Discovery of the first ataxia telangiectasia and Rad3-related (ATR) degraders for cancer treatment

L Huang, J Shao, W Lai, H Gu, J Yang, S Shi… - European Journal of …, 2024 - Elsevier
The first examples of ataxia telangiectasia and Rad3-related (ATR) PROTACs were
designed and synthesized. Among them, the most potent degrader, ZS-7, demonstrated …

[HTML][HTML] Thalidomide derivatives degrade BCL-2 by reprogramming the binding surface of CRBN

J Wang, M Heinz, K Han, VJ Shah… - Cell Reports Physical …, 2024 - cell.com
Recent studies demonstrate that modified thalidomide chemically alters the binding surface
of its binding E3 ligase, CRBN, leading to the degradation of new substrate proteins. In this …

From classic medicinal chemistry to state‐of‐the‐art interdisciplinary medicine: Recent advances in proteolysis‐targeting chimeras technology

X Zhao, Y Chen, H Su, L Zhang - Interdisciplinary Medicine, 2023 - Wiley Online Library
Proteolysis‐targeting chimeras (PROTACs) is a targeted protein degradation (TPD)
technique effected by hijacking the ubiquitin‐proteasome system (UPS) of the cells. A …

mRNA PROTACs: engineering PROTACs for high‐efficiency targeted protein degradation

X Xue, C Zhang, X Li, J Wang, H Zhang, Y Feng… - MedComm, 2024 - Wiley Online Library
Proteolysis‐targeting chimeras (PROTACs) are essential bifunctional molecules that target
proteins of interest (POIs) for degradation by cellular ubiquitination machinery. Despite …

Design, synthesis, and evaluation of BCL‐2 targeting PROTACs

A Bricelj, YLD Ng, M Gobec, R Kuchta… - … A European Journal, 2024 - Wiley Online Library
BCL‐2, a member of the BCL‐2 protein family, is an antiapoptotic factor that regulates the
intrinsic pathway of apoptosis. Due to its aberrant activity, it is frequently implicated in …

Mivebresib synergized with PZ703b, a novel Bcl-xl PROTAC degrader, induces apoptosis in bladder cancer cells via the mitochondrial pathway

Y Xu, Z Lei, J Zhu, L Wan - Biochemical and Biophysical Research …, 2022 - Elsevier
Bladder cancer is a common urinary cancer that still lacks effective treatments. In the present
study, we evaluated the effect of BET inhibitor, mivebresib, in combination with PZ703b, a …

[HTML][HTML] Single-cell RNA sequencing reveals the effects of hederasaponin C in the treatment of diabetic nephropathy

J Liu, Q Zhang, W Zhao, J Guo, YK Wong… - Acta Materia …, 2023 - ucl.scienceopen.com
There is great demand for the development of novel efficient therapeutic strategies or
preventative measures to alleviate the life-threatening complications of type 2 diabetes …

Computational Modeling of PROTAC Ternary Complexes and Linker Design

SA Miller, GV Andrianov, V Mischley… - … Chemical Biology to …, 2023 - Wiley Online Library
Proteolysis targeting chimeras (PROTACs) are heterobifunctional ligands that promote
targeted protein degradation (TPD) by reprogramming E3 ubiquitin ligase activity. By affixing …

Advances in Preclinical Mantle Cell Lymphoma Research: A Novel Combination Regimen and a Novel Mouse Model

FD Brown - 2023 - rave.ohiolink.edu
Abstract Mantle Cell Lymphoma (MCL) is a B cell lymphoma distinguished from other B cell
lymphomas by at (11; 14)(q13: q32) translocation juxtaposing the CCND1 gene downstream …

HDAC3 and HDAC8 PROTAC dual degrader reveals roles of histone acetylation in gene regulation

Y Xiao, S Hale, N Awasthee, C Meng, X Zhang… - Cell chemical …, 2023 - cell.com
HDAC3 and HDAC8 have critical biological functions and represent highly sought-after
therapeutic targets. Because histone deacetylases (HDACs) have a very conserved catalytic …