Results 41 to 50 of about 799,914 (365)

An Enantiomer of an Oral Small Molecule TSH Receptor Agonist Exhibits Improved Pharmacologic Properties

open access: yesFrontiers in Endocrinology, 2016
We are developing an orally available small molecule, allosteric TSH receptor (TSHR) agonist for follow up diagnostics of patients with thyroid cancer.
Susanne Neumann   +7 more
doaj   +1 more source

Neuroreceptor Activation by Vibration-Assisted Tunneling [PDF]

open access: yesScientific Reports 5, Article number: 9990 Published 2015, 2015
G protein-coupled receptors (GPCRs) constitute a large family of receptor proteins that sense molecular signals on the exterior of a cell and activate signal transduction pathways within the cell. Modeling how an agonist activates such a receptor is fundamental for an understanding of a wide variety of physiological processes and it is of tremendous ...
arxiv   +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

Target sites for chemical regulation of strigolactone signaling

open access: yesFrontiers in Plant Science, 2014
Demands for plant growth regulators (chemicals that control plant growth) are increasing globally, especially in developing countries. Both positive and negative plant growth regulators are widely used to enhance crop production and to suppress unwanted ...
Hidemitsu eNakamura   +3 more
doaj   +1 more source

α1D-Adrenoceptors are responsible for the high sensitivity and the slow time-course of noradrenaline-mediated contraction in conductance arteries [PDF]

open access: yes, 2013
The objective of this study was to determine whether the different time-course characteristics of α1-adrenoceptor-mediated contraction in arteries can be related to the subtypes involved.
Alexander   +53 more
core   +1 more source

Immune Checkpoints as Therapeutic Targets in Autoimmunity

open access: yesFrontiers in Immunology, 2018
Antibodies that block the immune checkpoint receptors PD1 and CTLA4 have revolutionized the treatment of melanoma and several other cancers, but in the process, a new class of drug side effect has emerged—immune related adverse events.
Christopher Paluch   +9 more
doaj   +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

Down Regulation with Luteal GnRH Agonist Therapy in Euploid Embryo Transfers Does Not Impact Pregnancy Rates [PDF]

open access: yes, 2020
Introduction : Gonadotropin-releasing hormone (GnRH) agonists have been used during assisted reproductive technology (ART) treatment for pituitary suppression and stimulation.
Bergin, MD, Keri   +4 more
core   +1 more source

Probing the role of the cation–π interaction in the binding sites of GPCRs using unnatural amino acids [PDF]

open access: yes, 2009
We describe a general application of the nonsense suppression methodology for unnatural amino acid incorporation to probe drug–receptor interactions in functional G protein-coupled receptors (GPCRs), evaluating the binding sites of both the M2 muscarinic
Ballesteros   +31 more
core   +3 more sources

A covalently bound photoisomerizable agonist. Comparison with reversibly bound agonists at electrophorus electroplaques [PDF]

open access: yes, 1980
After disulphide bonds are reduced with dithiothreitol, trans-3-(alpha-bromomethyl)-3’-[alpha-(trimethylammonium)methyl]azobenzene (trans-QBr) alkylates a sulfhydryl group on receptors.
Erlanger, Bernard F.   +4 more
core   +2 more sources

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