Results 101 to 110 of about 22,949 (304)

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

Effects of Ivermectin as an Allosteric Modulator of nAChRs on Dopamine Release

, 2022
Dopamine (DA) terminals are regulated by acetylcholine activity on nicotinic receptors (nAChRs). Nicotine reduces DA release from low frequency stimulation, but enhances release at higher frequencies.
Robinson, J. Kayden, Bishop, Samantha, Foote, Sarah E., Graul, Benjamin E., Steimle, Emma, Hafen, Caylor, Yorgason, Jordan, Wadsworth, Hillary, Barlow, Joshua   +8 more
core  

Autoimmune Encephalitis in Acute Care—Pathology, Diagnosis, and Management

Advanced Science, EarlyView.
ABSTRACT Autoimmune encephalitis (AE) is characterized by immune‐mediated inflammation of the brain parenchyma, presenting with various neurological syndromes, including but not limited to seizures, altered consciousness, neuropsychiatric symptoms, and movement disorders.
Suneesh Thilak, David Okoh, William Scotton, Shanika Samarasekera, Vikram Patil, Suresh Renukappa, Andrew Macduff, Subashini Suresh, Rajeev Krishnadas, Tonny Veenith   +9 more
wiley   +1 more source

Molecular Glue cc‐885 Inhibits VHL‐Deficient Clear Cell Renal Cell Carcinoma via ETS1 Degradation

Advanced Science, EarlyView.
VHL‐deficient kidney cancer lacks effective treatments. This study reveals that the molecular glue degrader cc‐885 hijacks the cellular recycling system to selectively destroy the oncogenic protein ETS1, effectively killing VHL‐mutant tumors. Combining CC‐885 with the approved drug belzutifan achieves powerful synergy, offering a promising new ...
Taowei Yang, Qihao Li, Kun Ye, Kezhi Liu, Mi Zhou, Minyu Chen, Lican Liao, Kangbo Huang, Zhu Wang, Qiong Deng, Jieyan Wang, Meiyu Jin, Xu Chen, Hui Liang, Jiaxing Zhang, Junhang Luo   +15 more
wiley   +1 more source

Dose‐Dependent Reprogramming of Chromatin Accessibility by SOX4 Drives the Transcriptional Response to Iron Overload

Advanced Science, EarlyView.
This study demonstrates that iron overload triggers widespread chromatin compaction and transcriptional repression in human granulosa cells, recapitulating features of endometriosis. The epigenetic reprogramming is orchestrated by a TFEB‐SOX4‐SWI/SNF axis, with SOX4 acting as a central, dosage‐sensitive regulator.
Feifei Li, Yaoqiu Wu, Guangyu Yang, Jingyi Lai, Xiaoyue Sun, Liyan Wang, Xiaoli Li, Jing Zhang, Qingxue Zhang, Hui Chen, Haiyan Lin, Bingxiang Xu, Junfeng Zhang, Hailong Wang, Anming Meng, Chunwei Cao   +15 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

Insights into the Allosteric Regulation of Human Hsp90 Revealed by NMR Spectroscopy

Biomolecules
Human heat shock protein 90 (Hsp90) is one of the most important chaperones that play a role in the late stages of protein folding. Errors in the process of the chaperone cycle can lead to diseases such as cancer and neurodegenerative diseases. Therefore,
Tjaša Goričan, Simona Golič Grdadolnik   +1 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

Development of novel, cns penetrant mglu3 selective negative allosteric modulator probes derived from a closely related mglu5 positive allosteric modulator

, 2012
Metabotropic glutamate (mGlu) receptors are examples of family C G-protein-coupled receptors that possess vast roles in the pathophysiology of central nervous system (CNS) disorders.
Bruner, Joshua Andrew
core  

GalR2-positive allosteric modulator exhibits anticonvulsant effects in animal models

, 2010
Galanin receptors type 1 (GalR1) and/or type 2 (GalR2) represent unique pharmacological targets for treatment of seizures and epilepsy. Previous studies have shown that the endogenous peptide ligand galanin exerts powerful anticonvulsant ...
Roger Baldwin, Tianyu Liu, Fengcheng Xia, Xiaoying Lu, Edward Roberts, Manuel Sanchez-Alavez, Claude G. Wasterlain, James Chang, Stephanie Wu, Tamas Bartfai   +9 more
core   +1 more source