• In the a first in vitro

  2021-11-15

  

  In the 2003, a first in vitro indication of modulation of FXR expression in CRC showed that FXR expression was absent in undifferentiated colon carcinoma cell line SW480, while it was progressively increasing along with the degree of cell differentiation in Caco2 and HT29 cells, and its transcriptio

• br Results and discussion br Conclusion In summary we design

  2021-11-15

  

  Results and discussion Conclusion In summary, we designed and discovered a series of novel GPR40 agonists containing 3,5-dimethylisoxazole with improved tPSA and ideal cLog P. Most of these compounds were confirmed as excellent GPR40 agonists in vitro. Especially, compound 11k exhibited robust

• Recently Bristol Myers Squibb and

  2021-11-15

  

  Recently, Bristol-Myers Squibb and Merck reported their GPR40 agonist research focused on the modification of α,β-position of phenylpropionic rac1 inhibitor derivatives. For example, in recent published patent applications, Bristol-Myers Squibb claimed the pyrrolidine and dihydropyrazole GPR40 agon

• Another lever to efficiently eradicate tumors including ovar

  2021-11-15

  

  Another lever to efficiently eradicate tumors including ovarian cancer might rely on their high addiction to iron [34]. In fact, ultrasmall silica-based nanoparticles, functionalized with melanoma-targeting peptide, efficiently triggered ferroptosis not only in cell culture but also in tumor bearing

• br Introduction Erythropoietin EPO is a glycoprotein hormone

  2021-11-15

  

  Introduction Erythropoietin (EPO) is a glycoprotein hormone and the principal stimulator of erythropoiesis (Jelkmann, 2011). EPO promotes the proliferation and differentiation of red blood cells, which is important for oxygen transport. Low EPO levels in blood cause anemia; however, excessive lev

• Arena Pharmaceutical introduced a biaryl

  2021-11-15

  

  Arena Pharmaceutical introduced a biaryl sulfone derivative with antagonistic activity at H3Rs known as APD-916, ((R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine), which was rationally designed from corresponding sulfonamides in order to yield compounds with short dura

• In the current study Olfml

  2021-11-15

  

  In the current study, Olfml1 knockdown increased YAP but decreased the respective target genes of canonical Wnt signaling and Hedgehog signaling, Axin2 and Gli1. YAP suppresses canonical Wnt via binding to Dishevelled and/or β-catenin [[39], [40], [41], [42]]. Tariki et al. reported that adenovirus-

• Based on our results we propose three possible mechanisms

  2021-11-15

  

  Based on our results, we propose three possible mechanisms of HER2 loss after trastuzumab-based therapy (Fig. 3). The first possibility is a result of the differential effects of treatments on clonal subsets. In breast cancer, such selective pressure has been suggested to preferentially eradicate HE

• Starting from the hypothesis that the linker

  2021-11-15

  

  Starting from the hypothesis that the linker portion of the inhibitor molecules does not necessarily require the presence of an alcohol/ether or a carbonyl group, the same research group performed another scaffold hopping analysis, obtaining 1500 new compounds as potentially active HO-1 inhibitors [

• The inhibitory concentration of atrial natriuretic factor at

  2021-11-15

  

  The 50% inhibitory concentration of atrial natriuretic factor at midgestation and term are –7.4 ± 0.12 and –7.38 ± 0.11, respectively, demonstrating no gestational age dependency in the effect of atrial natriuretic factor on spontaneous contractile activity. Diethyl amine/nitric oxide starts to inh

• CFTRinh-172 mg A general synthetic pathway to these tricycli

  2021-11-12

  

  A general synthetic pathway to these tricyclic structures is described in (detailed procedures can be accessed in the patent application WO 2011/014520 A2). Benzylation of the appropriate ketoester using KHMDS, followed by treatment with DMF-dimethyl acetal yielded the racemic (dimethylamino)-methyl

• We tested this hypothesis with two experiments

  2021-11-12

  

  We tested this hypothesis with two experiments. In the first experiment OVX monkeys implanted with an E2 Biperiden HCl (this results in LH levels similar to the level during the follicular phase) were treated with daily injections of letrozole for 1 week and then EB was injected systemically mimick

• br Acknowledgments br Introduction Postmenopausal

  2021-11-12

  

  Acknowledgments Introduction Postmenopausal osteoporosis, which is primarily caused by 5-Methyl-CTP receptor deficiency, has been a worldwide health problem and threatens postmenopausal women of all races. An estimated 80% of osteoporosis patients in the United States are women, and approxima

• Here we investigated on epigenetic regulatory mechanisms of

  2021-11-12

  

  Here, we investigated on epigenetic regulatory mechanisms of ALX/FPR2 expression. Epigenetic changes, that include phosphorylation, acetylation, methylation and ubiquitination of DNA and histone proteins, occur in a variety of diseases [21] and are being recognized as key targets for personalized me

• Reports described a range of synthetic GPR agonists with des

  2021-11-12

  

  Reports described a range of synthetic GPR40 agonists with desirable safety and efficacy profiles, compared with existing antidiabetic therapies such as insulin and sulfonylureas [[20], [21], [22], [23], [24], [25], [26], [27], [28]]. Among them, several small molecules were tested in the clinical t

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