[HTML][HTML] Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules
Chemical biology strategies for directly perturbing protein homeostasis including the
degradation tag (dTAG) system provide temporal advantages over genetic approaches and …
degradation tag (dTAG) system provide temporal advantages over genetic approaches and …
The dTAG system for immediate and target-specific protein degradation
Dissection of complex biological systems requires target-specific control of the function or
abundance of proteins. Genetic perturbations are limited by off-target effects …
abundance of proteins. Genetic perturbations are limited by off-target effects …
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 …
[HTML][HTML] Targeted degradation via direct 26S proteasome recruitment
C Bashore, S Prakash, MC Johnson… - Nature Chemical …, 2023 - nature.com
Engineered destruction of target proteins by recruitment to the cell's degradation machinery
has emerged as a promising strategy in drug discovery. The majority of molecules that …
has emerged as a promising strategy in drug discovery. The majority of molecules that …
[HTML][HTML] Targeted protein degradation via intramolecular bivalent glues
O Hsia, M Hinterndorfer, AD Cowan, K Iso, T Ishida… - Nature, 2024 - nature.com
Targeted protein degradation is a pharmacological modality that is based on the induced
proximity of an E3 ubiquitin ligase and a target protein to promote target ubiquitination and …
proximity of an E3 ubiquitin ligase and a target protein to promote target ubiquitination and …
Small-molecule hydrophobic tagging–induced degradation of HaloTag fusion proteins
TK Neklesa, HS Tae, AR Schneekloth… - Nature chemical …, 2011 - nature.com
The ability to regulate any protein of interest in living systems with small molecules remains
a challenge. We hypothesized that appending a hydrophobic moiety to the surface of a …
a challenge. We hypothesized that appending a hydrophobic moiety to the surface of a …
[HTML][HTML] A method for the acute and rapid degradation of endogenous proteins
Methods for the targeted disruption of protein function have revolutionized science and
greatly expedited the systematic characterization of genes. Two main approaches are …
greatly expedited the systematic characterization of genes. Two main approaches are …
HaloPROTACS: use of small molecule PROTACs to induce degradation of HaloTag fusion proteins
DL Buckley, K Raina, N Darricarrere, J Hines… - ACS chemical …, 2015 - ACS Publications
Small molecule-induced protein degradation is an attractive strategy for the development of
chemical probes. One method for inducing targeted protein degradation involves the use of …
chemical probes. One method for inducing targeted protein degradation involves the use of …
Targeted protein degradation as a powerful research tool in basic biology and drug target discovery
Controlled perturbation of protein activity is essential to study protein function in cells and
living organisms. Small molecules that hijack the cellular protein ubiquitination machinery to …
living organisms. Small molecules that hijack the cellular protein ubiquitination machinery to …
Merging PROTAC and molecular glue for degrading BTK and GSPT1 proteins concurrently
Z Yang, Y Sun, Z Ni, C Yang, Y Tong, Y Liu, H Li… - Cell Research, 2021 - nature.com
Dear Editor, Targeted protein degradation (TPD) represents a promising research field that
has quickly attracted attention and efforts from both academia and pharmaceutical industry …
has quickly attracted attention and efforts from both academia and pharmaceutical industry …