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FXa is a vitamin K dependent serine protease
2022-05-09
FXa is a vitamin K-dependent serine protease consisting of two chains linked by a disulfide bridge. The heavy chain contains 303 Octyl-α-ketoglutarate receptor and the light chain has 139 amino acids. The catalytic triad comprised of Ser195, His57, and Asp102 exhibits the trypsin-like β-barrel stru
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br Place in Therapy In the
2022-05-09
Place in Therapy In the case of minor bleeding, the anticoagulant effects of all FXa inhibitors except betrixaban, which has a longer half-life, will diminish within 24-48 hours of discontinuation of the drug provided the patient has normal renal function. In these cases stopping the FXa inhibito
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Recent findings of us suggest that compounds that inhibit
2022-05-09
Recent findings of us suggest that compounds that inhibit both FAAH and TRPV1 may be more efficacious in pain relief than those targeting only one such protein. As continuation of our efforts to identify new molecules able to target simultaneously both FAAH and TRPV1 receptors, we hypothesized that
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The current study aimed to understand the roles and
2022-05-09
The current study aimed to understand the roles and the underlying mechanisms of XIST in LSCC, by focusing on the regulation by miR-124-3p, which was previously identified as a target of XIST [12]. We found that the XIST expression is positively correlated with the stages of LSCC in patients. Knockd
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br Acknowledgments I thank Takeshi Sakaba
2022-05-09
Acknowledgments I thank Takeshi Sakaba for critical reading of the manuscript and helpful comments. This work was supported by JSPS/MEXT KAKENHI Grant Numbers 17K19466, 17H03548. Introduction The oral route of drug application is the main route in pharmacology since it is easy to handle and o
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br Cellular transportation of nanoparticles
2022-05-09
Cellular transportation of nanoparticles and nanocomplexes Endocytosis and exocytosis are critically important phenomena in cellular metabolism, which involve the complex vesicular system. They deal with major cellular transportation activities including membrane homeostasis by transporting prote
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This study has some limitations The RDS technique was
2022-05-09
This study has some limitations. The RDS technique was not effective for the population of MSM from Natal, as it has not reached the sample size initially calculated. Few seeds had enough waves to disperse the sample and make it closer to a probabilistic sample, even with all efforts from the resear
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br Introduction Lysine acetylation is an
2022-05-09
Introduction Lysine acetylation is an important post-translational modification that is found on numerous cellular proteins, including both histone and non-histone proteins [1], [2]. Dynamic acetylation and deacetylation is regulated by enzymes called histone acetyltransferases (HATs) as writers
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br Histamine H R The cloning of the
2022-05-09
Histamine H4R The cloning of the H3R (Lovenberg et al., 1999) provided a template for the search of other aromatase inhibitors receptors, and resulted in the most recent discovery of histamine H4R. This concluded with six independent groups that have reported the cloning of the H4R (Leurs et al.,
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Despite these studies little is known
2022-05-09
Despite these studies, little is known about the regulation of defence genes during AM root colonization. In the present study, we characterized the Ptc52 gene from tomato (named here as SlPtc52), a member of the gene family of non-heme oxygenases, and analysed its molecular characteristics. This ge
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The zinc dependent HDACs are classified into
2022-05-09
The zinc-dependent HDACs are classified into four groups based on their structure, complex formation, and expression pattern: class I (HDAC1, HDAC2, HDAC3, and HDAC8), class IIa (HDAC4, HDAC5, HDAC7, and HDAC9), class IIb (HDAC6 and HDAC10), and class IV (HDAC11) [16]. We recently reported on a cyto
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cpmt Evaluating the plausibility of this selective scenario
2022-05-07
Evaluating the plausibility of this selective scenario is challenging because of the uncertainties concerning the biological role of calpain-10 and the significance of its variants with regard to gene function and disease susceptibility. However, from a strictly evolutionary standpoint, our findings
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Because of its excellent GPR
2022-05-07
Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, Cyanine 3-dCTP was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an extensive pane
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Armed with this knowledge we looked at
2022-05-07
Armed with this knowledge, we looked at ways to reduce the log of through nitrogen incorporation while still maintaining potency via installation of ortho substituents such as chloro, methyl, bromo, and thiomethyl (). In general, pyridine analogs were less active ( vs ; vs ; vs ) than their simpl
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Because AM had limited efficacy on rodent
2022-05-07
Because (AM-3189) had limited efficacy on rodent GPR40, we used two rodent models expressing human GPR40 to demonstrate efficacy of (AM-3189). First, we used human islet transplanted nude mice. In this model, endogenous pancreatic β-cells were ablated using streptozotocin, and mice were rescued to
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