• Estrogen treatment in postmenopausal women requires

  2021-03-10

  

  Estrogen treatment in postmenopausal women requires combination with a progestogen in order to prevent endometrial stimulation. This is not necessary, however, with tibolone as progestogenic activity is associated with its Δ4-metabolite that is formed in the liver, as well as locally in the endometr

• br Declaration of conflicting interests br Funding

  2021-03-10

  

  Declaration of conflicting interests Funding The author(s) disclosed receipt of the following financial support for the research, authorship, and/or publication of this article: This work was supported by CT Stem Cell grant # 15-RMB-YALE-07 (to L.E.N), and by an unrestricted Research Gift from

• br Cytochrome P monooxygenases Cytochrome

  2021-03-10

  

  Cytochrome P450 monooxygenases Cytochrome P450 monooxygenases (P450s) belong to one of Nature’s most versatile group of enzymes for C–H functionalization and are able to perform challenging regioselective and stereoselective activations of remote, unactivated C(sp3)–H bonds, for which there are o

• br Conflict of interest statement br Introduction

  2021-03-10

  

  Conflict of interest statement Introduction Endothelins (ETs) are a family of multifunctional, naturally occurring peptides with long-lasting vasoconstrictor and pressor effects (Zhou et al., 2004). They are synthesized as a large protein, the pre-proET-1 or Big ET-1, which is subsequently cle

• Our data also showed that D dopamine

  2021-03-09

  

  Our data also showed that D2 dopamine receptor was down-regulated in the hippocampus, NAc and striatum of F1-MEP animals, which was only significant in the hippocampus. Both agonists and antagonists of D2 dopamine receptor are able to decrease heroin self-administration (Hemby et al., 1996; Rowlett

• For example nM MTX markedly stimulates the differentiation o

  2021-03-09

  

  For example, 200nM MTX markedly stimulates the differentiation of the monocytic U937 Fluconazole [39], but only 10nM MTX is sufficient for the inhibition of clonogenicity in the ALL and APL cell lines [22]. Furthermore, an even lower concentration of MTX (2nM) selectively induces the expression of

• Beside the previously reported Topo I

  2021-03-09

  

  Beside the previously reported Topo I inhibition, time and concentration dependent CRM1 inhibitory properties of klavuzon derivatives have been shown as a second mechanism of action in this work. Especially, compounds 3 and 20 are the most effective derivatives and they completely inhibit CRM1 acti

• Although differences in several nociceptive

  2021-03-09

  

  Although, differences in several nociceptive tests have previously been described across strains (Mogil et al., 1999), it is the first time that pain sensitivity in response to chemical and thermal stimuli has been evaluated in B6,129CRHtklee mice. Our results showed no differences in pain sensitivi

• Similar to Bdnf acute administration of RG did

  2021-03-09

  

  Similar to Bdnf4, acute administration of RG108 did not alter gene expression of Gria1 and Hdac2, despite their relevance for the task. Gria1 belongs to the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic Nitecapone receptor receptor (AMPAR) family that is known to be crucial for LTP and the streng

• Clozapine synthesis br Conclusions br Acknowledgements This

  2021-03-09

  

  Conclusions Acknowledgements This work was supported by funding from the Natural Sciences and Engineering Research Council of Canada (RGPIN-2017-06346 to JB), National Institute of Child Health and Human Development (5R01HD083930-02 to JB), and the National Institute of Biomedical Imaging and

• N Cyclopentylmethyl analog exhibited fold less potent recept

  2021-03-09

  

  N-Cyclopentylmethyl analog 25 exhibited 2.3-fold less potent receptor affinity and 1.6-fold less potent antagonist activity. Among the compounds tested, the N-isobutyl analog 23 showed the most potent EP1 receptor affinity and antagonist activity. In summary, a series of 4-( 2-[alkyl(phenylsulfonyl

• The present study intended to characterize the predominant c

  2021-03-09

  

  The present study intended to characterize the predominant cholinesterasic form found in tissues of three tropical fish species, namely Phalloceros harpagos Lucinda, 2008 (common name guaru), Pterygoplichthys pardalis Castelnau, 1855 (common name cascudo) and Astyanax altiparanae Garutti and Britski

• The mechanisms by which coregulators control the

  2021-03-09

  

  The mechanisms by which coregulators control the actions of estrogen receptors are still a topic of ongoing research. From studies in cancer cells, we have learned that a large group of coregulators have specific structural motifs that than affect their contact with ER ligand-binding domains (Heery

• papain br Materials and methods br

  2021-03-09

  

  Materials and methods Results Discussion This study demonstrates that various progestogens combined with E2 had different effects on breast cell growth. These effects had an inverse correlation with the changes of the PRA/PRB ratio. E2's antiapoptotic effects on MCF-7 papain may be related

• Emphysema is an important component of COPD which is

  2021-03-09

  

  Emphysema is an important component of COPD, which is responsible for airflow limitation. In the present study, a significant airspace enlargement was observed 21 days after elastase administration. Interestingly, daily administration of olaparib provided greater protection against emphysema as comp

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