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br Material and methods br Results Table shows
2024-06-06
Material and methods Results Table 1 shows that in addition to Leu/CysAP and DPPIV, genes for AspAP, ArgAP, MetAP, APM and PSA are expressed in adipocytes. The kinetic parameters of these AP are also shown in Table 1, revealing that APM has the highest Vmax and catalytic efficiency (Kcat/Km),
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The lactam emerged as lead
2024-06-06
The lactam (6) emerged as lead candidate due to its high selectivity, outstanding potency (against ALK or in clinically known ALK mutants), low in vitro clearance, and low efflux potential. The lactam (6) was selected for further profiling against the resistant ALK mutants. Preclinical rat pharmacok
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Camptothecin As we previously observed in the NSFT Fukumoto
2024-06-06
As we previously observed in the NSFT (Fukumoto et al., 2014), the effect of LY341495 in the FST was also inhibited by a 5-HT1A receptor antagonist, indicating the role of the 5-HT1A receptor in the actions of LY341495. Among the 5-HT1A receptors, which exist both presynaptically and postsynapticall
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Subsequently Palvimaki et al corroborated Ni and
2024-06-06
Subsequently, Palvimaki et al. (1999) corroborated Ni and Miledi's study by demonstrating that treatment with fluoxetine leads to 43% occupancy of the 5-HT2C receptors. Moreover, the affinity of fluoxetine for 5HT2C receptors (Ki 65 nM) is close to its affinity for 5-HT transporters (Ki 33 nM) (Ni a
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Systematic administration of ABT amino bromophenyl morpholin
2024-06-06
Systematic administration of ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin-3-yl) pyrido[2,3-d] pyrimidine), a potent and selective non-nucleoside AK inhibitor, also generates analgesic effects in animal models of pain (Jarvis et al., 2000, Kowaluk et al., 2000, Suzuki et al., 2001), sug
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br Conclusion br Conflicts of interest br Introduction
2024-06-06
Conclusion Conflicts of interest Introduction Enzymes are widely applied as biocatalysts in fields such as synthetic chemistry [1], pharmaceuticals [2], environmental treatment [3], and food technology [4] because they can catalyze chemical transformations in a highly selective manner under
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Because LTs are proved to mediate multiple biological and pa
2024-06-06
Because LTs are proved to mediate multiple biological and pathological responses in various disease states, the 5-LO biosynthetic pathway producing LTs from AA have been the target of drug discovery efforts for over two decades. As observed from literature, a pile of research efforts has been direct
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It has been known that LOX is the rate limiting
2024-06-06
It has been known that 5-LOX is the rate-limiting enzyme for the products of LTs, and LTs actively participate in the activation of neutrophils [10]. In our study, we determined whether 5-LOX was upregulated in pancreatic tissues during ANP. Moreover, we investigated whether the inhibition of expres
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Several dehidropregnenolone derivatives functionalized at C
2024-06-06
Several 16-dehidropregnenolone derivatives functionalized at C3, C4, C5 and C6 (Fig. 7) were prepared and evaluated as 5α-reductase inhibitors bearing in mind that after the formation of an enzyme-steroid complex a nucleophilic portion of the enzyme attacks the double bond of the steroid through Mic
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br Clinical realities br Commentary on uses of
2024-06-06
Clinical realities Commentary on uses of selective 17,20 lyase inhibitors If continued monitoring of these same parameters along with tracking of circulating ACTH in human trials confirms these new drugs are the long sought after 17,20 lyase inhibitors, then we may for the first time be able t
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Given the recent discovery of regions of single stranded DNA
2024-06-05
Given the recent discovery of regions of single-stranded DNA in the nuclei of hypoxic cells, the role for ATR in the response to hypoxic stress seems clearer . Zou and Elledge demonstrated that both Ddc 2 (the homolog of ATRIP) and ATRIP have a lower affinity for double-strand breaks than they do f
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Citral or dimethyl octadien al is a mixture of
2024-06-05
Citral or 3,7-dimethyl-2,6-octadien-1-al is a mixture of two stereoisomeric monoterpene aldehydes (the trans isomer geranial, citral A (40–62%)) and the cis isomer neral, citral B (25–38%) and serves one of the main constituent of essential oils of C. citratusis used in cosmetic, food, fungicides, p
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Reactive oxygen species is an aspect of oxidative
2024-06-05
Reactive oxygen species is an aspect of oxidative stress which are associated with many diseases such as rheumatoid arthritis, diabetes, inflammation, atherosclerosis and cancers (Collins, 2005; Halliwell, 1994). Thus, the need for naturally occurring antioxidants is of crucial importance. Some biop
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Finally impaired endothelial integrity culminates in
2024-06-05
Finally, impaired endothelial integrity culminates in an increased plasma protein concentration in the interstitial space, and thus accumulation of fluid in the ECM, favoring the swelling of the face and limbs [2] mainly. Concurrently with this systemic change, there is intense activation of coagula
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While there is structural information on the core of the
2024-06-05
While there is structural information on the core of the amyloid fibril, less is known about oligomer structure. There is evidence that the C-terminal of Aβ may form beta barrels in some oligomer species (Tay et al., 2013, Do et al., 2016), or may exist as loosely aggregated strands in other oligome
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