Current advances and development strategies of orally bioavailable PROTACs
S Zeng, Y Ye, H Xia, J Min, J Xu, Z Wang, Y Pan… - European Journal of …, 2023 - Elsevier
Proteolysis-targeting chimeras (PROTACs) have been an area of intensive research with the
potential to extend drug space not target to traditional molecules. In the last half decade, we …
potential to extend drug space not target to traditional molecules. In the last half decade, we …
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 …
Clinical translation of targeted protein degraders
NR Kong, LH Jones - Clinical Pharmacology & Therapeutics, 2023 - Wiley Online Library
Targeted protein degradation (TPD) has emerged as a potentially transformational
therapeutic modality with considerable promise. Molecular glue degraders remodel the …
therapeutic modality with considerable promise. Molecular glue degraders remodel the …
Targeted degradation of extracellular secreted and membrane proteins
Targeted protein degradation (TPD) involving chimeric molecules has emerged as one of
the most promising therapeutic modalities in recent years. Among various reported TPD …
the most promising therapeutic modalities in recent years. Among various reported TPD …
Development of a covalent cereblon-based PROTAC employing a fluorosulfate warhead
RP Nowak, L Ragosta, F Huerta, H Liu… - RSC Chemical …, 2023 - pubs.rsc.org
Many cereblon (CRBN) ligands have been used to develop proteolysis targeting chimeras
(PROTACs), but all are reversible binders of the E3 ubiquitin ligase. We recently described …
(PROTACs), but all are reversible binders of the E3 ubiquitin ligase. We recently described …
Application and challenges of nitrogen heterocycles in PROTAC linker
Y Li, J Qu, L Jiang, X Peng, K Wu, M Chen… - European Journal of …, 2024 - Elsevier
The absence of effective active pockets makes traditional molecularly targeted drug
strategies ineffective against 80% of human disease-related proteins. The PROTAC …
strategies ineffective against 80% of human disease-related proteins. The PROTAC …
Selective and potent PROTAC degraders of c-Src kinase
W Mao, NM Vandecan, CR Bingham… - ACS Chemical …, 2023 - ACS Publications
Using dasatinib linked to E3 ligase ligands, we identified a potent and selective dual Csk/c-
Src PROTAC degrader. We then replaced dasatinib, the c-Src-directed ligand, with a …
Src PROTAC degrader. We then replaced dasatinib, the c-Src-directed ligand, with a …
[HTML][HTML] ALK inhibitors in cancer: mechanisms of resistance and therapeutic management strategies
D Poei, S Ali, S Ye, R Hsu - Cancer Drug Resistance, 2024 - ncbi.nlm.nih.gov
Anaplastic lymphoma kinase (ALK) gene rearrangements have been identified as potent
oncogenic drivers in several malignancies, including non-small cell lung cancer (NSCLC) …
oncogenic drivers in several malignancies, including non-small cell lung cancer (NSCLC) …
[HTML][HTML] Characteristic roadmap of linker governs the rational design of PROTACs
Y Dong, T Ma, T Xu, Z Feng, Y Li, L Song, X Yao… - … Pharmaceutica Sinica B, 2024 - Elsevier
Proteolysis targeting chimera (PROTAC) technology represents a groundbreaking
development in drug discovery, leveraging the ubiquitin‒proteasome system to specifically …
development in drug discovery, leveraging the ubiquitin‒proteasome system to specifically …
Targeting fusion oncoproteins in childhood cancers: challenges and future opportunities for developing therapeutics
SK Verma, KL Witkin, A Sharman… - JNCI: Journal of the …, 2024 - academic.oup.com
Fusion oncoproteins are associated with childhood cancers and have proven challenging to
target, aside from those that include kinases. As part of its efforts for targeting childhood …
target, aside from those that include kinases. As part of its efforts for targeting childhood …