Results 71 to 80 of about 11,341 (256)

PROTACs targeting epigenetic proteins

Acta Materia Medica, 2023
The field of epigenetics pertains to alterations in gene function that are inherited without changes in the DNA sequence, including histone modifications, post-translational modifications of amino acids, and covalent modifications of DNA bases. These alteration pathways modulate the transformation of genotypes into specific phenotypes.
Chao Zhang, Yuna He, Xiuyun Sun, Wenyi Wei, Yanlong Liu, Yu Rao   +5 more
openaire   +3 more sources

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

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

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

Protective Effects of Non-Anticoagulant Activated Protein C Variant (D36A/L38D/A39V) in a Murine Model of Ischaemic Stroke [PDF]

, 2015
Ischaemic stroke is caused by occlusive thrombi in the cerebral vasculature. Although tissue-plasminogen activator (tPA) can be administered as thrombolytic therapy, it has major limitations, which include disruption of the blood-brain barrier and an ...
Andreou, AP, Crawley, JTB, Efthymiou, M, Lane, DA, Ma, D, Noormohamed, FH, Watts, HR, Yu, Y   +7 more
core   +2 more sources

Natural Products Inspired Scaffold Diversification Leads to Unnatural Molecular Warhead and Covalent Strategy to Modulating Protein Function through Electrophilic Bromine Transfer

Advanced Science, EarlyView.
We report a new thiolate‐reactive α,α‐gem‐dibromo lactam warhead that activates transcription factor Nrf2 and demonstrates anti‐inflammatory activities, which have implications in cancer, neurodegeneration, and cardiovascular diseases. RNA‐seq illuminated detailed transcriptional profiles, and chemical reactions with cysteine‐containing compounds ...
Beau R. Brummel, Sofia Kokkaliari, Qiwen Gao, Jinjing Chen, Larissa Costa de Almeida, Srinivasarao Tenneti, Derek A. Leas, Eli Levit, Lewis S. Alexander, Khalil A. Abboud, Pingrong Wei, Michael D. Cameron, James R. Rocca, Ranjala Ratnayake, Donna D. Zhang, Hendrik Luesch, Robert W. Huigens III   +16 more
wiley   +1 more source

Identification of probe-quality degraders for Poly(ADP-ribose) polymerase-1 (PARP-1)

Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Poly(ADP-ribose) polymerase-1 (PARP-1), a critical DNA repair enzyme in the base excision repair pathway, has been pursued as an attractive cancer therapeutic target.
Zhimin Zhang, Xinyue Chang, Chixiao Zhang, Shenxin Zeng, Meihao Liang, Zhen Ma, Zunyuan Wang, Wenhai Huang, Zhengrong Shen   +8 more
doaj   +1 more source

Development of Liposome Systems for Enhancing the PK Properties of Bivalent PROTACs

Pharmaceutics, 2023
Proteolysis-Targeting Chimeras (PROTACs) are a promising new technology in drug development. They have rapidly evolved in recent years, with several of them in clinical trials.
Ponien Kou, Elizabeth S. Levy, An D. Nguyen, Donglu Zhang, Shu Chen, Yusi Cui, Xing Zhang, Fabio Broccatelli, Jennifer Pizzano, Jennifer Cantley, Elizabeth Bortolon, Emma Rousseau, Michael Berlin, Peter Dragovich, Vijay Sethuraman   +14 more
doaj   +1 more source

Trombingenerációs vizsgálatok és klinikai alkalmazásuk [PDF]

, 2014
Thrombin is a key enzyme of the coagulation system, having both pro- And anticoagulant functions. Thus, the generation of thrombin is one of the most important steps in coagulation.
Kern A, Várnai, Katalin, Vásárhelyi, Barna   +2 more
core   +1 more source

PROTACs in the Management of Prostate Cancer

Molecules, 2023
Cancer treatments with targeted therapy have gained immense interest due to their low levels of toxicity and high selectivity. Proteolysis-Targeting Chimeras (PROTACs) have drawn special attention in the development of cancer therapeutics owing to their unique mechanism of action, their ability to target undruggable proteins, and their focused target ...
Poornachandra Yedla, Ahmed O. Babalghith, Vindhya Vasini Andra, Riyaz Syed   +3 more
openaire   +3 more sources