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In an effort to determine if one ARI was
2023-05-25

In an effort to determine if one 5ARI was more effective than the other, the Enlarged Prostate International Comparator Study (EPICS) [17] compared treatment with finasteride and dutasteride in 1630 men over the age of 50 and concluded that after one year of treatment, both groups had statistically
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br LOX in colorectal cancer Colorectal cancer CRC like
2023-05-25

5-LOX in colorectal cancer Colorectal cancer (CRC) like other malignancies exhibits an overexpression of 5-LOX. Ohd et al. (Ohd et al., 2003) revealed in a study that malignant colon tissues overexpress 5-LOX activity and retain elevated levels of inflammatory mediators, leukotrienes. Additionall
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ABC super family proteins are found in
2023-05-25

ABC super family proteins are found in all forms of life and ABC-F subfamily of proteins are involved in cellular processes such as translational control and antibiotic resistance by ribosomal protection [3], [5]. The Mtb ABC proteins that do not contain transmembrane domains have not been studied [
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br Conflict of interest br
2023-05-25

Conflict of interest Acknowledgements Introduction The mitogen-activated protein kinase (MAPK) pathway is an important intracellular signaling system that regulates diverse cellular functions, such as proliferation, differentiation, and apoptosis [1]. Apoptosis signal-regulating kinase 1 (
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Introduction Cytochrome P CYP aromatase catalyzes the
2023-05-25

Introduction Cytochrome P450 19 (CYP19; aromatase) catalyzes the conversion of androgens to estrogens in a three-reaction sequence, where each step depends on NADPH and O2 [[1], [2], [3]]. The first two steps are accepted to be hydroxylations of the steroid C19 methyl group, whereas the final step
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Although the gene that encodes DHFR has been strongly conser
2023-05-24

Although the gene that encodes DHFR has been strongly conserved during evolution, subtle differences in the active sites of bacterial, human and parasite CB-5083 have been exploited to develop DHFR inhibitors specific to particular pathogens 1, 3. For example, pyrimethamine and cycloguanil bind str
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Based on structure activity relationship of several SARM tem
2023-05-24

Based on structure activity relationship of several SARM templates, Ligand Pharmaceuticals chose LGD2226 as their first clinical candidate (Miner et al., 2007). Although LGD2226 demonstrated myo- and osteo-anabolic activity and maintenance of sexual function in various preclinical models, the develo
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PF is orally bioavailable and has appropriate
2023-05-24

PF-06409577 is orally bioavailable and has appropriate pharmacokinetic properties for use in rodents, allowing us to evaluate its impact on lipid and cholesterol biosynthesis in vivo (Cameron et al., 2016). PF-06409577 lowered the incorporation of 14C-acetate into hepatic lipids in vivo in a dose de
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When arachidonic acid is used as a substrate
2023-05-24

When arachidonic Oligomycin Complex is used as a substrate, the platelet-type 12S-lipoxygenase produces predominantly the 12S-hydroperoxy derivative. In contrast, the leukocyte-type 12S-lipoxygenases generate substantial amounts of the 15-lipoxygenase product in addition to the 12S-hydroperoxy deri
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Ala a branched chain amino acid has been reported
2023-05-24

Ala, a branched chain amino acid, has been reported to play a functional role in intracellular pH regulation, and it typically accumulates in response to various stresses (Limami et al., 2008, Rocha et al., 2010). Our data demonstrated that increasing Cd concentrations at lower Cd doses resulted in
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Imatinib was first approved for the
2023-05-24

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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Imatinib was first approved for the
2023-05-24

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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Similarly compound was prepared from aldehyde
2023-05-24

Similarly, CFDA-SE synthesis 13 was prepared from aldehyde 8d by following similar procedures (Scheme 3). Condensation of 13 with 7b or 7e provided the corresponding amides 9j or 9k, which then went through O-debenzylation by BCl3 to deliver the final compounds 10j and 10k in 37% and 32% overall yi
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agonists simulate norepinephrine NE in binding to presynapti
2023-05-24

α2 agonists simulate norepinephrine (NE) in binding to presynaptic surface autoreceptors, which in turn mediates feedback inhibition of NE release. Another major control mechanism for noradrenergic neurotransmission is termination of signaling by presynaptic NE transporter (NET)-mediated NE reuptake
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In conclusion we have shown
2023-05-24

In conclusion, we have shown that mGlu7 receptors negatively regulate α1-adrenergic receptor signalling in heterologous expression systems, alkaline phosphatase inhibitors tissue and living animals. This interaction might represent a protective mechanism aimed at restraining an excessive activation
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