Results 61 to 70 of about 1,168,781 (390)

Serotonin and motherhood: From molecules to mood [PDF]

open access: yes, 2019
Emerging research points to a valuable role of the monoamine neurotransmitter, serotonin, in the display of maternal behaviors and reproduction-associated plasticity in the maternal brain.
Li, Ming   +2 more
core   +2 more sources

From omics to AI—mapping the pathogenic pathways in type 2 diabetes

open access: yesFEBS Letters, EarlyView.
Integrating multi‐omics data with AI‐based modelling (unsupervised and supervised machine learning) identify optimal patient clusters, informing AI‐driven accurate risk stratification. Digital twins simulate individual trajectories in real time, guiding precision medicine by matching patients to targeted therapies.
Siobhán O'Sullivan   +2 more
wiley   +1 more source

Potential Adiponectin Receptor Response Modifier Therapeutics

open access: yesFrontiers in Endocrinology, 2019
Many human diseases may benefit from adiponectin replacement therapy, but due to pharmacological disadvantages of the intact protein, druggable options focus on peptidic, and small molecule agonists of the adiponectin receptor.
Laszlo Otvos, Laszlo Otvos, Laszlo Otvos
doaj   +1 more source

STING agonist therapy in combination with PD-1 immune checkpoint blockade enhances response to carboplatin chemotherapy in high-grade serous ovarian cancer

open access: yesBritish Journal of Cancer, 2018
High-grade serous carcinoma (HGSC) of the ovary is predominantly diagnosed at late stages and primarily treated with debulking surgery followed by platinum/taxane-based chemotherapy.
A. Ghaffari   +6 more
semanticscholar   +1 more source

Agonist binding, agonist affinity and agonist efficacy at G protein‐coupled receptors [PDF]

open access: yesBritish Journal of Pharmacology, 2008
Measurements of affinity and efficacy are fundamental for work on agonists both in drug discovery and in basic studies on receptors. In this review I wish to consider methods for measuring affinity and efficacy at G protein coupled receptors (GPCRs).
openaire   +3 more sources

The anabolic steroid stanozolol is a potent inhibitor of human MutT homolog 1

open access: yesFEBS Letters, EarlyView.
MutT homolog 1 (MTH1) is a member of the NUDIX superfamily of enzymes and is an anticancer drug target. We show that stanozolol (Stz), an anabolic steroid, is an unexpected nanomolar inhibitor of MTH1. The X‐ray crystal structure of the human MTH1–Stz complex reveals a unique binding scaffold that could be utilized for future inhibitor development ...
Emma Scaletti Hutchinson   +7 more
wiley   +1 more source

A Synthetic Agonist to Vasoactive Intestinal Peptide Receptor-2 Induces Regulatory T Cell Neuroprotective Activities in Models of Parkinson’s Disease

open access: yesFrontiers in Cellular Neuroscience, 2019
A paradigm shift has emerged in Parkinson’s disease (PD) highlighting the prominent role of CD4+ Tregs in pathogenesis and treatment. Bench to bedside research, conducted by others and our own laboratories, advanced a neuroprotective role for Tregs ...
R. Lee Mosley   +8 more
doaj   +1 more source

A photoisomerizable muscarinic antagonist. Studies of binding and of conductance relaxations in frog heart [PDF]

open access: yes, 1982
These experiments employ the photoisomerizable compound, 3,3'-bis- [alpha-(trimethylammonium)methyl]azobenzene (Bis-Q), to study the response to muscarinic agents in frog myocardium. In homogenates from the heart, trans-Bis-Q blocks the binding of [3H]-N-
Birdsall, Nigel J. M.   +5 more
core   +1 more source

Allosteric coupling from G protein to the agonist binding pocket in GPCRs

open access: yesNature, 2016
G-protein-coupled receptors (GPCRs) remain the primary conduit by which cells detect environmental stimuli and communicate with each other. Upon activation by extracellular agonists, these seven-transmembrane-domain-containing receptors interact with ...
Brian T DeVree   +14 more
semanticscholar   +1 more source

TRPM8 levels determine tumor vulnerability to channel agonists

open access: yesMolecular Oncology, EarlyView.
TRPM8 is a Ca2+ permissive channel. Regardless of the amount of its transcript, high levels of TRPM8 protein mark different tumors, including prostate, breast, colorectal, and lung carcinomas. Targeting TRPM8 with channel agonists stimulates inward calcium currents followed by emptying of cytosolic Ca2+ stores in cancer cells.
Alessandro Alaimo   +18 more
wiley   +1 more source

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