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Aminoglutethimide first generation aromatase inhibitor has b
2025-01-17
Aminoglutethimide, first generation aromatase inhibitor, has been tried as an antiepileptic drug in combination with other standard drugs (Aguilar et al., 1961). Letrozole is a third generation reversible non-steroidal aromatase inhibitor, approved by US-FDA, for the treatment of postmenopausal wome
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As with most G protein coupled receptors GPCRs sustained
2025-01-17
As with most G protein-coupled receptors (GPCRs), sustained activation of APJ can cause desensitization and this has been reported to occur for APJ-mediated effects on cytoplasmic Ca2+ concentration, as well as for effects on activity of adenylyl cyclase, ERK and Akt (Ishida et al., 2004, Masri et a
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br LO synaptic integrity and memory Interestingly several gr
2025-01-16
12/15LO, synaptic integrity, and memory Interestingly, several groups have found that 12/15LO directly modulates synaptic function. Normandin and colleagues reported that pharmacological inhibition of 12/15LO modulates rat hippocampal long-term depression (LTD), a process by which neuronal synapt
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br Regulation of BCAA catabolism The BCAA catabolic system i
2025-01-16
Regulation of BCAA catabolism The BCAA catabolic system is equipped in mammalian cells to dispose of excess BCAAs, presumably resulting in relatively stable concentrations of BCAAs in blood and tissues in humans. The main BCAA catabolic pathway is localized in the mitochondria of all tissues. The
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br Discussion With recently improved understanding of the
2025-01-16
Discussion With recently improved understanding of the role of βARK1 in the progression of HF and as a potential therapeutic target in HF, we explored the relationship between plasma βARK1, as a marker of chronic sympathetic overactivation, and physical symptoms in HF. Our main findings were 1) e
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AMPK is a serine threonine protein
2025-01-16
AMPK is a serine/threonine protein kinase composed of a catalytic α subunit with the activating phosphorylation site (Thr172) and two regulatory subunits, β and γ. The two AMPK variants, α1 and α2, show different cellular localization in mammalian cells. AMPKα2 is detected in nuclear and non-nuclear
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Adiponectin belongs to the CTRP
2025-01-16
Adiponectin belongs to the CTRP (C1q/TNF-related protein) superfamily. Except for adiponectin, 15 additional members have been identified (CTRP1-15) (Schaffler and Buechler, 2012). Of all the CTRPs, CTRP9 has the highest identity to adiponectin in globular domain (Wong et al., 2009). The structure o
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br ACK inhibitors Since ACK activation is correlated with po
2025-01-16
ACK1 inhibitors Since ACK1 activation is correlated with poor prognosis in various cancers, strong efforts are being directed by multiple groups towards developing highly potent and specific small molecule inhibitors targeting the ACK1 kinase. At least eight small molecule kinase inhibitors have
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Earlier studies revealed an interaction between HSP and ACK
2025-01-16
Earlier studies revealed an interaction between HSP90β and ACK1 [15]. In the proteomic approach, we show that ACK1 associates with HSP90α and HSP90β. Additionally, we confirm the existence of a HSP90-ACK1 complex with co-IP experiments. We further analysed whether an inhibition of HSP90 affected the
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The cytoplasmic domain of muscle AChR is
2025-01-16
The cytoplasmic domain of muscle AChR is not accessible to Capecitabine in vivo. Theoretically, therapy with the cytoplasmic domains should be safe. Safety is demonstrated by the facts that: (1) rats repeatedly immunized with the cytoplasmic domains in TiterMax adjuvant do not develop EAMG, althoug
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Using constant potential amperometry and electrochemical
2025-01-16
Using constant potential amperometry and electrochemical enzyme-based biosensors selective for choline—and, therefore, an accurate readout of Dopamine receptor ligand release (Baker et al., 2015; Bruno et al., 2006a; Parikh et al., 2004, 2007)—tonic and phasic release of acetylcholine were measured
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br Conflict of interest statement br Benign prostatic
2025-01-16
Conflict of interest statement Benign prostatic hyperplasia (BPH) is a highly complex process characterized by an increased number of epithelial and stromal Ethacrynic Acid in the transition zone. , , Autopsy studies by McNeal detail the evolution of histological changes within these 2 cellul
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br Funding This work was supported by
2025-01-16
Funding This work was supported by Arena Pharmaceuticals, Inc, San Diego, CA, USA. Introduction 5-hydroxytryptamine 1B (5-HT1B) receptors are widely distributed in the central nervous system (CNS); they have various modulatory functions in drug reinforcement, appetitive behaviors, stress, moo
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Inhibitors of mPGES are considered as safe alternative
2025-01-16
Inhibitors of mPGES-1 are considered as safe alternative to NSAIDs in the treatment of chronic inflammatory diseases that are characterized by excessive PGE2 production (Bahia et al., 2014; Khurana and Jachak, 2016; Koeberle et al., 2016; Korotkova and Jakobsson, 2014; Norberg et al., 2013; Psarra e
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br Materials and methods br Results br
2025-01-16
Materials and methods Results Discussion Prostate cancer represents an ideal candidate for chemoprevention because of its high incidence and long latency to clinically significant disease [17]. The precancerous lesion PIN may also be a suitable target for ablation in chemoprevention strateg
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