Results 41 to 50 of about 310 (140)

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

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

Poster Sessions

HemaSphere, Volume 10, Issue S1, June 2026.
wiley   +1 more source

Design Strategies, Chemistry and Therapeutic Insights of Multi-target Directed Ligands as Antidepressant Agents. [PDF]

Curr Neuropharmacol, 2022
Singh K, Bhatia R, Kumar B, Singh G, Monga V.   +4 more
europepmc   +1 more source

Update on the Discovery of Efflux Pump Inhibitors against Critical Priority Gram-Negative Bacteria. [PDF]

Antibiotics (Basel), 2023
Compagne N, Vieira Da Cruz A, Müller RT, Hartkoorn RC, Flipo M, Pos KM.   +5 more
europepmc   +1 more source

Probing antibacterial drugs for Fusobacterium nucleatum subsp. nucleatum ATCC 25586 targeting UDP-N-acetylglucosamine 1-carboxyltransferase. [PDF]

J Adv Pharm Technol Res, 2023
Saputri D, Mubarak Z, Mudatsir M, Setyawati I, Setiawan AG, Abrar M.   +5 more
europepmc   +1 more source

Synthesis, bioactivity, and molecular docking of novel arylpiperazine derivatives as potential AR antagonists. [PDF]

Front Chem, 2022
Qi Y, Chen H, Chen S, Shen J, Li J.
europepmc   +1 more source

Design, synthesis and biological evaluation of 1-Aryl-5-(4-arylpiperazine-1-carbonyl)-1H-tetrazols as novel microtubule destabilizers. [PDF]

J Enzyme Inhib Med Chem, 2021
Wang C, Li Y, Liu Z, Wang Z, Liu Z, Man S, Zhang Y, Bao K, Wu Y, Guan Q, Zuo D, Zhang W.   +11 more
europepmc   +1 more source

Influence of cellular lipid content on influenza A virus replication. [PDF]

Arch Virol, 2020
Limsuwat N, Boonarkart C, Phakaratsakul S, Suptawiwat O, Auewarakul P.   +4 more
europepmc   +1 more source

σ₂ Receptor and Its Role in Cancer with Focus on a MultiTarget Directed Ligand (MTDL) Approach. [PDF]

Molecules, 2021
Abatematteo FS, Niso M, Lacivita E, Abate C.   +3 more
europepmc   +1 more source