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At one time the biological effects of cAMP were
2021-02-24
At one time, the biological effects of cAMP were thought to be mediated exclusively by Protein Kinase A (PKA). Consistent with this, PKA inhibitors have been shown to reverse the effects of cAMP-elevating agents on VSMC proliferation [5]. However, we recently reported that cAMP-mediated inhibition o
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bacteriological It is well known that acrolein a metabolite
2021-02-24
It is well known that acrolein, a metabolite of cyclophosphamide, is responsible for the cyclophosphamide-induced cystitis, and that acrolein is capable of activating TRPA1 channels expressed in the capsaicin-sensitive primary afferents [2], [11]. In this context, it is likely that the early phase o
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Introduction The annual global market of industrial enzymes
2021-02-24
Introduction The annual global market of industrial opioid receptor is reported to be billions of USD [1], [2], [3], [4], [5], [6], [7], and impacts commercial sectors that include energy, animal feed, household products, food processing and pharmaceuticals [1], [2], [5], [6]. Enzymatic processing
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Lavallee et al reported that
2021-02-24
Lavallee et al. [30] reported that PREG could be esterified by lecithin:cholesterol acyltransferase (LCAT). LCAT uses cholesterol and phosphatidyl choline present in the newly formed high-density lipoprotein (HDL) as substrates and convert them into cholesteryl esters and lysophosphatidyl choline. T
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br Acknowledgements The authors are
2021-02-24
Acknowledgements The authors are supported by National Institutes of Health grants (CA162804, CA92584, and CA13499 to DJC and CA166677 to BPPC) and Cancer Prevention and Research Institute of Texas (RP110465 to DJC). The cellular response to DNA double-strand break (DSB) formation is an essent
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Several highly potent CysLT receptor
2021-02-23
Several highly potent CysLT1 receptor antagonists with large structural AZD6738 have been developed. Beyond antagonists with structures analogous to cysteinyl leukotrienes, other subclasses comprise: (a) hydroxyacetophenones, (b) indoles and indazoles, (c) quinolines, benzothiazoles, and thiazoles.
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In cancer interactions between the transformed cancer
2021-02-23
In cancer, interactions between the transformed cancer coelenterazine and other cell types recruited to the tumor are important. Tumor associated macrophages provide cancer cells with a suitable low-grade inflammatory milieu including growth promoting factors. Our results suggest a novel pro-tumori
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Recently it has been shown that among
2021-02-23
Recently, it has been shown that among the ELR (+) chemokines mentioned above, particularly IL-8 induces neutrophil migration via CXCR-1 chemokine receptor. For example, Godaly et al. [18] reported the potent role of CXCR-1 chemokine receptor in the process of neutrophil migration across epithelial
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Previous studies on the chemokines
2021-02-23
Previous studies on the chemokines role in depression are not detailed enough, and cannot sufficiently demonstrate even a hypothetical mechanism explaining the differences in levels of particular chemokines and their receptors, in relation to the severity of depression [29], [30]. Previous studies o
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As described above we designed and synthesized
2021-02-23
As described above, we designed and synthesized a new 1,4-di-substituted isoquinoline lead compound, and was identified as a ligand with moderate potency for the CRTH2 receptor. We initially we examined the effects of the steric factor of R group on the CRTH2 binding potency (). When the methyl grou
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(+)- Corydaline Taken together our results demonstrate that
2021-02-23
Taken together, our results demonstrate that the changes of striatal dopamine release and locomotor activity observed following chronic nicotine treatment and consequent acute withdrawal are mediated by CRF1, but not CRF2. Previous studies have already indicated that blocking CRF1 would prevent some
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br Funding sources br Introduction Psychiatric
2021-02-23
Funding sources Introduction Psychiatric comorbidities affect up to 70% of people with pharmacoresistant epilepsy and significantly impact quality of life [1]. Psychiatric comorbidities in epilepsy have been thought to be due to psychosocial stress. However, recent evidence suggests a more com
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pth hormone Based on the above we hypothesized that a PROTAC
2021-02-23
Based on the above, we hypothesized that a PROTAC strategy would be effective to induce CK2 protein degradation. Herein reported is an approach for the preparation of novel PROTACs via “click reaction” for degradation of CK2 protein (Fig. 2). Importantly, “click reaction” is a very facile, selective
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orexin Despite the sources of error
2021-02-23
Despite the sources of error discussed above, several trends have emerged and much valuable data are available regarding binding affinities of progestogens for different steroid receptors. All the progestogens bind to the PR with a high affinity, typically in the nanomolar range. For example the syn
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When women reach the menopause they experience a
2021-02-23
When women reach the menopause they experience a number of physical complaints such as hot flushes, vaginal dryness and mood changes [1]. Bone loss also becomes manifest at this time [1], [2], but women will often not suffer from back pain before a vertebral fracture occurs. Women who have had one f
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