instance, the fusion of an E3 ubiquitin ligase to a suitable ...
Lysosomal Biology and Function: Modern View of Cellular Debris Bin
WEBMay 4, 2020 · The lysosomal lumen contains a battery of soluble hydrolytic enzymes that degrade proteins (proteases), triglycerides (lysosomal acid lipase; LAL), glycoproteins (glycosidases), heparan sulphate (sulfatases), and nucleic acids (nucleases, RNAase and …
Targeted protein degradation: A promise for undruggable proteins
WEBMay 17, 2021 · Targeted protein degradation (TPD) by PROTACs allows drug hunters to eliminate disease-causing proteins from the cellular environment. In this review, Samarasinghe and Crews discuss the beginning, the …
Targeted protein degradation: mechanisms, strategies and …
WEBApr 4, 2022 · Protein degradation via the ubiquitin-proteasome system (UPS). Proteins undergo ubiquitin-dependent degradation by a suite of three enzymes. E1 interacts with E2, and transfers the ubiquitin molecule to E2. E2 interacts with E3-binding substrate and transfers the ubiquitin molecule to the substrate.
New Role Introduced: PDF-Bin, Protein Targeting the Degradation ...
WEBApr 21, 2024 · The paper reports a novel protein-targeting degradation technology named PDF-Bin. The core component of this technology is a bispecific antibody capable of simultaneously binding to the p62 protein and the target protein.
Ubiquitin-independent proteasomal degradation driven by C …
WEBJun 1, 2023 · Although most eukaryotic proteins are targeted for proteasomal degradation by ubiquitination, a subset have been demonstrated to undergo ubiquitin-independent proteasomal degradation (UbInPD). However, little is known about the molecular mechanisms driving UbInPD and the degrons involved.
The Advent of Directed Protein Degraders in Drug Discovery
WEBAug 20, 2019 · This technology takes advantage of the ubiquitin–proteasome system – the cellular ‘dustbin’ mechanism – to selectively degrade a protein of interest (POI). In brief, a PROTAC is a bifunctional heterodimer that binds simultaneously to a POI and to a ubiquitin E3 ligase, the two ends being linked together by a chemical tether.
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