Results 11 to 20 of about 363,849 (261)

Modulation of type 1 cannabinoid receptor activity by cannabinoid by-products from Cannabis sativa and non-cannabis phytomolecules

Frontiers in Pharmacology, 2022
Cannabis sativa contains more than 120 cannabinoids and 400 terpene compounds (i.e., phytomolecules) present in varying amounts. Cannabis is increasingly available for legal medicinal and non-medicinal use globally, and with increased access comes the ...
Ayat Zagzoog, Ashley Cabecinha, Hanan Abramovici, Robert B. Laprairie, Robert B. Laprairie   +4 more
doaj   +1 more source

Chemotranscriptomic analysis of 7-hydroxymatairesinol-related effects on MCF7 human breast tumor cells

Акушерство, гинекология и репродукция, 2023
Introduction. Establishing the effects of anticancer drugs on the transcriptome is an important procedure in postgenomic pharmacology necessary to comprehensively assess the desired and undesirable effects of candidate drugs.
I. Yu. Torshin, A. N. Rubashkina, O. A. Gromova   +2 more
doaj   +1 more source

Discovery of Novel Delta Opioid Receptor (DOR) Inverse Agonist and Irreversible (Non-Competitive) Antagonists

Molecules, 2021
The delta opioid receptor (DOR) is a crucial receptor system that regulates pain, mood, anxiety, and similar mental states. DOR agonists, such as SNC80, and DOR-neutral antagonists, such as naltrindole, were developed to investigate the DOR in vivo and ...
Parthasaradhireddy Tanguturi, Vibha Pathak, Sixue Zhang, Omar Moukha-Chafiq, Corinne E. Augelli-Szafran, John M. Streicher   +5 more
doaj   +1 more source

29th Annual GP2A Medicinal Chemistry Conference

Pharmaceuticals, 2021
The 29th Annual GP2A (Group for the Promotion of Pharmaceutical chemistry in Academia) Conference was a virtual event this year due to the COVID-19 pandemic and spanned three days from Wednesday 25 to Friday 27 August 2021.
Jean-Jacques Helesbeux, Laura Carro, Florence O. McCarthy, Vânia M. Moreira, Francesca Giuntini, Niamh O’Boyle, Susan E. Matthews, Gülşah Bayraktar, Samuel Bertrand, Christophe Rochais, Pascal Marchand   +10 more
doaj   +1 more source

A Brain-Penetrating Hsp90 Inhibitor NXD30001 Inhibits Glioblastoma as a Monotherapy or in Combination With Radiation

Frontiers in Pharmacology, 2020
Glioblastoma multiforme (GBM) is a highly heterogeneous disease, which is initiated and sustained by various molecular alterations in an array of signal transduction pathways.
Hao Chen, Hao Chen, Yuanying Gong, Yufang Ma, Reid C. Thompson, Jialiang Wang, Zhixiang Cheng, Zhixiang Cheng, Lixia Xue   +8 more
doaj   +1 more source

The role of pharmacology in anticancer drug development

ADMET and DMPK, 2018
Drug development consists of many sequential and parallel steps; failure in one of the steps can lead to discontinuation of the process. The process is time-consuming and very expensive, especially the clinical phase.
Godefridus J. Peters, Anne-Sophie Govaerts, Hans R. Hendriks, for EORTC Pharmacology and Molecular Mechanism Group   +3 more
doaj   +1 more source

Biophysical modeling indicates a high affinity of ethyl esters of omega-3 polyunsaturated fatty acids to the enzymes of the pro-inflammatory arachidonic acid cascade

Фармакоэкономика, 2022
Background. Omega-3 polyunsaturated fatty acids (ω-3 PUFAs) are widely used in modern cardiology. The anti-inflammatory effect of eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) is realized, in particular, by modulating the activity of the ...
I. Yu. Torshin, O. A. Gromova
doaj   +1 more source

Indomethacin Enhances Type 1 Cannabinoid Receptor Signaling

Frontiers in Molecular Neuroscience, 2019
In addition to its known actions as a non-selective cyclooxygenase (COX) 1 and 2 inhibitor, we hypothesized that indomethacin can act as an allosteric modulator of the type 1 cannabinoid receptor (CB1R) because of its shared structural features with the ...
Robert B. Laprairie, Robert B. Laprairie, Kawthar A. Mohamed, Ayat Zagzoog, Melanie E. M. Kelly, Melanie E. M. Kelly, Lesley A. Stevenson, Roger Pertwee, Eileen M. Denovan-Wright, Ganesh A. Thakur   +9 more
doaj   +1 more source

Pharmacological hallmarks of allostery at the M4 muscarinic receptor elucidated through structure and dynamics

eLife, 2023
Allosteric modulation of G protein-coupled receptors (GPCRs) is a major paradigm in drug discovery. Despite decades of research, a molecular-level understanding of the general principles that govern the myriad pharmacological effects exerted by GPCR ...
Ziva Vuckovic, Jinan Wang, Vi Pham, Jesse I Mobbs, Matthew J Belousoff, Apurba Bhattarai, Wessel AC Burger, Geoff Thompson, Mahmuda Yeasmin, Vindhya Nawaratne, Katie Leach, Emma T van der Westhuizen, Elham Khajehali, Yi-Lynn Liang, Alisa Glukhova, Denise Wootten, Craig W Lindsley, Andrew Tobin, Patrick Sexton, Radostin Danev, Celine Valant, Yinglong Miao, Arthur Christopoulos, David M Thal   +23 more
doaj   +1 more source

The novel thiosemicarbazone, di-2-pyridylketone 4-cyclohexyl-4-methyl-3-thiosemicarbazone (DpC), inhibits neuroblastoma growth in vitro and in vivo via multiple mechanisms

Journal of Hematology & Oncology, 2016
Background Neuroblastoma is a relatively common and highly belligerent childhood tumor with poor prognosis by current therapeutic approaches. A novel anti-cancer agent of the di-2-pyridylketone thiosemicarbazone series, namely di-2-pyridylketone 4,4 ...
Zhu-Ling Guo, Des R. Richardson, Danuta S. Kalinowski, Zaklina Kovacevic, Kian Cheng Tan-Un, Godfrey Chi-Fung Chan   +5 more
doaj   +1 more source