Targeted protein modification as a paradigm shift in drug discovery
Abstract Targeted Protein Modification (TPM) is an umbrella term encompassing numerous
tools and approaches that use bifunctional agents to induce a desired modification over the …
tools and approaches that use bifunctional agents to induce a desired modification over the …
Novel approaches to targeted protein degradation technologies in drug discovery
Y Xue, AA Bolinger, J Zhou - Expert opinion on drug discovery, 2023 - Taylor & Francis
Introduction Target protein degradation (TPD) provides a novel therapeutic modality, other
than inhibition, through the direct depletion of target proteins. Two primary human protein …
than inhibition, through the direct depletion of target proteins. Two primary human protein …
Dual roles of FAK in tumor angiogenesis: A review focused on pericyte FAK
J Zhang, W Li, W Wang, Q Chen, Z Xu, M Deng… - European Journal of …, 2023 - Elsevier
Focal adhesion kinase (FAK), also known as protein tyrosine kinase 2 (PTK2), is a
ubiquitously expressed non-receptor tyrosine kinase, that plays a pivotal role in integrin …
ubiquitously expressed non-receptor tyrosine kinase, that plays a pivotal role in integrin …
Proteolysis-targeting chimeras in biotherapeutics: Current trends and future applications
The success of inhibitor-based therapeutics is largely constrained by the acquisition of
therapeutic resistance, which is partially driven by the undruggable proteome. The …
therapeutic resistance, which is partially driven by the undruggable proteome. The …
Small molecule tractable PARP inhibitors: Scaffold construction approaches, mechanistic insights and structure activity relationship
A Thakur, M Rana, J Mathew, S Nepali, CH Pan… - Bioorganic …, 2023 - Elsevier
Diverse drug design strategies viz. molecular hybridization, substituent installation, scaffold
hopping, isosteric replacement, high-throughput screening, induction and separation of …
hopping, isosteric replacement, high-throughput screening, induction and separation of …
[HTML][HTML] PROTACs in gastrointestinal cancers
Y Chen, Q Yang, J Xu, L Tang, Y Zhang, F Du… - Molecular Therapy …, 2022 - cell.com
Proteolysis targeting chimera (PROTAC) presents a powerful strategy for targeted protein
degradation (TPD). The heterobifunctional PROTAC molecule consists of an E3 ligase …
degradation (TPD). The heterobifunctional PROTAC molecule consists of an E3 ligase …
Discovery of the GSH responsive “Y-PROTACs” targeting ALK and CDK4/6 as a potential treatment for cancer
S Wang, D Luo, C Pu, X Ma, H Zhang, Z Feng… - European Journal of …, 2023 - Elsevier
Combination of different molecular target inhibitors is an available method to improve the
therapeutic effect on tumors. Herein, to achieve both tumor cell targeting and ALK …
therapeutic effect on tumors. Herein, to achieve both tumor cell targeting and ALK …
[HTML][HTML] PROTACs in the management of prostate cancer
P Yedla, AO Babalghith, VV Andra, R Syed - Molecules, 2023 - mdpi.com
Cancer treatments with targeted therapy have gained immense interest due to their low
levels of toxicity and high selectivity. Proteolysis-Targeting Chimeras (PROTACs) have …
levels of toxicity and high selectivity. Proteolysis-Targeting Chimeras (PROTACs) have …
[HTML][HTML] From PROTAC to TPD: Advances and Opportunities in Targeted Protein Degradation
S Wang, F He, C Tian, A Sun - Pharmaceuticals, 2024 - mdpi.com
PROTAC is a rapidly developing engineering technology for targeted protein degradation
using the ubiquitin–proteasome system, which has promising applications for inflammatory …
using the ubiquitin–proteasome system, which has promising applications for inflammatory …
[HTML][HTML] PROTACs: Current and Future Potential as a Precision Medicine Strategy to Combat Cancer
KA Rutherford, KJ McManus - Molecular Cancer Therapeutics, 2024 - AACR
Proteolysis targeting chimeras (PROTAC) are an emerging precision medicine strategy,
which targets key proteins for proteolytic degradation to ultimately induce cancer cell killing …
which targets key proteins for proteolytic degradation to ultimately induce cancer cell killing …