Results 61 to 70 of about 205,233 (331)

Theory of partial agonist activity of steroid hormones

open access: yesAIMS Molecular Science, 2015
The different amounts of residual partial agonist activity (PAA) of antisteroids under assorted conditions have long been useful in clinical applications but remain largely unexplained.
Carson C. Chow   +3 more
doaj   +1 more source

To Probe Full and Partial Activation of Human Peroxisome Proliferator-Activated Receptors by Pan-Agonist Chiglitazar Using Molecular Dynamics Simulations

open access: yesPPAR Research, 2020
Chiglitazar is a promising new-generation insulin sensitizer with low reverse effects for the treatment of type II diabetes mellitus (T2DM) and has shown activity as a nonselective pan-agonist to the human peroxisome proliferator-activated receptors ...
Holli-Joi Sullivan   +4 more
doaj   +1 more source

Measuring ligand efficacy at the mu-opioid receptor using a conformational biosensor. [PDF]

open access: yes, 2018
The intrinsic efficacy of orthosteric ligands acting at G-protein-coupled receptors (GPCRs) reflects their ability to stabilize active receptor states (R*) and is a major determinant of their physiological effects.
Livingston, Kathryn E   +4 more
core  

Partial Agonists for A3 Adenosine Receptors [PDF]

open access: yesCurrent Topics in Medicinal Chemistry, 2004
AbstractFor Abstract see ChemInform Abstract in Full Text.
Zhan-Guo, Gao, Kenneth A, Jacobson
openaire   +2 more sources

Molecular determinants of signal transduction in tropomyosin receptor kinases

open access: yesFEBS Open Bio, EarlyView.
Tropomyosin receptor kinases control critical neuronal functions, but how do the same receptors produce diverse cellular responses? This review explores the structural mechanisms behind Trk signaling diversity, focusing on allosteric modulation and ligand bias.
Giray Enkavi
wiley   +1 more source

Buprenorphine – an attractive opioid with underutilized potential in treatment of chronic pain

open access: yesJournal of Pain Research, 2015
Ish K Khanna, Sivaram PillarisettiNeuroPn Therapeutics, Alpharetta, GA, USAAbstract: Despite proven clinical utility, buprenorphine has not been used widely for the treatment of chronic pain.
Khanna IK, Pillarisetti S
doaj  

Nicotinic Activity of Arecoline, the Psychoactive Element of "Betel Nuts", Suggests a Basis for Habitual Use and Anti-Inflammatory Activity. [PDF]

open access: yesPLoS ONE, 2015
Habitual chewing of "betel nut" preparations constitutes the fourth most common human self-administration of a psychoactive substance after alcohol, caffeine, and nicotine.
Roger L Papke   +2 more
doaj   +1 more source

Determining the neurotransmitter concentration profile at active synapses [PDF]

open access: yes, 2009
Establishing the temporal and concentration profiles of neurotransmitters during synaptic release is an essential step towards understanding the basic properties of inter-neuronal communication in the central nervous system.
A Barberis   +144 more
core   +2 more sources

Tumor‐stromal crosstalk and macrophage enrichment are associated with chemotherapy response in bladder cancer

open access: yesFEBS Open Bio, EarlyView.
Chemoresistance in bladder cancer: Macrophage recruitment associated with CXCL1, CXCL5 and CXCL8 expression is characteristic of Gemcitabine/Cisplatin (Gem/Cis) Non‐Responder tumors (right side) while Responder tumors did not show substantial tumor‐stromal crosstalk (left side). All biological icons are attributed to Bioicons: carcinoma, cancerous‐cell‐
Sophie Leypold   +11 more
wiley   +1 more source

Stochastic Chemical Reactions in Micro-domains

open access: yes, 2004
Traditional chemical kinetics may be inappropriate to describe chemical reactions in micro-domains involving only a small number of substrate and reactant molecules.
D. Holcman   +7 more
core   +2 more sources

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