[PDF][PDF] Inducible degradation of target proteins through a tractable affinity-directed protein missile system
LM Simpson, TJ Macartney, A Nardin, LJ Fulcher… - Cell Chemical …, 2020 - cell.com
The affinity-directed protein missile (AdPROM) system utilizes specific polypeptide binders
of intracellular proteins of interest (POIs) conjugated to an E3 ubiquitin ligase moiety to …
of intracellular proteins of interest (POIs) conjugated to an E3 ubiquitin ligase moiety to …
Targeting endogenous proteins for degradation through the affinity-directed protein missile system
LJ Fulcher, LD Hutchinson, TJ Macartney… - Open …, 2017 - royalsocietypublishing.org
Targeted proteolysis of endogenous proteins is desirable as a research toolkit and in
therapeutics. CRISPR/Cas9-mediated gene knockouts are irreversible and often not feasible …
therapeutics. CRISPR/Cas9-mediated gene knockouts are irreversible and often not feasible …
[PDF][PDF] Targeting endogenous K-RAS for degradation through the affinity-directed protein missile system
K-RAS is known as the most frequently mutated oncogene. However, the development of
conventional K-RAS inhibitors has been extremely challenging, with a mutation-specific …
conventional K-RAS inhibitors has been extremely challenging, with a mutation-specific …
An affinity-directed protein missile system for targeted proteolysis
The von Hippel–Lindau (VHL) protein serves to recruit the hypoxia-inducible factor alpha
(HIF1α) protein under normoxia to the CUL2 E3 ubiquitin ligase for its ubiquitylation and …
(HIF1α) protein under normoxia to the CUL2 E3 ubiquitin ligase for its ubiquitylation and …
Development of BromoTag: a “bump-and-hole”–PROTAC system to induce potent, rapid, and selective degradation of tagged target proteins
Small-molecule-induced protein depletion technologies, also called inducible degrons,
allow degradation of genetically engineered target proteins within cells and animals. Here …
allow degradation of genetically engineered target proteins within cells and animals. Here …
Covalently engineered nanobody chimeras for targeted membrane protein degradation
H Zhang, Y Han, Y Yang, F Lin, K Li… - Journal of the …, 2021 - ACS Publications
The targeted degradation of membrane proteins would afford an attractive and general
strategy for treating various diseases that remain difficult with the current proteolysis …
strategy for treating various diseases that remain difficult with the current proteolysis …
In vivo knockdown of pathogenic proteins via specific and nongenetic inhibitor of apoptosis protein (IAP)-dependent protein erasers (SNIPERs)
N Ohoka, K Okuhira, M Ito, K Nagai, N Shibata… - Journal of Biological …, 2017 - ASBMB
Many diseases, especially cancers, result from aberrant or overexpression of pathogenic
proteins. Specific inhibitors against these proteins have shown remarkable therapeutic …
proteins. Specific inhibitors against these proteins have shown remarkable therapeutic …
Development of a small hybrid molecule that mediates degradation of His-Tag fused proteins
K Okitsu, T Hattori, T Misawa, T Shoda… - Journal of Medicinal …, 2018 - ACS Publications
In recent years, the induction of target–protein degradation via the ubiquitin–proteasome
system (UPS) mediated by small molecules has attracted attention, and this approach has …
system (UPS) mediated by small molecules has attracted attention, and this approach has …
[HTML][HTML] SNIPERs—Hijacking IAP activity to induce protein degradation
M Naito, N Ohoka, N Shibata - Drug Discovery Today: Technologies, 2019 - Elsevier
The induction of protein degradation by chimeric small molecules represented by proteolysis-
targeting chimeras (PROTACs) is an emerging approach for novel drug development. We …
targeting chimeras (PROTACs) is an emerging approach for novel drug development. We …
Bifunctional small molecules that mediate the degradation of extracellular proteins
Targeted protein degradation (TPD) has emerged as a promising therapeutic strategy. Most
TPD technologies use the ubiquitin–proteasome system, and are therefore limited to …
TPD technologies use the ubiquitin–proteasome system, and are therefore limited to …