Results 41 to 50 of about 11,335 (243)

The Potential of Proteolytic Chimeras as Pharmacological Tools and Therapeutic Agents

Molecules, 2020
The induction of protein degradation in a highly selective and efficient way by means of druggable molecules is known as targeted protein degradation (TPD).
Bernat Coll-Martínez, Antonio Delgado, Bernat Crosas   +2 more
doaj   +1 more source

PROTAC technology for the treatment of Alzheimer’s disease: advances and perspectives

Acta Materia Medica, 2022
Neurodegenerative diseases are characterized by the progression of neuronal degeneration, resulting in dysfunction of cognition and mobility. Many neurodegenerative diseases are due to proteinopathies arising from unusual protein accumulation and ...
Hiroyuki Inuzuka, Jing Liu, Wenyi Wei, Abdol-Hossein Rezaeian   +3 more
doaj   +1 more source

Nanotherapies for Atherosclerosis: Targeting, Catalysis, and Energy Transduction

Advanced Healthcare Materials, EarlyView.
Atherosclerosis management is hindered by poor drug targeting and plaque heterogeneity. Nanotechnology overcomes these barriers via three core strategies: (1) target‐engineered nanocarriers that achieve lesion‐specific precision via ligand modification, biomimetic camouflage, stimuli‐responsive release, and self‐propelling nanomotors; (2) catalytic ...
Yuqi Yang, Jingguo Qu, Tonghuan Xiao, Xinyang Han, Michael Tin‐Cheung Ying   +4 more
wiley   +1 more source

Dual targeting of EZH2 and PD-L1 in Burkitt’s lymphoma enhances immune activation and induces apoptotic pathway

Frontiers in Immunology
IntroductionEnhancer of zeste homolog 2 (EZH2) catalyzes H3K27me3, an epigenetic modification linked to gene silencing, and its overexpression contributes to the progression of hematological malignancies.
Yurim Jeong, Hyewon Jang, Se Been Kim, Minseo Yu, Ra Eun Kim, Wan-Su Choi, Youngwoo Jeon, Jung-Yeon Lim   +7 more
doaj   +1 more source

Current strategies for the design of PROTAC linkers: a critical review

Exploration of Targeted Anti-tumor Therapy, 2020
PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules consisting of two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to bind to a protein of interest, connected by a chemical linker.
Robert I. Troup, Charlene Fallan, Matthias G. J. Baud   +2 more
doaj   +1 more source

VHL-recruiting PROTAC attenuates renal fibrosis and preserves renal function via simultaneous degradation of Smad3 and stabilization of HIF-2α

Cell & Bioscience, 2022
Background Renal fibrosis is the pathological foundation of various chronic kidney diseases progressing to end stage renal failure. However, there are currently no nephroprotective drugs targeted to the fibrotic process in clinical practice.
Jiayi Yang, Yuyi Ruan, Dan Wang, Jinjin Fan, Ning Luo, Huiting Chen, Xiaoyan Li, Wei Chen, Xin Wang   +8 more
doaj   +1 more source

MDM2-BCL-XL PROTACs enable degradation of BCL-XL and stabilization of p53

Acta Materia Medica, 2022
Inhibition or degradation of the anti-apoptotic protein BCL-XL is a viable strategy for cancer treatment. Despite the recent development of PROTACs for degradation of BCL-XL, the choice of E3 ligase has been restricted to VHL and CRBN.
Mengyang Chang, Feng Gao, Jing Chen, Giri Gnawali, Wei Wang   +4 more
doaj   +1 more source

Strawberry Notch 1 Acts as a Transcriptional Regulator Driving Oncogenic Programs in Liver Carcinogenesis

Advanced Science, EarlyView.
This study reports that SBNO1 protein is upregulated in several cancer entities. SBNO1 protein interacts with the basal transcription factor TFIID via TAF4, enabling its recruitment to transcription start sites and the modulation of target gene expression.
Sarah Fritzsche, Raisatun Nisa Sugiyanto, Kira Gür, Alina Krumme, Maxime Le Marois, Angelika Fraas, Aslihan Inal, Mario Huerta, Vanessa Henriques, Eva Eiteneuer, Thomas Albrecht, Alphonse Charbel, Michael T. Dill, Carsten Sticht, Carolina De La Torre, Stefan Pusch, Arianeb Mehrabi, Kai Breuhahn, Junfang Ji, Peter Schirmacher, Benjamin Goeppert, Stephanie Roessler   +21 more
wiley   +1 more source

Identification and removal of a cryptic impurity in pomalidomide-PEG based PROTAC

Beilstein Journal of Organic Chemistry
Chemically induced dimerization is a powerful tool for studying protein function, wherein the IMiD (the “immunomodulatory drug”) class of PROTAC molecules with a PEG linker is frequently used to promote targeted protein degradation. The standard protocol
Bingnan Wang, Yong Lu, Chuo Chen
doaj   +1 more source

Chemical-Mediated Targeted Protein Degradation in Neurodegenerative Diseases

Life, 2021
Neurodegenerative diseases, including Alzheimer’s disease, Huntington’s disease, and Parkinson’s disease, are a class of diseases that lead to dysfunction of cognition and mobility.
Soonsil Hyun, Dongyun Shin
doaj   +1 more source