Results 151 to 160 of about 1,044,728 (382)

Berberine–cinnamic acid co‐crystal effect in ameliorating hyperlipidemia might be regulated through the PI3K/AKT/mTOR/SREBP‐1 signaling pathway

FEBS Open Bio, EarlyView.
Berberine–cinnamic acid co‐crystal (BBR‐CA) inhibits the phosphorylation of the phosphatidylinositol 3‐kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR) pathway, suppressing the transfer of pre‐sterol regulatory element‐binding proteins‐1 (SREBP‐1) from the endoplasmic reticulum to the nucleus. This results in a decrease in the expression level of
Wenheng Gao, Yunlong Li, Lihua Chen, Wenshuo Yang, Yong He, Ye Yang, Dengke Yin, Song Tan   +7 more
wiley   +1 more source

Short‐term actions of epigalocatechin‐3‐gallate in the liver: a mechanistic insight into hypoglycemic and potential toxic effects

FEBS Open Bio, EarlyView.
Epigallocatechin‐3‐gallate (EGCG) acutely inhibited gluconeogenesis and enhanced glycolysis, glycogenolysis, and fatty acid oxidation in perfused rat livers. Mechanistic assays revealed mitochondrial uncoupling, inhibition of pyruvate carboxylation and glucose‐6‐phosphatase, shift of NADH/NAD+ ratios toward oxidation, and loss of membrane integrity ...
Carla Indianara Bonetti, Bruna Lopes Correia, Francielle Cristina Nakamura Manicardi, Nairana Mithieli de Queiroz Eskuarek Melo, Vanesa de Oliveira Pateis, Jurandir Fernando Comar, Anacharis Babeto de Sá‐Nakanishi, Adelar Bracht, Lívia Bracht   +8 more
wiley   +1 more source

Preclinical evaluation of the immunomodulatory lymphocyte trafficking drug FTY720 for HIV prevention in the female genital mucosa of macaques [PDF]

, 2014
Monica Morris, Rachael D. Aubert, Katherine Butler, Tara Henning, James Mitchell, Leecresia Jenkins, David A. Garber, Janet M. McNicholl, Ellen N. Kersh   +8 more
openalex   +1 more source

Indoleamine 2,3‐dioxygenase 1 inhibition reverses cancer‐associated fibroblast‐mediated immunosuppression in high‐grade serous ovarian cancer

FEBS Open Bio, EarlyView.
CAF‐mediated immunosuppression in ovarian cancer is driven by IDO1, reducing T‐cell function. Inhibiting IDO1 restores T‐cell proliferation and cytotoxicity, increases cancer cell apoptosis, and may help overcome CAF‐induced immune suppression in high‐grade serous ovarian cancer. Targeting IDO1 may improve antitumor immunity.
Hyewon Lee, Jung Yoon Ho, In Sun Hwang, Youn Jin Choi   +3 more
wiley   +1 more source

PM288. Preclinical Evaluation of Neutral Cannabinoid CB1 Receptor Antagonists and Cannabinoid CB1 Receptor Negative Allosteric Modulators for Treating Drug Addiction [PDF]

, 2016
Eliot L. Gardner, Guo‐Hua Bi, Ganesh A. Thakur, Alexandros Makriyannis, Herbert H. Seltzman, Xianghu He, Zheng‐Xiong Xi   +6 more
openalex   +1 more source

Celecoxib in breast cancer prevention and therapy. [PDF]

, 2018
Breast cancer has a high incidence worldwide. The results of substantial studis reveal that inflammation plays an important role in the initiation, development, and aggressiveness of many malignancies. The use of celecoxib, a novel NSAID, is repetitively
Cao, Wei, Hao, Qiongyu, Li, Jieqing, Vadgama, Jaydutt V, Wu, Yong   +4 more
core  

Thrombolytic proteins profiling: High‐throughput activity, selectivity, and resistance assays

FEBS Open Bio, EarlyView.
We present optimized biochemical protocols for evaluating thrombolytic proteins, enabling rapid and robust screening of enzymatic activity, inhibition resistance, and fibrin affinity, stimulation, and selectivity. The outcome translates to key clinical indicators such as biological half‐life and bleeding risk. These assays streamline the development of
Martin Toul, Alan Strunga, Jiri Damborsky, Zbynek Prokop   +3 more
wiley   +1 more source

In silico predictions of drug-induced changes in human cardiac contractility align with experimental recordings

Frontiers in Pharmacology
Drug-induced changes in cardiac contractility (inotropy) can lead to cardiotoxicity, a major cause of discontinuation in drug development. Preclinical approaches to assess cardiac inotropy are imperfect, with in vitro assays limited to stem cell-derived ...
Cristian Trovato, Cristian Trovato, Stefano Longobardi, Elisa Passini, Kylie A. Beattie, Maxx Holmes, Khuram W. Chaudhary, Eric I. Rossman, Blanca Rodriguez   +8 more
doaj   +1 more source

ATG4B is required for mTORC1‐mediated anabolic activity and is associated with clinical outcomes in non‐small cell lung cancer

FEBS Open Bio, EarlyView.
The relationship between anabolic and catabolic processes governing lung cancer cell growth is nuanced. We show that ATG4B, an autophagy regulator, is elevated in lung cancer and that high ATG4B is associated with worse patient outcomes. Targeting ATG4B in cells reduces growth, protein synthesis, and mTORC1 activity, demonstrating a new relationship ...
Patrick J. Ryan, Bethany C. Guerra, Selina Uranga, Jessica M. Cardin, Steven E. Riechman, Mariana Janini Gomes, James D. Fluckey   +6 more
wiley   +1 more source

Supplementary Tables S1-4 from Design and Preclinical Evaluation of a Novel B7-H4–Directed Antibody–Drug Conjugate, AZD8205, Alone and in Combination with the PARP1-Selective Inhibitor AZD5305

, 2023
Krista Kinneer, Philipp Wortmann, Zachary A. Cooper, Niall J. Dickinson, Luke A. Masterson, Thais Cailleau, Ian Hutchinson, Balakumar Vijayakrishnan, Mary McFarlane, Kathryn Ball, Michael Davies, Arthur Lewis, Yue Huang, Anton I. Rosenbaum, Jiaqi Yuan, Jon Chesebrough, Judith Anderton, Noel R. Monks, Steven Novick, Jixin Wang, Nazzareno Dimasi, R. James Christie, Darrin Sabol, Frances Anne Tosto, Yann Wallez, Elisabetta Leo, Mark R. Albertella, Anna D. Staniszewska, David A. Tice, Philip W. Howard, Nadia Luheshi, Puja Sapra   +31 more
openalex   +1 more source