Results 61 to 70 of about 1,089 (172)

Towards the convergent therapeutic potential of G protein‐coupled receptors in autism spectrum disorders

British Journal of Pharmacology, Volume 182, Issue 14, Page 3044-3067, July 2025.
Abstract Autism spectrum disorders (ASDs) are diagnosed in 1/100 children worldwide, based on two core symptoms: deficits in social interaction and communication, and stereotyped behaviours. G protein‐coupled receptors (GPCRs) are the largest family of cell‐surface receptors that transduce extracellular signals to convergent intracellular signalling ...
Anil Annamneedi, Caroline Gora, Ana Dudas, Xavier Leray, Véronique Bozon, Pascale Crépieux, Lucie P. Pellissier   +6 more
wiley   +1 more source

The translational value of ligand‐receptor binding kinetics in drug discovery

British Journal of Pharmacology, Volume 181, Issue 21, Page 4117-4129, November 2024.
Abstract The translation of in vitro potency of a candidate drug, as determined by traditional pharmacology metrics (such as EC50/IC50 and KD/Ki values), to in vivo efficacy and safety is challenging. Residence time, which represents the duration of drug‐target interaction, can be part of a more comprehensive understanding of the dynamic nature of drug‐
Hongli Liu, Haoran Zhang, Adriaan P. IJzerman, Dong Guo   +3 more
wiley   +1 more source

In Vitro approach for identification of a leading cytochrome P450 isoenzyme responsible for biotransformation of novel arylpiperazine drug candidates and their inhibition potency towards CYP3A4. [PDF]

, 2020
Presented article is a follow-up study of previous work, published in PLoS ONE in 2015 regarding metabolic stability of arylpiperazine derivatives, a very promising group of novel antidepressants.
Król, Marek, Bączek, Tomasz, Ulenberg, Szymon, Belka, Mariusz, Georgiev, Paweł, Herold, Franciszek   +5 more
core   +1 more source

Solid-Phase Synthesis of Arylpiperazine Derivatives and Implementation of the Distributed Drug Discovery (D3) Project in the Search for CNS Agents

Molecules, 2011
We have successfully implemented the concept of Distributed Drug Discovery (D3) in the search for CNS agents. Herein, we demonstrate, for the first time, student engagement from different sites around the globe in the development of new biologically ...
William L. Scott, Ziniu Zhou, Martin J. O’Donnell, Grzegorz Satała, Andrzej J. Bojarski, Jean Martinez, Gaël Nomezine, Maciej Pawłowski, Gilles Subra, Katarzyna Grychowska, Joanna Król, Paweł Zajdel   +11 more
doaj   +1 more source

TAS3681, an androgen receptor antagonist, prevents drug resistance driven by aberrant androgen receptor signaling in prostate cancer

Molecular Oncology, Volume 18, Issue 8, Page 1980-2000, August 2024.
The androgen receptor (AR) antagonist TAS3681 is effective against AR mutations, which leads to agonistic activity of AR signal inhibitors, and had an antitumor effect in an AR‐splice variant 7 (AR‐V7)‐positive enzalutamide‐resistant xenograft model. TAS3681 suppresses aberrant AR activation, including AR overexpression and expression of constitutively
Shohei Yoshida, Daisuke Kajiwara, Masanao Seki, Manabu Tayama, Yuki Tanaka, Hiroya Mizutani, Ryoto Fujita, Keisuke Yamamura, Shigeo Okajima, Masanori Asai, Kazuhisa Minamiguchi   +10 more
wiley   +1 more source

Mechanistic study of novel arylpiperazine derivative NAF19 in prostate cancer treatment based on network pharmacology approach

Romanian Journal of Laboratory Medicine
Our preliminary studies identified the arylpiperazine derivative NAF19 as a promising therapeutic agent against prostate cancer, though its precise mechanisms remained unclear.
Jiang Hua, Xu Mingzhen, Jiang Songsong, Huang Weiqiang, Chen Hong   +4 more
doaj   +1 more source

Short Synthesis of Enantiopure trans-3-Arylpiperazine-2-carboxylic Acid Derivatives via Diaza-Cope Rearrangement

, 2016
An efficient synthetic method was developed for the construction of enantiomerically pure trans-3-arylpiperazine-2-carboxylic acid derivatives using diaza-Cope rearrangement (DCR) as a key step starting from (R,R)/(S,S)-1,2-bis(2-hydroxyphenyl)-1,2 ...
Soon Ho Kwon (2062855), Jik Chin (2062858), Sang Min Lee (507437), B. Moon Kim (1608127), Sang Moon Byun (2062852)   +4 more
core   +1 more source

Synthesis and biological evaluation of N-arylpiperazine derivatives of 4,4-dimethylisoquinoline-1,3(2H,4H)-dione as potential antiplatelet agents

Journal of Enzyme Inhibition and Medicinal Chemistry, 2018
Despite the substantial clinical success of aspirin and clopidogrel in secondary prevention of ischemic stroke, up to 40% of patients remain resistant to the available antiplatelet treatment.
Monika Marcinkowska, Magdalena Kotańska, Agnieszka Zagórska, Joanna Śniecikowska, Monika Kubacka, Agata Siwek, Adam Bucki, Maciej Pawłowski, Marek Bednarski, Jacek Sapa, Małgorzata Starek, Monika Dąbrowska, Marcin Kołaczkowski   +12 more
doaj   +1 more source

In silico studies of piperazine derivatives as potent anti-proliferative agents against PC-3 prostate cancer cell lines

Heliyon, 2020
Quantitative Structure Activity Relationship studies were carried out on arylpiperazine derivatives to investigate their anti-proliferate activity against prostate PC-3 cancer cell lines.
Fabian A. Ikwu, Gideon A. Shallangwa, Paul A. Mamza, Adamu Uzairu   +3 more
doaj   +1 more source

Exploration of N-arylpiperazine Binding Sites of D2 Dopaminergic Receptor

, 2015
The crystal structures of the D3 dopamine receptor and several other G-protein coupled receptors (GPCRs) were published in recent times. Those 3D structures are used by us and other scientists as a template for the homology modeling and ligand docking ...
Kostić Rajačić, Slađana, Šukalović, Vladimir, Šoškić, Vukić   +2 more
core   +1 more source