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 …
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
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 …
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 …
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 …
proteins of interest (POIs) for degradation by cellular ubiquitination machinery. Despite …
Design, synthesis, and evaluation of BCL‐2 targeting PROTACs
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 …
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 …
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 …
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 …
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 …
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
HDAC3 and HDAC8 have critical biological functions and represent highly sought-after
therapeutic targets. Because histone deacetylases (HDACs) have a very conserved catalytic …
therapeutic targets. Because histone deacetylases (HDACs) have a very conserved catalytic …