Unexpected discoveries in the targeted protein degradation of squalene synthase and DCAF15
JGF Hoock - 2023 - orbit.dtu.dk
Protein degradation is a universal process performed by human cells to recycle unused
proteins and to adapt to an ever-changing environment. Targeted protein degradation (TPD) …
proteins and to adapt to an ever-changing environment. Targeted protein degradation (TPD) …
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 …
[HTML][HTML] Identification of non-conventional small molecule degraders and stabilizers of squalene synthase
JGF Hoock, C Rossetti, M Bilgin, L Depta… - Chemical …, 2023 - pubs.rsc.org
Squalene synthase (SQS) is an essential enzyme in the mevalonate pathway, which
controls cholesterol biosynthesis and homeostasis. Although catalytic inhibitors of SQS have …
controls cholesterol biosynthesis and homeostasis. Although catalytic inhibitors of SQS have …
[HTML][HTML] Special Focus Issue–Targeted protein degradation: a new paradigm in medicinal chemistry
H Wall - Future Medicinal Chemistry, 2022 - Taylor & Francis
Targeted protein degradation by small-molecule degraders represents a new and exciting
mode of action in drug discovery. Proteolysis-targeting chimeras (PROTACs) represent a …
mode of action in drug discovery. Proteolysis-targeting chimeras (PROTACs) represent a …
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 …
Targeting the Undruggables----the Power of Protein Degraders
C Zhang, Y Liu, G Li, Z Yang, C Han, X Sun, C Sheng… - Science Bulletin, 2024 - Elsevier
Undruggable targets typically refer to a class of therapeutic targets that are difficult to target
through conventional methods or have not yet been targeted, but are of great clinical …
through conventional methods or have not yet been targeted, but are of great clinical …
PROTAC-mediated Target
H WEINMANN - … : Successful Strategies in Drug Discovery and …, 2020 - books.google.com
In the constant pursuit of medicinal chemistry to expand the druggable space and develop
novel strategies to target essential disease driving proteins, small-molecule-induced protein …
novel strategies to target essential disease driving proteins, small-molecule-induced protein …
[图书][B] Inducing Targeted Protein Degradation: From Chemical Biology to Drug Discovery and Clinical Applications
P Cromm - 2022 - books.google.com
Inducing Targeted Protein Degradation Enables drug developers in academia and industry
to expand the range of accessible drug targets through induced protein degradation Since …
to expand the range of accessible drug targets through induced protein degradation Since …
Targeted Protein Degradation
AM Cacace, CM Hickey, M Békés - Springer
Molecules designed to induce ubiquitylation and subsequent degradation of specific target
proteins have become the focus of intense research interest across the biotech and …
proteins have become the focus of intense research interest across the biotech and …
Targeted Protein Degradation
D Kotlarek, A Pawlik, M Sagan… - Technology Transfer …, 2020 - ingentaconnect.com
Targeted Protein Degradation (TPD) is an emerging new modality of drug discovery that
offers unprecedented therapeutic benefits over traditional protein inhibition. Most …
offers unprecedented therapeutic benefits over traditional protein inhibition. Most …
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