Results 71 to 80 of about 1,364,815 (358)

Structural overview and perspectives of the nuclear receptors, a major family as the direct targets forsmall-molecule drugs

open access: yesActa Biochimica et Biophysica Sinica, 2021
The nuclear receptors (NRs) are an evolutionarily related family of transcription factors, which share certain common structural characteristics and regulate the expressions of various genes by recognizing different response elements.
Li Fengwei   +3 more
doaj   +1 more source

Fluorescent ligand for human progesterone receptor imaging in live cells. [PDF]

open access: yes, 2013
We employed molecular modeling to design and then synthesize fluorescent ligands for the human progesterone receptor. Boron dipyrromethene (BODIPY) or tetramethylrhodamine were conjugated to the progesterone receptor antagonist RU486 (Mifepristone ...
Baker, Michael E   +5 more
core   +1 more source

Mapping the evolution of mitochondrial complex I through structural variation

open access: yesFEBS Letters, EarlyView.
Respiratory complex I (CI) is crucial for bioenergetic metabolism in many prokaryotes and eukaryotes. It is composed of a conserved set of core subunits and additional accessory subunits that vary depending on the organism. Here, we categorize CI subunits from available structures to map the evolution of CI across eukaryotes. Respiratory complex I (CI)
Dong‐Woo Shin   +2 more
wiley   +1 more source

Selective glucocorticoid receptor properties of GSK866 analogs with cysteine reactive warheads [PDF]

open access: yes, 2017
Synthetic glucocorticoids (GC) are the mainstay therapy for treatment of acute and chronic inflammatory disorders. Due to the high adverse effects associated with long-term use, GC pharmacology has focused since the nineties on more selective GC ligand ...
Atucha   +61 more
core   +2 more sources

Reciprocal control of viral infection and phosphoinositide dynamics

open access: yesFEBS Letters, EarlyView.
Phosphoinositides, although scarce, regulate key cellular processes, including membrane dynamics and signaling. Viruses exploit these lipids to support their entry, replication, assembly, and egress. The central role of phosphoinositides in infection highlights phosphoinositide metabolism as a promising antiviral target.
Marie Déborah Bancilhon, Bruno Mesmin
wiley   +1 more source

Genome-Wide Characterization of the Nuclear Receptor Gene Family in Macrostomum lignano Imply Its Evolutionary Diversification

open access: yesFrontiers in Marine Science, 2021
Nuclear receptors (NRs), a series of key transcription factors that are mostly activated by endogenous ligands or environmental xenobiotics, are reportedly good phylogenetic markers of animal genome evolution. As the early diverging class of bilaterians,
Yunying Cheng   +3 more
doaj   +1 more source

Effect of antiandrogen flutamide on measures of hepatic regeneration in rats [PDF]

open access: yes, 1989
Male rat liver undergoes a process of demasculinization during hepatic regeneration following partial hepatectomy. The possibility that antiandrogens might potentiate this demasculinization process and in so doing augment the hepatic regenerative ...
A Francavilla   +36 more
core   +1 more source

Spatiotemporal and quantitative analyses of phosphoinositides – fluorescent probe—and mass spectrometry‐based approaches

open access: yesFEBS Letters, EarlyView.
Fluorescent probes allow dynamic visualization of phosphoinositides in living cells (left), whereas mass spectrometry provides high‐sensitivity, isomer‐resolved quantitation (right). Their synergistic use captures complementary aspects of lipid signaling. This review illustrates how these approaches reveal the spatiotemporal regulation and quantitative
Hiroaki Kajiho   +3 more
wiley   +1 more source

Dopaminergic, glutamatergic but not opioidergic mechanisms mediate induction of FOS-like protein by cocaethylene [PDF]

open access: yes, 1997
Cocaethylene is a psychoactive metabolite formed\ud during the combined consumption of cocaine and ethanol. As\ud this metabolite has many properties in common with cocaine, it is conceivable that cocaethylene administration may induce the activity of ...
DiPirro, Dr. J.M.   +3 more
core  

A novel human glucocorticoid receptor SNP results in increased transactivation potential. [PDF]

open access: yes, 2017
Glucocorticoids are one of the most widely used therapeutics in the treatment of a variety of inflammatory disorders. However, it is known that there are variable patient responses to glucocorticoid treatment; there are responders and non-responders, or ...
Cho, Kiho   +5 more
core   +3 more sources

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