Results 71 to 80 of about 128,101 (191)

A Novel Phenanthridionone Based Scaffold As a Potential Inhibitor of the BRD2 Bromodomain: Crystal Structure of the Complex.

PLoS ONE, 2016
Bromodomain containing proteins recognize the level of histone acetylation and regulate epigenetically controlled processes like gene transcription and chromatin modification.
Shailesh Tripathi, Shruti Mathur, Prashant Deshmukh, Ramu Manjula, Balasundaram Padmanabhan   +4 more
doaj   +1 more source

Multiple Roles of Brd4 in the Infectious Cycle of Human Papillomaviruses

Frontiers in Molecular Biosciences, 2021
Human Papillomaviruses (HPV) reproduce in stratified epithelia by establishing a reservoir of low- level infection in the dividing basal cells and restricting the production of viral particles to terminally differentiated cells.
Alison A. McBride, Alix Warburton, Simran Khurana   +2 more
doaj   +1 more source

Intravenous Lipopolysaccharide Challenge in Healthy Participants Reveals Pharmacodynamic Markers in Blood and Bone Marrow for Early‐Phase Oncology Drug Development

Clinical Pharmacology &Therapeutics, EarlyView.
Demonstrating pharmacological effects in early‐phase oncology clinical trials remains challenging, largely due to the lack of robust pharmacodynamic markers. Lipopolysaccharide (LPS) is used as an immune challenge agent in healthy participants to study drugs for autoimmune conditions.
Igor Radanović, Ingrid Tomljanović, Wieke H. Grievink, Diana R. Pereira, Michelle Osse, Peter van Balen, Maria J. Juachon, Marieke L. de Kam, Lisa Pagan, Manon A.A. Jansen, Matthijs Moerland, Jacobus J. Bosch   +11 more
wiley   +1 more source

GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family

ACS Medicinal Chemistry Letters, 2020
Pan-BET inhibitors have shown profound efficacy in a number of in vivo preclinical models and have entered the clinic in oncology trials where adverse events have been reported. These inhibitors interact equipotently with the eight bromodomains of the BET family of proteins.
Alex Preston, Stephen J. Atkinson, Paul Bamborough, Chun-wa Chung, Laurie J. Gordon, Paola Grandi, James R. J. Gray, Lee A. Harrison, Antonia J. Lewis, David Lugo, Cassie Messenger, Anne-Marie Michon, Darren J. Mitchell, Rab K. Prinjha, Inmaculada Rioja, Jon Seal, Simon Taylor, Pierre Thesmar, Ian D. Wall, Robert J. Watson, James M. Woolven, Emmanuel H. Demont   +21 more
openaire   +3 more sources

BET Bromodomain Inhibition Synergizes with PARP Inhibitor in Epithelial Ovarian Cancer

Cell Reports, 2017
Summary: PARP inhibition is known to be an effective clinical strategy in BRCA mutant cancers, but PARP inhibition has not been applied to BRCA-proficient tumors.
Sergey Karakashev, Hengrui Zhu, Yuhki Yokoyama, Bo Zhao, Nail Fatkhutdinov, Andrew V. Kossenkov, Andrew J. Wilson, Fiona Simpkins, David Speicher, Dineo Khabele, Benjamin G. Bitler, Rugang Zhang   +11 more
doaj   +1 more source

Systemic aging fuels heart failure: Molecular mechanisms and therapeutic avenues

ESC Heart Failure, Volume 12, Issue 2, Page 1059-1080, April 2025.
Abstract Systemic aging influences various physiological processes and contributes to structural and functional decline in cardiac tissue. These alterations include an increased incidence of left ventricular hypertrophy, a decline in left ventricular diastolic function, left atrial dilation, atrial fibrillation, myocardial fibrosis and cardiac ...
Zhuyubing Fang, Umar Raza, Jia Song, Junyan Lu, Shun Yao, Xiaohong Liu, Wei Zhang, Shujuan Li   +7 more
wiley   +1 more source

Artificial intelligence empowers targeted protein degradation: Core technological innovations, multi‐scenario applications, and translational prospects

Smart Molecules, EarlyView.
AI is transforming TPD by improving the design, prediction, and optimization of degraders such as PROTACs, molecular glues, and LYTACs. This review summarizes key AI‐driven advances, highlights applications across drug discovery stages, and discusses remaining challenges and future directions for accelerating the development of therapies against ...
Shuanglin Qin, Rui Peng, Guangshuai Zhang, Si Yan, Jin Xiao, Zishu Liu, Ziyu Tan, Qingqing Xie, Shangjie Li, Wei Luo, Xiaohe Xiao   +10 more
wiley   +1 more source

Bromodomain and Extraterminal Proteins as Novel Epigenetic Targets for Renal Diseases

Frontiers in Pharmacology, 2019
Epigenetic mechanisms, especially DNA methylation and histone modifications, are dynamic processes that regulate the gene expression transcriptional program in normal and diseased states. The bromodomain and extraterminal (BET) protein family (BRD2, BRD3,
Jose Luis Morgado-Pascual, Jose Luis Morgado-Pascual, Sandra Rayego-Mateos, Sandra Rayego-Mateos, Lucia Tejedor, Lucia Tejedor, Beatriz Suarez-Alvarez, Beatriz Suarez-Alvarez, Marta Ruiz-Ortega, Marta Ruiz-Ortega   +9 more
doaj   +1 more source

BRD9 inhibition as potential treatment option for testicular germ cell tumors

Andrology, EarlyView.
Abstract Background Testicular germ cell tumors (TGCT) are the predominant tumor in younger males. Usually, 5‐year survival rates are quite high, but 15–20% of patients with metastatic non‐seminomas are resistant to standard cisplatin‐based therapy.
Aylin Hansen, Christine Sanders, Florian Fronhoffs, Kai Funke, Glen Kristiansen, Hubert Schorle   +5 more
wiley   +1 more source

Scalable syntheses of the BET bromodomain inhibitor JQ1

Tetrahedron Letters, 2015
We have developed methods involving the use of alternate, safer reagents for the scalable syntheses of the potent BET bromodomain inhibitor JQ1. A one-pot three step method, involving the conversion of a benzodiazepine to a thioamde using Lawesson's reagent, followed by amidrazone formation and installation of the triazole moiety furnished JQ1.
Syeda, Shameem Sultana, Jakkaraj, Sudhakar, Georg, Gunda I.   +2 more
openaire   +2 more sources