Chasing molecular glue degraders: screening approaches
A Domostegui, L Nieto-Barrado… - Chemical Society …, 2022 - pubs.rsc.org
… Here, we provide an overview of the “molecular glue” concept, … clinical and preclinical
molecular glue degraders, and discuss … , molecular glue degraders can induce the degradation of …
molecular glue degraders, and discuss … , molecular glue degraders can induce the degradation of …
Haven't got a glue: protein surface variation for the design of molecular glue degraders
… in ubiquitination and subsequent degradation of the recruited … already work as molecular
glue degraders, with many more … by monovalent degraders, with a focus on molecular glues …
glue degraders, with many more … by monovalent degraders, with a focus on molecular glues …
Rational discovery of molecular glue degraders via scalable chemical profiling
C Mayor-Ruiz, S Bauer, M Brand, Z Kozicka… - Nature chemical …, 2020 - nature.com
… be liganded via small organic molecules. Conversely, molecular glue degraders were shown
to … thalidomide analogs (IMiDs) as molecular glue degraders exemplify how this particular …
to … thalidomide analogs (IMiDs) as molecular glue degraders exemplify how this particular …
Rational chemical design of molecular glue degraders
ES Toriki, JW Papatzimas, K Nishikawa… - ACS central …, 2023 - ACS Publications
… Targeted protein degradation with molecular glue degraders … through proteasome-mediated
degradation. However, we … -targeting ligands into molecular glue degraders. To overcome …
degradation. However, we … -targeting ligands into molecular glue degraders. To overcome …
Emerging strategies for prospective discovery of molecular glue degraders
… degradation of the target. Proteolysis-targeting chimeras (PROTACs) and molecular glue
(MG) degraders are two major classes of protein degraders (Figure 1a). PROTACs are bivalent …
(MG) degraders are two major classes of protein degraders (Figure 1a). PROTACs are bivalent …
Profiling the landscape of drug resistance mutations in neosubstrates to molecular glue degraders
… To identify candidate drug resistance mechanisms to molecular glue degraders, we … treated
with either vehicle or the appropriate molecular glue degraders to select for candidate drug …
with either vehicle or the appropriate molecular glue degraders to select for candidate drug …
Discovery of molecular glue degraders via isogenic morphological profiling
A Ng, F Offensperger, JA Cisneros… - ACS Chemical …, 2023 - ACS Publications
Molecular glue degraders (MGDs) are small molecules that degrade proteins of interest via
the ubiquitin–proteasome system. While MGDs were historically discovered serendipitously, …
the ubiquitin–proteasome system. While MGDs were historically discovered serendipitously, …
Design principles for cyclin K molecular glue degraders
Z Kozicka, DJ Suchyta, V Focht, G Kempf… - Nature chemical …, 2024 - nature.com
… Of particular interest are molecular glue degraders, which … discoveries of other molecular
glue degraders 7,8,9,10,11,12,… (CDK) inhibitor, is a molecular glue degrader that binds CDK12–…
glue degraders 7,8,9,10,11,12,… (CDK) inhibitor, is a molecular glue degrader that binds CDK12–…
Novel mechanisms of molecular glue-induced protein degradation
S Alabi - Biochemistry, 2021 - ACS Publications
… molecular glues have exceptional promise as a therapeutic modality. (1) Thus far, molecular
glue degraders … molecular glues can be utilized to induce the degradation of neosubstrates. …
glue degraders … molecular glues can be utilized to induce the degradation of neosubstrates. …
Simple structural modifications converting a bona fide MDM2 PROTAC degrader into a molecular glue molecule: a cautionary tale in the design of PROTAC degraders
… a PROTAC MDM2 degrader but instead works as a molecular glue, inducing degradation of
a … can convert a bona fide PROTAC degrader into a molecular glue compound, which has a …
a … can convert a bona fide PROTAC degrader into a molecular glue compound, which has a …
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