Results 181 to 190 of about 159,662 (351)

Ligand bias and inverse agonism on 5‐HT2A receptor‐mediated modulation of G protein activity in post‐mortem human brain

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Whereas biased agonism on the 5‐HT2A receptor has been ascribed to hallucinogenic properties of psychedelics, no information about biased inverse agonism on this receptor is available. In schizophrenia, increased 5‐HT2A receptor constitutive activity has been suggested, highlighting the therapeutic relevance of inverse ...
Itziar Muneta‐Arrate, Patricia Miranda‐Azpiazu, Igor Horrillo, Rebeca Diez‐Alarcia, J. Javier Meana   +4 more
wiley   +1 more source

Backbone-free duplex-stacked monomer nucleic acids exhibiting Watson-Crick selectivity. [PDF]

, 2018
We demonstrate that nucleic acid (NA) mononucleotide triphosphates (dNTPs and rNTPs), at sufficiently high concentration and low temperature in aqueous solution, can exhibit a phase transition in which chromonic columnar liquid crystal ordering ...
Bellini, Tommaso, Clark, Noel A, Fraccia, Tommaso P, Hayden, Emily, Smith, Gregory P, Todisco, Marco, Zanchetta, Giuliano, Zhu, Chenhui   +7 more
core   +1 more source

ERNEST COST action overview on the (patho)physiology of GPCRs and orphan GPCRs in the nervous system

British Journal of Pharmacology, EarlyView.
G protein‐coupled receptors (GPCRs) are a large family of cell surface receptors that play a critical role in nervous system function by transmitting signals between cells and their environment. They are involved in many, if not all, nervous system processes, and their dysfunction has been linked to various neurological disorders representing important
Necla Birgül Iyison, Clauda Abboud, Dayana Abboud, Abdulrasheed O. Abdulrahman, Ana‐Nicoleta Bondar, Julie Dam, Zafiroula Georgoussi, Jesús Giraldo, Anemari Horvat, Christos Karoussiotis, Alba Paz‐Castro, Miriam Scarpa, Hannes Schihada, Nicole Scholz, Bilge Güvenc Tuna, Nina Vardjan   +15 more
wiley   +1 more source

Glutaminase‐1 Mediated Glutaminolysis to Glutathione Synthesis Maintains Redox Homeostasis and Modulates Ferroptosis Sensitivity in Cancer Cells

Cell Proliferation, EarlyView.
GLS1‐mediated glutaminolysis supports GSH synthesis in cancer cells. GLS1 KO increases ROS, downregulates GPX4, and upregulates GPX1, making cells more sensitive to ferroptosis. Combining GLS1 or GPX1 inhibitors with a GPX4 inhibitor synergistically suppresses cancer growth.
Changsen Bai, Jialei Hua, Donghua Meng, Yue Xu, Benfu Zhong, Miao Liu, Zhaosong Wang, Wei Zhou, Liming Liu, Hailong Wang, Yang Liu, Lifang Li, Xiuju Chen, Yueguo Li   +13 more
wiley   +1 more source

Derivatives of Guanosine Triphosphate with Ribose 2′‐Hydroxyl Substituents [PDF]

, 1976
Ernest Hamel
openalex   +1 more source

Toward molecular phenotyping of temporal lobe epilepsy by spatial omics

Epilepsia, EarlyView.
Abstract Objective In temporal lobe epilepsy (TLE), detection of the epileptogenic zone predicts a good surgical outcome. When submitted to 18F‐fluorodeoxyglucose positron emission tomography (PET), some patients display lateralized, focal hypometabolism in the temporal lobe (PET+), whereas others appear normometabolic (PET−).
Isabeau Vermeulen, Ronny Mohren, Micca Neusinger, Tobias A. Dancker, Michiel Vandenbosch, Jan Beckervordersandforth, Benjamin Balluff, Rianna P. Van der Hel, Olaf E. M. G. Schijns, Govert Hoogland, Kim Rijkers, Berta Cillero‐Pastor, ACE epilepsy surgery group, Gwendolyn de Bruyn, Albert Colon, Jim Dings, Marc Hendriks, Danny Hilkman, Christianne Hoeberigs, Jochem van der Pol, Lotte de Jong, Kim Rijkers, Sylvia Klinkenberg, Vivianne van Kranen–Mastenbroek, Jeske Nelissen, Pieter Kubben, Walter M. Palm, Rob P. W. Rouhl, Olaf Schijns, Ilse van Straaten, Simon Tousseyn, Marielle Vlooswijk, Louis Wagner, Dorien Weckhuysen   +33 more
wiley   +1 more source

PI5P4K inhibitors: promising opportunities and challenges

The FEBS Journal, EarlyView.
Developing inhibitors is like climbing a steep, challenging mountain. PI5P4K inhibitors hold significant promise for the treatment of cancer, immune disorders, and neurological diseases. However, the path to success is fraught with hurdles, and researchers are therefore required to apply their expertise to overcome critical “checkpoints.” While some ...
Koh Takeuchi, Lisa Nagase, Shun Kageyama, Hirotaka Kanoh, Masashi Oshima, Aki Ogawa‐Iio, Yoshiki Ikeda, Yuki Fujii, Sei Kondo, Natsuki Osaka, Takeshi Masuda, Tsukasa Ishihara, Yoshikazu Nakamura, Yoshihisa Hirota, Takehiko Sasaki, Toshiya Senda, Atsuo T. Sasaki   +16 more
wiley   +1 more source

Modification of guanine nucleotide-regulatory components in brain membranes. II. Relationship of guanosine 5'-triphosphate effects on opiate receptor binding and coupling receptors with adenylate cyclase [PDF]

, 1984
SR Childers, G R Lariviere
openalex   +1 more source

Y12C mutation disrupts IMPDH cytoophidia and alters cancer metabolism

The FEBS Journal, EarlyView.
IMPDH, the rate‐limiting enzyme for de novo GTP synthesis, can form polymers and cytoophidia to enhance activity by reducing GTP inhibition. In this study, a Y12C mutation in IMPDH2 was introduced via ABEmax base‐editing in human cancer cell lines to disrupt IMPDH polymerisation.
Chia‐Chun Chang, Min Peng, Gerson Dierley Keppeke, Li‐Kuang Tsai, Ziheng Zhang, Li‐Mei Pai, Li‐Ying Sung, Ji‐Long Liu   +7 more
wiley   +1 more source

Pharmacology and clinical potential of guanylyl cyclase C agonists in the treatment of ulcerative colitis

Drug Design, Development and Therapy, 2013
Giovanni M Pitari Department of Pharmacology and Experimental Therapeutics, Thomas Jefferson University, Philadelphia, PA, USA Abstract: Agonists of the transmembrane intestinal receptor guanylyl cyclase C (GCC) have recently attracted interest as ...
Pitari GM
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