Results 71 to 80 of about 19,325 (262)

Progress in GABAA receptor agonists for insomnia disorder

Frontiers in Pharmacology
Insomnia is the most common sleep disorder in which an individual has trouble falling or staying asleep. Chronic sleep loss interferes with daily functioning and adversely affects health.
Weiyi Wang, Wanting Fu, Hongyan Zhu, Jing Ma, Jian Zhang, Jia Qi   +5 more
doaj   +1 more source

Structural Optimization of the Diarylurea PSNCBAM-1, an Allosteric Modulator of Cannabinoid Receptor 1

Current Therapeutic Research, 2020
: Background: Structure–activity relationship studies improve the pharmacological and pharmacokinetic properties of a lead compound such as PSNCBAM-1, an allosteric modulator of the cannabinoid receptor 1.
Rachel Dopart, Sri Sujana Immadi, Dai Lu, Debra A. Kendall   +3 more
doaj   +1 more source

Ligand‐Induced Electronic Response Enables Predictive QM/MM Simulations

Advanced Science, EarlyView.
Quantum mechanics/molecular mechanics (QM/MM) simulations are powerful tools for modeling complex molecular systems; however, their predictability has been constrained by the ambiguous definition of the QM region. An electronically informed protocol is introduced that defines QM regions by quantifying guest‐induced orbital shifts and charge ...
Nichika Ozawa, Nahoko Kuroki, Hirotoshi Mori   +2 more
wiley   +1 more source

Identification of a unique Ca2+-binding site in rat acid-sensing ion channel 3

Nature Communications, 2018
Acid-sensing ion channels (ASICs) sense changes in extracellular acidity with Ca2+ as an allosteric modulator and channel blocker. Here authors use electrophysiology and molecular dynamics simulation to identify the residue in ASIC3 which modulates ...
Zhicheng Zuo, Rachel N. Smith, Zhenglan Chen, Amruta S. Agharkar, Heather D. Snell, Renqi Huang, Jin Liu, Eric B. Gonzales   +7 more
doaj   +1 more source

ZBTB21 Is a Dual Suppressor of Pyroptosis and MHC‐I Antigen Presentation That Promotes Tumor Immune Evasion

Advanced Science, EarlyView.
ZBTB21 is a transcription factor that epigenetically suppresses pyroptosis and MHC‐I antigen presentation, enabling tumor immune evasion. Genetic ablation of ZBTB21 activates pyroptotic cell death and enhances antigen presentation, recruiting CD8+ T cells to overcome immune checkpoint blockade resistance.
Lei Zhao, Linlin Sheng, Jianhao Qiu, Junjie Ma, Kai Jin, Binggong Zhao, Tianrun Miao, Jing Chen, Yehong Li, Zhan Zhang, Dongfeng Sun, Yongmeng Li, Hui Tian   +12 more
wiley   +1 more source

The 10–23 DNAzyme in Biosensing and Diagnostics: Applications, Challenges, and Future Directions

Angewandte Chemie, EarlyView.
This review focuses on the 10–23 DNAzyme in diagnostics, spanning unregulated and regulated target‐recognition modes, and their functionalization across colorimetric, fluorescent, electrochemical, electrochemiluminescent, and intracellular biosensing strategies.
Connor Nurmi, Jake Brill, Sanne Roumans, Amal Mathai, John D. Brennan, Yingfu Li   +5 more
wiley   +2 more sources

A Metal‐Free Carbon Monoxide Prodrug Suppresses Metastasis of Pancreatic and Breast Cancer

Advanced Science, EarlyView.
A metal‐free carbon monoxide (CO) prodrug, CO‐116, delivers controlled systemic CO without inhalation. CO suppresses the HRG1–heme axis, reducing intracellular heme availability. Attenuation of this pathway inhibits metastatic progression in pancreatic and triple‐negative breast cancer models.
Tiantian Zhang, Xiang Chen, Xiaoxiao Yang, Muskan Gori, Rohit Kumar Varshnaya, Dongning Liu, Cheryl Zhang, Michelle Yi Qin Chen, Zhengming Chen, George Zhang, Erika Patel, Qiyue Mao, Tan A. Ince, Chalet Tan, Binghe Wang, Yi‐Chieh Nancy Du   +15 more
wiley   +1 more source

Endothelial GPR68 Is Essential for Arteriogenesis and Represents a Therapeutic Target in a Model of Peripheral Artery Disease

Advanced Science, EarlyView.
Endothelial GPR68 is identified as a critical regulator of collateral artery growth in peripheral artery disease. Genetic and pharmacological evidence demonstrates that GPR68 integrates hemodynamic cues to drive monocyte recruitment and inflammatory remodeling, thereby promoting collateral arteriogenesis and tissue perfusion after ischemia ...
Yiyan Song, Senyi Peng, Zhilei Huang, Miao Yu, Mingyue Wu, Yuexin Zhu, Zeyi Zhou, Yongshan Liu, Yalin Zhang, Yu Huang, Zhongxing Wang, Fu‐Li Xiang, Jie Xu   +12 more
wiley   +1 more source

Distinct potency of compounds targeting the T1R3 subunit in modulating the response of human sweet and umami taste receptors

Scientific Reports
The heterodimeric G-protein-coupled receptors T1R2/T1R3 and T1R1/T1R3 have been identified as sweet and umami taste receptors, respectively, and both of these receptors share the T1R3 subunit.
Maiko Kawasaki, Yuta Kidera, Ryusei Goda, Chiaki Taketani, Misato Ide, Wataru Fujii, Tomoya Nakagita, Takumi Misaka   +7 more
doaj   +1 more source

Analysis of equilibrium binding of an orthosteric tracer and two allosteric modulators.

PLoS ONE, 2019
Allosteric ligands bind to receptors at sites that are distinct from those endogenous agonists and orthosteric pharmacological agents interact with. Both an allosteric and orthosteric ligand bind simultaneously to the receptor to form a ternary complex ...
Jan Jakubík, Alena Randáková, Esam E El-Fakahany, Vladimír Doležal   +3 more
doaj   +1 more source