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Natural products are a diverse
2021-10-04

Natural products are a diverse and interesting source for the discovery of new lead structures (Newman and Cragg, 2016). After a successful era of natural product research, many pharmaceutical companies stopped their investment in natural product-driven drug discovery in the 1990s. The reason behind
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On correlating acute rejection to different risk
2021-10-03

On correlating acute rejection to different risk markers by multiple linear regression analysis, we found that serum FasL and serum creatinine were variables that were independently associated with AR. Carstens et al., reported that significant differences were present between acute rejection and ze
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On the other hand G
2021-10-03

On the other hand, G9a/GLP could also alter neuronal function without directly altering the transcription level of particular plasticity-related protein: the consolidation of early-LTP to late-LTP, as well as the reversal of mGluR-LTD by G9a/GLP inhibition required PKMζ translation and its downstrea
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A phase I clinical trial has been
2021-10-03

A phase I clinical trial has been completed for assessing CEP-26401 in cognitive impairment in healthy individuals without disclosing any results (NCT01903824). Although CEP-26401 is under clinical trial study, several projects are in progress for synthesizing novel irdabisant analogs in order to im
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Pharmacologic approaches of inhibiting GSNOR activity have
2021-10-02

Pharmacologic approaches of inhibiting GSNOR activity have reached the point of clinical development with the recent announcement of the first cystic fibrosis patients treated with the first-in-class GSNOR inhibitor, N6022 (N30 Pharmaceuticals). Clinical development is ongoing for other indications
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The compounds described in this paper were prepared using a
2021-10-02

The compounds described in this paper were prepared using a modular approach that allowed diversification of R or R at the final step (). Route A involved amide coupling of -butyl 4-(methylamino)piperidine-1-carboxylate with phenyl acetic acids (step a) using 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-m
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After the origin of the family of genes
2021-10-02

After the origin of the family of genes for receptors for peptides similar to glucagon, the genes have not remained static. Not only have their sequences evolved, but also like peptides similar to glucagon (Irwin, 2001, Irwin, 2009, Irwin, 2012, Ng et al., 2010, Hwang et al., 2013), the numbers of g
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br Acknowledgments br Introduction Postmenopausal osteoporos
2021-10-02

Acknowledgments Introduction Postmenopausal osteoporosis, which is primarily caused by Nocodazole 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 approximately 30% of
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At this point it needs however to be mentioned
2021-10-01

At this point it needs, however, to be mentioned that most in vivo studies regarding the herein discussed nuclear receptors were performed in rodents, especially in mice. Due to the significant differences in metabolism in mice and humans, not all results are translatable between these species and h
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Phenformin The overall very satisfactory potency profile of
2021-10-01

The overall very satisfactory potency profile of compounds 7a–l suggests that 1,3,4-thiadiazole-2-carboxamide moiety was a suitable periphery group to add to the 3-phenylpropanoic Phenformin core in order to improve affinity to FFA1. The agonist activity in this series appears to be particularly sen
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We also wonder what function s both FPPS and
2021-10-01

We also wonder what function(s) both FPPS1 and FPPS2 genes had in leaf. As some research indicated that the alpha-farnesene was also detected in ripe leaf of crabapple (Malus sp.) (Wu et al., 2012), one or both of them may be related to the synthesis of alpha-farnesene in leaf. To our knowledge, the
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br Methods br Results br Discussion In the general
2021-10-01

Methods Results Discussion In the general population BNP has been established as a marker for DNQX disodium salt failure diagnosis. Moreover, there is growing evidence that elevated levels of natriuretic-peptides may improve CV risk prediction in the general population above traditional ris
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br Significance Cellular heterogeneity for phenotypic featur
2021-10-01

Significance Cellular heterogeneity for phenotypic features is a key mechanism underlying disease progression and therapeutic resistance, yet its regulation is poorly understood at the molecular level. Our findings demonstrate that endocrine resistance is associated with higher transcriptomic het
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br Acknowledgement The work was supported by the
2021-10-01

6. Acknowledgement The work was supported by the NSFC through Grant Nos. 11535016 and 11475232. It was also supported by CAS. The authors thank their collaborators for beneficial discussions and enthusiastic supports in the simulations and calculations. Introduction Hypoxia-inducible factors
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Mitochondrial binding by HK prevents mortality by inhibiting
2021-10-01

Mitochondrial binding by HK prevents mortality by inhibiting pro-apoptotic factor (Bcl-2 family)-mediated opening of the mitochondrial permeability transition pore (mPTP) (Arora and Pedersen, 1988, Calmettes et al., 2016, Kodde et al., 2007, Pedersen et al., 2002, Rosano, 2011, Schindler and Foley,
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