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 …
Emerging and Re-emerging Warheads for Targeted Covalent Inhibitors: An Update
L Hillebrand, XJ Liang, RAM Serafim… - Journal of Medicinal …, 2024 - ACS Publications
Covalent inhibitors and other types of covalent modalities have seen a revival in the past two
decades, with a variety of new targeted covalent drugs having been approved in recent …
decades, with a variety of new targeted covalent drugs having been approved in recent …
Discovery of a Highly Potent and Selective BRD9 PROTAC Degrader Based on E3 Binder Investigation for the Treatment of Hematological Tumors
H Duan, J Zhang, R Gui, Y Lu, A Pang… - Journal of Medicinal …, 2024 - ACS Publications
BRD9 is a pivotal epigenetic factor involved in cancers and inflammatory diseases. Still, the
limited selectivity and poor phenotypic activity of targeted agents make it an atypically …
limited selectivity and poor phenotypic activity of targeted agents make it an atypically …
Structure-guided design and optimization of covalent VHL-targeted sulfonyl fluoride PROTACs
RR Shah, E De Vita, PS Sathyamurthi… - Journal of Medicinal …, 2024 - ACS Publications
Proteolysis-targeting chimeras (PROTACs) are heterobifunctional molecules that have
emerged as a therapeutic modality to induce targeted protein degradation (TPD) by …
emerged as a therapeutic modality to induce targeted protein degradation (TPD) by …
Breaking Bad Proteins—Discovery Approaches and the Road to Clinic for Degraders
Proteolysis-targeting chimeras (PROTACs) describe compounds that bind to and induce
degradation of a target by simultaneously binding to a ubiquitin ligase. More generally …
degradation of a target by simultaneously binding to a ubiquitin ligase. More generally …
Synthetic modification of protein surfaces to mediate induced-proximity pharmacology
LH Jones - RSC Medicinal Chemistry, 2024 - pubs.rsc.org
Molecular glues and bifunctional small molecules, such as targeted protein degraders,
induce protein proximity to mediate gain-of-function pharmacology. Emerging technologies …
induce protein proximity to mediate gain-of-function pharmacology. Emerging technologies …
Development of sulfonyl fluoride chemical probes to advance the discovery of cereblon modulators
Sulfonyl fluoride EM12-SF was developed previously to covalently engage a histidine
residue in the sensor loop of cereblon (CRBN) in the E3 ubiquitin ligase complex …
residue in the sensor loop of cereblon (CRBN) in the E3 ubiquitin ligase complex …
PROTACs: Principles and Mechanisms
RS Saluja, MP Vaidya, PS Kharkar - PROTAC-Mediated Protein …, 2024 - Springer
Abstract Proteolysis Targeting Chimeras (PROTACs), a groundbreaking technology that has
revolutionized the landscape of targeted protein degradation and therapeutics, is a clinically …
revolutionized the landscape of targeted protein degradation and therapeutics, is a clinically …
Development and characterization of the first selective class IIb histone deacetylase degraders
S Zhai, L Schäker-Hübner, M Hanl, L Jacobi… - 2024 - chemrxiv.org
Proteolysis-targeting chimeras (PROTACs) are emerging new therapeutic modalities that
facilitate the targeted degradation of disease-relevant proteins via an event-driven mode of …
facilitate the targeted degradation of disease-relevant proteins via an event-driven mode of …
Targeting the STAT3 pathway with STAT3 degraders
Z Wang, X Liao, H He, X Guo, J Chen - Trends in Pharmacological …, 2024 - cell.com
Signal transducer and activator of transcription 3 (STAT3) has been widely considered as a
therapeutic target for various diseases, especially tumors. Thus far, several STAT3 inhibitors …
therapeutic target for various diseases, especially tumors. Thus far, several STAT3 inhibitors …