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br GPCRs form heterotetramers In
2019-11-14
GPCRs form heterotetramers In addition to homodimers and heterodimers, for several family A receptor heteromers, experimental evidence supports the presence of higher order rearrangements as tetrameric structures, comprised of two different homodimers, each able to signal with its preferred G pro
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br Introduction Addiction to opioids such as morphine is a
2019-11-14
Introduction Addiction to opioids such as morphine is a chronic disorder that affects the mesocorticolimbic dopaminergic pathway in the brain. Activation of the pathway ultimately leads to dopamine release in the nucleus accumbens (NAc) (Di Chiara et al., 1998) and stimulation of dopamine recepto
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br Molecular modeling simulation study Molecular modeling st
2019-11-13
Molecular modeling simulation study Molecular modeling study was performed through docking of the test compounds into the binding site of hDHFR enzyme using Discovery Studio 2.5 software. Computational docking is an algorithm designed to determine the suitable position and the orientation of the
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br DDR receptor and MMP expression Type II
2019-11-13
DDR2 receptor and MMP-13 expression Type II collagen protein in articular cartilage is highly stable structure as its half-life is 117 years [43]. The chondrocytes have limited ability to synthesis type II collagen protein in the matrix of mature articular cartilage once the collagen gets disrupt
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From materials science it is known that the
2019-11-13
From materials science, it is known that the differences in the annealing temperature is the main factor that mostly influences La (Takai et al., 2003, Cançado et al., 2006). In analogy, controlling the pyrolysis temperature and neurotensin receptor during residues burning might be a key aspect to r
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In our former work our interest was in discovery of
2019-11-13
In our former work, our interest was in discovery of novel VEGFR-2 inhibitors as anti-angiogenesis agents. Along this line, with natural alkaloid taspine as the lead compound, rounds of structure optimization were performed to develop novel VEGFR-2 inhibitors [[13], [14], [15]]. Among them, BPS-7, b
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Consistent with the known tolerance of the Suzuki
2019-11-13
Consistent with the known tolerance of the Suzuki–Miyaura reaction to a wide range of aryl substituents, we subsequently found that the commercially available 3-hydroxyphenylboronic N6022 pinacol ester () could be coupled to , to give directly and in comparable yield. Smooth conversion of into w
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A second advance came with the discovery that conformational
2019-11-13
A second advance came with the discovery that conformationally-flexible benzamide analogs having an N-phenylpiperazine moiety possessed good affinity and modest selectivity for D3 versus D2 receptors [3,[14], [15], [16]]. This observation spawned a significant effort by medicinal chemists to develop
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Indeed some studies that examined the morphine
2019-11-12
Indeed, some studies that examined the morphine response have reported that the (C) allele of rs4818 was associated with a low dose administered compared to that given for individuals with the (G) allele (Rakvag et al., 2008). In a publication about Tunisian patients with cancer by Chatti et al. (2
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In vitro studies in NSCLC cell lines expressing
2019-11-12
In vitro studies in NSCLC cell lines expressing EGFR mutants (T790M mutation, exon 19 deletion E746-A750, L858R/T790M double mutation), demonstrated that Rociletinib potently inhibits proliferation in the mutant EGFR NSCLC mk-801 with Growth inhibition (GI50) values ranging from 7 to 32 nmol/L. In
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br Acknowledgements The authors are supported by
2019-11-12
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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Classical DHFR inhibitors such as methotrexate MTX bind tigh
2019-11-12
Classical DHFR inhibitors such as methotrexate (MTX) bind tightly to the enzyme and possess adequate clinical pharmacokinetics. MTX bind to the DHFR binding site through the formation of hydrogen bonds with Asn64, Lys68, Arg28, Arg70, Val115 and Ile7 amino BMS 195614 residues as well as hydrophobic
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Arsenic could cause apoptosis in both
2019-11-12
Arsenic could cause apoptosis in both benign and malignant cells (Akao et al., 2000, Gupta et al., 2003, Namgung and Xia, 2001). However, at present, little is known about the consequences of arsenic-treated urothelial cells in autophagy and expression of its related proteins. In addition, the alter
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In conclusion our work provides the preclinical
2019-11-12
In conclusion, our work provides the preclinical evidence showing the potent in vivo efficacy of AT7519 on chemoresistant cancer 7867 mg and its underlying mechanisms of action. Our work supports the biological rationale behind the clinical trials initiated with AT7519, particularly for the treatmen
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Self Determination Theory SDT as described by Ryan
2019-11-12
Self-Determination Theory (SDT), as described by Ryan and Deci (2000) is “an approach to human motivation and personality that uses traditional empirical methods while employing an organismic metatheory highlighting the importance of humans\' evolved inner resources for personality development and b
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