Rapid and reversible knockdown of endogenously tagged endosomal proteins via an optimized HaloPROTAC degrader [PDF]
, 2019 Inducing post-translational protein knockdown is an important approach to probe biology and validate drug targets. An efficient strategy to achieve this involves expression of a protein of interest fused to an exogenous tag, allowing tag-directed ...
Alessi, Dario +7 more
core +4 more sources
Antiviral PROTACs: Opportunity borne with challenge
Cell Insight, 2023 Proteolysis targeting chimera (PROTAC) degradation of pathogenic proteins by hijacking of the ubiquitin-proteasome-system has become a promising strategy in drug design. The overwhelming advantages of PROTAC technology have ensured a rapid and wide usage,
Jinsen Liang +6 more
doaj +1 more source
Structural basis of PROTAC cooperative recognition for selective protein degradation [PDF]
, 2017 Inducing macromolecular interactions with small molecules to activate cellular signaling is a challenging goal. PROTACs (proteolysis-targeting chimeras) are bifunctional molecules that recruit a target protein in proximity to an E3 ubiquitin ligase to ...
A Illendula +67 more
core +3 more sources
Targeting protein function: the expanding toolkit for conditional disruption [PDF]
, 2016 A major objective in biological research is to understand spatial and temporal requirements for any given gene, especially in dynamic processes acting over short periods, such as catalytically driven reactions, subcellular transport, cell division, cell ...
Bennett, Daimark, Campbell, Amy E
core +1 more source
PROTAC Technology: Opportunities and Challenges [PDF]
ACS Medicinal Chemistry Letters, 2020 PROTACs-induced targeted protein degradation has emerged as a novel therapeutic strategy in drug development and attracted the favor of academic institutions, large pharmaceutical enterprises (e.g., AstraZeneca, Bayer, Novartis, Amgen, Pfizer, GlaxoSmithKline, Merck, and Boehringer Ingelheim, etc.), and biotechnology companies.
Hongying Gao, Xiuyun Sun, Yu Rao
openaire +2 more sources
Iterative design and optimization of initially inactive Proteolysis Targeting Chimeras (PROTACs) identify VZ185 as a potent, fast and selective von Hippel-Lindau (VHL)-based dual degrader probe of BRD9 and BRD7 [PDF]
, 2018 Developing PROTACs to redirect the ubiquitination activity of E3 ligases and potently degrade a target protein within cells can be a lengthy and unpredictable process, and it remains unclear whether any combination of E3 and target might be productive ...
Ciulli, Alessio +10 more
core +6 more sources
Journal of the American Chemical Society, 2021 Targeted protein degradation has emerged as a new paradigm to manipulate cellular proteostasis. Proteolysis-targeting chimeras (PROTACs) are bifunctional small molecules that recruit an E3 ligase to a target protein of interest, promoting its ...
Adam D Cotton +4 more
semanticscholar +1 more source
Advances in targeted degradation of endogenous proteins [PDF]
, 2019 Protein silencing is often employed as a means to aid investigations in protein function and is increasingly desired as a therapeutic approach. Several types of protein silencing methodologies have been developed, including targeting the encoding genes ...
Fulcher, Luke +2 more
core +2 more sources
Antibody RING-Mediated Destruction of Endogenous Proteins [PDF]
, 2020 International ...
Abidi, Naima +7 more
core +4 more sources
Surface probing by fragment-based screening and computational methods identifies ligandable pockets on the von Hippel-Lindau (VHL) E3 ubiquitin ligase [PDF]
, 2018 Beyond the targeting of E3 ubiquitin ligases to inhibit protein homeostasis, E3 ligase binders can be repurposed as targeted protein degraders (PROTACs or molecular glues).
Ciulli, Alessio +2 more
core +4 more sources