[HTML][HTML] Discovery of E3 ligase ligands for target protein degradation

J Lee, Y Lee, YM Jung, JH Park, HS Yoo, J Park - Molecules, 2022 - mdpi.com
… a PG (12)-based PROTAC, SJ10542, with highly selective JAK … a selective degrader of
HDAC3 with a submicromolar activity … 31 showed a powerful anticancer activity in breast, ovarian, …

Design, Synthesis, and Biological Evaluation of Selective TBL1X Degraders and PP2A Activators & Refinement of SARS-CoV-2 Envelope Protein Structure in a Native …

R Yang - 2023 - search.proquest.com
… potential as a PROTAC in effectively and selectively degrading … levels and demonstrated
strong antitumor activity in mice … targeted a band region on BCL-xL for ubiquitination, indicating …

Strategies toward discovery of potent and orally bioavailable proteolysis targeting chimera degraders of androgen receptor for the treatment of prostate cancer

X Han, L Zhao, W Xiang, C Qin, B Miao… - Journal of medicinal …, 2021 - ACS Publications
… of an orally active PROTAC AR degrader for the treatment of … , the design of PROTAC degraders
to achieve excellent oral … strategies toward discovering potent PROTAC degraders of AR …

[HTML][HTML] Cancer-specific delivery of proteolysis-targeting chimeras (PROTACs) and their application to cancer immunotherapy

Y Moon, SI Jeon, MK Shim, K Kim - Pharmaceutics, 2023 - mdpi.com
… The same research group also carried out a series of experiments for the design of the most
effective mAb-PROTAC conjugates using BRD4-degrading PROTACs [99,100]. They have …

Design, synthesis, and biological evaluation of novel protopanoxadiol derivatives based PROTACs technology for the treatment of lung cancer

P Wang, H Zhu, J Liu, S Xu, Y Chen, J Xu, Y Zhao… - Bioorganic …, 2023 - Elsevier
… trials in 2019 and achieved satisfactory safety and efficacy … A05 exhibited the most potent
antitumor activity with an IC 50 … In summary, by introducing different PROTAC substitutions at …

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
PROTAC technology achieves targeted protein degradation … of PROTAC technology, molecular
glue technology, degrader-… exhibited minimal degradation of BCL-XL in platelets, and in …

Stimuli-activatable PROTACs for precise protein degradation and cancer therapy

J Gao, L Yang, S Lei, F Zhou, H Nie, B Peng, T Xu… - Science bulletin, 2023 - Elsevier
PROTAC prodrug-based nanomedicine to improve PROTAC … ha-PROTAC behaved potent
EGFR-degrading activity in a … to activate the PROTAC prodrugs and achieve precise protein …

[HTML][HTML] Targeted protein degradation: A promising approach for cancer treatment

MZI Khan, A Nazli, I Naz, D Khan, I Haq… - Journal of Pharmaceutical …, 2023 - Elsevier
… -E3” complex and is sufficient to achieve appropriate … the ability of a PROTAC to degrade
the targeted protein [84]. The … -based BCL-XL PROTAC XZ739 showed 20 times more potency

[HTML][HTML] Targeting protein degradation pathways in tumors: Focusing on their role in hematological malignancies

A Wolska-Washer, P Smolewski - Cancers, 2022 - mdpi.com
… PROTACs drive POIs into the UPS degrading system by … fact that both sites achieved similar
PROTAC exposure. Perhaps … latter effect was paralleled by a significant reduction in Bcl-xL

[PDF][PDF] Constructing a warhead of PROTAC with aptamer for tumor-selective degradation of nucleolin

L Zhang, L Li, X Wang, J Dai, L Zhou, Y Zhang, T Xie… - researchgate.net
… -PROTAC conjugate could achieve targeted antitumor activity … E3 ligases and still degrade
nucleolin. PROTACs promote … PROTAC to degrade its target are questions that need further …