[HTML][HTML] Commentary: PROTACs make undruggable targets druggable: challenge and opportunity

B Lu, J Ye - Acta Pharmaceutica Sinica. B, 2021 - ncbi.nlm.nih.gov
… Navitoclax is an inhibitor of BCL-XL, which is a potential anti-cancerBCL-XL degrader
DT2216 (navitoclax fused to a VHL-… a safe and effective first-in-class anticancer agent targeting …

Degraders Upgraded: The Rise of PROTACs in Hematological Malignancies

JML Casan, JF Seymour - Blood, 2024 - Elsevier
degrader that retards cellular proliferation and induces apoptosis in multiple cancer cell lines.
Selective STAT3 depletion was achieved over … , a BCL-XL targeting PROTAC that engages …

Recent advances in small molecule PROTACs for the treatment of cancer

W Li, RM Elhassan, X Hou… - Current medicinal …, 2021 - ingentaconnect.com
… , high doses are required to achieve biological activity in vivo, which … Bcl-2, Mcl-1 and Bcl-xL,
is a vital reason for tumor cells to … the PROTAC strategy has a powerful ability to degrade

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] 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, …

[HTML][HTML] Using proteolysis-targeting chimera technology to reduce navitoclax platelet toxicity and improve its senolytic activity

Y He, X Zhang, J Chang, HN Kim, P Zhang… - Nature …, 2020 - nature.com
… Here, we report the use of PROTAC technology to reduce … and synthesized a series of
Bcl-xl-Ps that target Bcl-xl to CRBN for … to degrade Bcl-xl and selectively induce IR-SC apoptosis. …

[HTML][HTML] Inhibition of anti-apoptotic Bcl-2 proteins in preclinical and clinical studies: current overview in cancer

S D'Aguanno, D Del Bufalo - Cells, 2020 - mdpi.com
… We and others previously reported the link of Bcl-xL protein … a Bcl-xL proteolysis-targeting
chimera (PROTAC) that targets … have potent in vitro proliferation inhibitory effect and to achieve

Recent Progress in DNA Damage Response-Targeting PROTAC Degraders

B Cheng, X Fei, Z Ding, X Peng, Z Su… - Journal of Medicinal …, 2024 - ACS Publications
… protein degradation achieved by a specific PROTAC molecule … In a SW620 xenograft
model, 4 displayed potent antitumor … inhibitor into a selective/specific PROTAC degrader. This …

Selectivity through Targeted Protein Degradation (TPD) Miniperspective

A Gopalsamy - Journal of Medicinal Chemistry, 2022 - ACS Publications
… binder but still achieve a high degree of selective degradation. One of … degraded by VHL
PROTAC 8, 14 kinases were degraded by cereblon PROTAC 9, and 6 kinases were degraded

[HTML][HTML] Peptide-based PROTAC degrader of FOXM1 suppresses cancer and decreases GLUT1 and PD-L1 expression

K Wang, X Dai, A Yu, C Feng, K Liu… - Journal of Experimental & …, 2022 - Springer
… Here, we develop a peptide-based PROTAC, which achieves the purpose of degrading
FOXM1 by facilitating the recruitment of E3 ubiquitin to FOXM1. Phage display technology was …