Results 61 to 70 of about 131,252 (300)

Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor [PDF]

Proceedings of the National Academy of Sciences, 2013
μ-Opioid receptors are among the most studied G protein-coupled receptors because of the therapeutic value of agonists, such as morphine, that are used to treat chronic pain. However, these drugs have significant side effects, such as respiratory suppression, constipation, allodynia, tolerance, and dependence, as well as abuse potential.
Neil T, Burford, Mary J, Clark, Tom S, Wehrman, Samuel W, Gerritz, Martyn, Banks, Jonathan, O'Connell, John R, Traynor, Andrew, Alt   +7 more
openaire   +2 more sources

The heterodimeric amino acid transporters (HAT) of the SLC7/SLC3 family: A structure−function relationships and relevance to human pathology

FEBS Letters, EarlyView.
Heterodimeric amino acid transporters consist of SLC7 and SLC3 family proteins arranged in a conserved structural organization. They regulate nutrient transport across cell membranes, supporting essential cellular functions. These transporters also contribute to xenobiotic/drug uptake and distribution.
Mariafrancesca Scalise, Tiziano Mazza, Raffaella Scanga, Lara Console, Michele Galluccio, Cesare Indiveri   +5 more
wiley   +1 more source

Membrane composition and thermodynamic identity as boundaries of life for synthetic cell research

FEBS Letters, EarlyView.
What makes a cell a cell? The boundary of a living cell is not just a wall. Read as a Markov blanket, the membrane separates internal from external states, generating identity and non‐equilibrium order. Can this identity be rebuilt from scratch in a synthetic cell?
Caterina Presutti, Bert Poolman
wiley   +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

Positive Allosteric Modulation of CB1 and CB2 Cannabinoid Receptors Enhances the Neuroprotective Activity of a Dual CB1R/CB2R Orthosteric Agonist

Life, 2020
Preclinical studies highlighted that compounds targeting cannabinoid receptors could be useful for developing novel therapies against neurodegenerative disorders.
Beatrice Polini, Chiara Cervetto, Sara Carpi, Simone Pelassa, Francesca Gado, Rebecca Ferrisi, Simone Bertini, Paola Nieri, Manuela Marcoli, Clementina Manera   +9 more
doaj   +1 more source

Allosteric modulators of human A2B adenosine receptor.

, 2014
Background Among adenosine receptors (ARs) the A2B subtype exhibits low affinity for the endogenous agonist compared with the A 1, A2A, and A3 subtypes and is therefore activated when concentrations of adenosine increase to a large extent following ...
Cosimelli B, MARTINI, CLAUDIA, Pugliesi I, Severi E, Greco G, Novellino E, GIACOMELLI, CHIARA, DANIELE, SIMONA, BARRESI, ELISABETTA, Laneri S, TALIANI, SABRINA, TRINCAVELLI, MARIA LETIZIA, DA SETTIMO PASSETTI, FEDERICO   +12 more
core   +1 more source

IMPDH inhibition enhances cytarabine efficacy in SAMHD1‐expressing leukaemia cells via guanine nucleotide depletion

Molecular Oncology, EarlyView.
Cytarabine is a key therapy for acute myeloid leukaemia (AML), but its efficacy is limited by the dNTPase SAMHD1, which hydrolyses its active metabolite. Screening nucleotide biosynthesis inhibitors revealed that IMPDH inhibitors selectively sensitise SAMHD1‐proficient AML cells to cytarabine.
Miriam Yagüe‐Capilla, Christopher Dirks, Caroline Eiden, Sonja K. Fesenmayer, Femke M. Hormann, Yolande Klootsema, Ingrid Lilienthal, Si Min Zhang, Nikolas Herold, Sean G. Rudd   +9 more
wiley   +1 more source

Allosteric Modulators: A Side Door [PDF]

Journal of Medicinal Chemistry, 2015
Allosteric modulators of the cannabinoid CB1 receptor were first discovered in 2005. Since then, although both negative and positive allosteric modulators have been uncovered, many questions remain about their site(s) of action, as well as the basis of their signaling.
openaire   +2 more sources

Loss of proton‐sensing TDAG8 increases tumor progression in mouse models of colon cancer

Molecular Oncology, EarlyView.
Loss of the pH‐sensing receptor TDAG8 accelerates colorectal cancer progression in mice. Animals lacking TDAG8 expression had increased tumor growth, DNA damage, and recruitment of tumor‐associated immune cells, including macrophages, neutrophils, and monocytes.
Ermanno Malagola, Yasmine Illi, Anna Bircher, Marijn Wilmink, Rachele F. Malagutti, Solenn Ottié, Cordelia Schuler, Pedro A. Ruiz, Cheryl de Vallière, Klaus Seuwen, Gerhard Rogler, Martin Hausmann   +11 more
wiley   +1 more source

The Structural Basis of ATP as an Allosteric Modulator [PDF]

PLoS Computational Biology, 2014
Adenosine-5'-triphosphate (ATP) is generally regarded as a substrate for energy currency and protein modification. Recent findings uncovered the allosteric function of ATP in cellular signal transduction but little is understood about this critical behavior of ATP.
Shaoyong Lu, Wenkang Huang, Qi Wang, Qiancheng Shen, Shuai Li, Ruth Nussinov, Jian Zhang 0037   +6 more
openaire   +4 more sources