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The nAChR has been considered
2024-04-09

The α7 nAChR has been considered an interesting potential target for numerous therapeutic indications over the last two decades, with GTS-21 one of the first candidates proposed for Alzheimer's disease [2], [3], [23]. Unfortunately, although many α7-selective agonists have been developed [21], none
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Our study like that of Zill et al
2024-04-09

Our study, like that of Zill et al. (2012) included European Caucasians, although their population was much smaller (n=162) and more heterogeneous (19–72years). Further, potential confounding or effect modification by other health, lifestyle or genetic factors was not considered. These differences m
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The role of DHT in
2024-04-09

The role of DHT in early teleost embryogenesis is not entirely clear or established, however additional studies that treat fish embryos to DHT or to specific srd5a inhibitors at critical stages of development (i.e. prior to sex differentiation) will shed light on the early functions of this androgen
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In the last decade the
2024-04-09

In the last decade, the zebrafish has emerged as a valuable vertebrate model to systematically dissect the genetic underpinnings of both vertebrate heart development and function [8,9], as well as distinct cardiac diseases such as congenital heart disease [10], cardiomyopathies [11,12] and cardiac a
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br Materials and methods br
2024-04-09

Materials and methods Results Discussion Many studies investigate the role of 12/15-LOX in cancer cell,23, 24, 25 however we here first found that host 12/15-LOX also plays an important role in metastasis progression. We have demonstrated that 12(S)-HETE increased melanoma cell adhesion to
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There are increasing repeated reports of amphotericin B resi
2024-04-08

There are increasing repeated reports of amphotericin B-resistance in pathogenic fungi including Candida spp. [35], [36]. Nolte et al. characterized some fluconazole and amphotericin B-resistant Candida albicans isolates from leukemia patients [37]. Fan-Havard et al. (1991) have shown multi-antifung
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Sorafenib was the first small RTK
2024-04-08

Sorafenib was the first small RTK inhibitor drug to be developed and was initially approved against renal cell carcinoma, then against hepatocellular carcinoma (HCC) and more recently for differentiated thyroid treatment [111]. Sunitinib soon followed, being approved for gastrointestinal stromal tum
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Here we found that AMPK directly phosphorylates EZH
2024-04-08

Here we found that AMPK directly phosphorylates EZH2 at Thr311 to disrupt its interaction with SUZ12 and to inhibit PRC2 enzymatic activity, which is supported by the increased expression of PRC2-repressed genes. Furthermore, the T311E-EZH2 mutant that mimics AMPK-mediated phosphorylation status sup
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br Conflict of interest statement br Introduction Tanshinone
2024-04-08

Conflict of interest statement Introduction Tanshinone IIA (Tan IIA) is a major active component of Salvia miltiorrhiza (S. miltiorrhiza), a well-known Chinese traditional medicine that is used for the treatment of cardiovascular and cerebrovascular diseases [1]. Tan IIA exhibits diverse pharm
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A unique finding in this
2024-04-08

A unique finding in this study is that 12/15-LO influences CREB phosphorylation in the murine brain. While previous reports have found that knockout of 5-lipoxygenase, a related enzyme that also uses arachidonic Imiquimod hydrochloride sale for substrate, can regulate CREB phosphoryation in the cont
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Recently two distinct small molecule inhibitors of
2024-04-08

Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer MK2 inhibitor with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces the g
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br Current therapies for metabolic diseases Inborn errors
2024-04-08

Current therapies for metabolic diseases Inborn errors of metabolism caused by deficiency of particular enzymes due to loss of function mutations or deletions have been treated by decreasing the intake of the enzymatic substrate, supplementation with an essential cofactor or vitamin, increasing m
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br Conflict of interest br Introduction The Piezo proteins P
2024-04-08

Conflict of interest Introduction The Piezo proteins, Piezo1/FAM38A and Piezo2/FAM38B, are multi-pass transmembrane proteins that have been identified as mechanically-activated (MA) homomultimeric, pore-forming ion channels [1,2]. Piezo1 is broadly expressed with its highest expression in blad
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Miltefosine It is well known that TCDD is the most potent
2024-04-08

It is well-known that TCDD is the most potent ligand of AhR and it regulates gene expression, such as CYP1A1, via activation of AhR (Mimura and Fujii-Kuriyama, 2003). Besides Tomblin et al. (2016) have recently shown that TCDD via AhR regulated L-type amino Miltefosine transporter 1 expression in M
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It is also possible that
2024-04-08

It is also possible that α2-adrenoceptor activation may inhibit glutamate accumulation by upregulating the glutamate-buffering activity of Müller Disulfiram mg through EAAT1 or adjusting EAAT2 in bipolar cells, as well as the NMDA receptor. Therefore, we investigated whether topical administration
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