Unifying catalysis framework to dissect proteasomal degradation paradigms
FP Rodriguez-Rivera, SM Levi - ACS Central Science, 2021 - ACS Publications
Diverging from traditional target inhibition, proteasomal protein degradation approaches
have emerged as novel therapeutic modalities that embody distinct pharmacological profiles …
have emerged as novel therapeutic modalities that embody distinct pharmacological profiles …
Inducing the degradation of Disease-related proteins using heterobifunctional molecules
Current drug development strategies that target either enzymatic or receptor proteins for
which specific small molecule ligands can be designed for modulation, result in a large …
which specific small molecule ligands can be designed for modulation, result in a large …
Critical assessment of targeted protein degradation as a research tool and pharmacological modality
Small molecules continue to dominate drug discovery because of their ease of use, lower
cost of manufacturing, and access to intracellular targets. However, despite these …
cost of manufacturing, and access to intracellular targets. However, despite these …
Targeted protein degradation mechanisms
Y Zhang, C Loh, J Chen, N Mainolfi - Drug Discovery Today: Technologies, 2019 - Elsevier
Targeted protein degradation mediated by small molecule degraders represents an exciting
new therapeutic opportunity to eliminate disease-causing proteins. These molecules recruit …
new therapeutic opportunity to eliminate disease-causing proteins. These molecules recruit …
The importance of cellular degradation kinetics for understanding mechanisms in targeted protein degradation
Targeted protein degradation has exploded over the past several years due to preclinical
and early clinical therapeutic success of numerous compounds, and the emergence of new …
and early clinical therapeutic success of numerous compounds, and the emergence of new …
Small-molecule degraders beyond PROTACs—challenges and opportunities
JM Kastl, G Davies, E Godsman… - … the Science of Drug …, 2021 - journals.sagepub.com
Targeted protein degradation (TPD) is a recent strategy, utilizing the cell's proteostasis
machinery to deplete specific proteins. This represents a paradigm shift in early drug …
machinery to deplete specific proteins. This represents a paradigm shift in early drug …
Perspectives on the development of first-in-class protein degraders
KM Rambacher, MF Calabrese… - Future Medicinal …, 2021 - Taylor & Francis
Targeted protein degradation is a broad and expanding field aimed at the modulation of
protein homeostasis. A focus of this field has been directed toward molecules that hijack the …
protein homeostasis. A focus of this field has been directed toward molecules that hijack the …
Identification and selectivity profiling of small-molecule degraders via multi-omics approaches
NS Scholes, C Mayor-Ruiz, GE Winter - Cell Chemical Biology, 2021 - cell.com
The therapeutic modality of targeted protein degradation promises to overcome limitations of
traditional pharmacology. Small-molecule degraders recruit disease-causing proteins to E3 …
traditional pharmacology. Small-molecule degraders recruit disease-causing proteins to E3 …
Targeted protein degradation: from mechanisms to clinic
Targeted protein degradation refers to the use of small molecules to induce the selective
degradation of proteins. In its most common form, this degradation is achieved through …
degradation of proteins. In its most common form, this degradation is achieved through …
From Degraders to Molecular Glues: New Ways of Breaking Down Disease‐Associated Proteins
YA Nagel, A Britschgi, A Ricci - Successful Drug Discovery, 2021 - Wiley Online Library
Targeted protein degradation is becoming a weapon of choice against targets considered
heretofore “undruggable.” Whereas most small molecules inhibit a protein by blocking its …
heretofore “undruggable.” Whereas most small molecules inhibit a protein by blocking its …