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Linagliptin is a recently approved dipeptidyl peptidase DPP
2024-11-18
Linagliptin is a recently approved dipeptidyl peptidase-4 (DPP-4) inhibitor and widely considered as first-line treatment for patients with type 2 diabetes. DPP-4 is responsible for the inactivation of incretin hormones, such as glucagon-like peptide 1 (GLP-1). GLP-1 is released by the intestine aft
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Some of the mechanisms that involve
2024-11-18
Some of the mechanisms that involve 12-LOX as a potential pathogenic enzyme are illustrated in Fig. 2. Direct β cell effects associated with the stimulation of 12-LOX activity include the activation of second messengers c-Jun N-terminal kinase and p38 MAPK, both of which show increased phosphorylat
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The relationship between AG and tau deposition in
2024-11-18
The relationship between AG and tau deposition in the presence of Aβ burden warrants more research in AD and in other primary tauopathies (not associated with accumulation of Aβ plaques). Our findings highlight the importance of measuring AG, as this relationship was not evident for total lasofoxife
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Imatinib was first approved for the treatment of Philadelphi
2024-11-18
Imatinib was first approved for the treatment of Philadelphia chromosome positive chronic myelogenous leukemia in 2001 [25]. This first approved small molecule antagonist is quite unusual in that it provides a durable response that lasts for more than a decade in the majority of patients. Imatinib h
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Our results add to previously published data on the contribu
2024-11-18
Our results add to previously published data on the contribution of ALDH3A1 to the optical properties of the cornea. Specifically, the study by Nees et al. (2002) was among the first to examine whether ALDH3A1 serves as a structural component in the cornea and similarly to lens crystallins. Their ex
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br Preliminary remarks Expression of the transcription facto
2024-11-18
Preliminary remarks Expression of the transcription factor aryl hydrocarbon receptor (AHR) and the AHR-repressor (AHRR) are both strikingly high in the src inhibitor of barrier organs skin and gut [1,2]. It is generally assumed that this reflects their role in linking environmental factors to an
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The cavity volume of the binding pocket may differ not
2024-11-18
The cavity volume of the binding pocket may differ not only between species but also among various AhR/ARNT isoforms within a single species. It is noteworthy that even a single amino Mouse iPSC Chemical Reprogramming Cocktails Kit plus substitution within a binding pocket may result in a change in
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In a recent series of studies from our
2024-11-18
In a recent series of studies from our laboratory, to characterize the contractile systems within the rat GM6001 wall, three conditions were identified that led to detrusor activity: spontaneous micro-contractions, electrical field stimulated (EFS) contractions and muscarinic agonist induced contra
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Although the effects of adenosine receptor signaling in acut
2024-11-18
Although the effects of adenosine receptor signaling in acute renal IRI have been attributed to the generation of high concentrations of adenosine, we have recently reported an increase in kidney levels of both AMP and adenosine, with a concomitant fall in ATP and ADP. We have also previously demons
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Materials and methods br Results
2024-11-18
Materials and methods Results Discussion The BV-tag-based electrochemiluminescence immunoassay is an extremely sensitive assay. It has been employed for detecting analytes present in only picogram quantities (e.g., bacterial toxins [26], Drug Library for Research [19]), measuring the activit
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Using constant potential amperometry and electrochemical enz
2024-11-18
Using constant potential amperometry and electrochemical enzyme-based biosensors selective for choline—and, therefore, an accurate readout of N-Acetylneuraminic acid sale release (Baker et al., 2015; Bruno et al., 2006a; Parikh et al., 2004, 2007)—tonic and phasic release of acetylcholine were meas
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rs G allele was previously associated with a decrease in
2024-11-18
rs523349 G allele was previously associated with a decrease in the conversion rate of testosterone to DHT (Beesley et al., 2007). This SRDA52 variant may have a trend towards higher testosterone availability, which according to the US Food and Drug Administration is described as a teratogen of categ
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Our co IP data show
2024-11-18
Our co-IP data show that 5HT1A or 5HT2A receptors do not heterodimerize with mGluR1α receptors. Given that both 5-HT and mGlu receptors are GPCRs and produce anxiolytic effects, a degree of cooperativity via a functional cross-talk may still exist between these receptors [11]. In addition to the fun
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br Conclusion There have been multiple
2024-11-18
Conclusion There have been multiple clinical trials and pre-clinical studies that have tested the utility of 5ARIs in treating prostate disease, as summarized in Fig. 1. Inhibiting androgen action through the use of finasteride and dutasteride has been established as a valuable resource for physi
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Crystal structures were obtained of sulfonamide and
2024-11-18
Crystal structures were obtained of sulfonamide 18 and amide 19 as a derivative of amide 36 (Fig. 7A and B). The precise rotameric orientation of amide 36 was of significant interest to understand the compound's interaction with the protein. As it would be difficult to assign the rotomer of 36, the
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