• A second advance came with the discovery that

  2021-06-19

  

  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

• ccr5 antagonist Inhibition of DHODH is reflected by an antip

  2021-06-19

  

  Inhibition of DHODH is reflected by an antiproliferative effect on peripheral blood mononuclear ccr5 antagonist (PBMCs), which can be measured by the inhibitory effect on their phytohemagglutinin (PHA) stimulated growth. The test was performed as described in the reference. Data for few selected co

• The p controls transcription of several genes that

  2021-06-19

  

  The p53 controls transcription of several genes that affect the release of cytochrome c in the mitochondrial apoptotic pathway [44]. In addition, p53 can induce a transcription-independent apoptosis through a direct interaction with the Bcl-2 family proteins [45]. However, the role of mitochondrial

• br Experimental procedures br Introduction Protein kinases r

  2021-06-19

  

  Experimental procedures Introduction Protein kinases represent one of the largest enzyme Fmoc-Cys(Trt)-ol in the human genome and act as signaling mediators in a variety of cellular processes (Manning et al., 2002). Because many diseases are associated with aberrant protein kinase activity, ta

• Introduction br CK in the Regulation of Hh Pathway CK

  2021-06-18

  

  Introduction CK1 in the Regulation of Hh Pathway CK1 was initially identified as a negative regulator of Hh signaling at the level of transcription factor Ci by genetic studies in Drosophila and genome-wide RNAi screen in Drosophila cultured tropisetron mg (Jia et al., 2005, Lum et al., 2003, P

• The modes of action of insecticides are classified by

  2021-06-18

  

  The modes of action of insecticides are classified by the Insecticide Resistance Action Committee (IRAC) [6]. In this classification, a large proportion of insecticides are categorized as nerve- and muscle-targeting insecticides, which encompass GABACl antagonists (Group 2) and GluCl allosteric modu

• In summary we have identified

  2021-06-18

  

  In summary, we have identified a series of amides as ERRγ agonists with suitable potency for further development. Our SAR studies of this chemotype identified SR19881 as the most potent full agonist of ERRγ with an EC=0.39 μM in a binding assay and an EC=4.7 μM in a cell-based assay. SR19881 was als

• Here we report for the first time that EphB

  2021-06-18

  

  Here, we report for the first time that EphB4 contains two NLS sequences and localises to the nucleus. This is mediated via an importin-α pathway and we show that EphB4 could potentially have a direct role in gene regulation. These data provide new insight into Eph receptor localisation and action a

• The role of Epac in the

  2021-06-18

  

  The role of Epac in the regulation of intracellular Ca homeostasis and contractility is still matter of debate. In rat adult cardiomyocytes, acute Epac stimulation decreased the amplitude of Ca transients [6], [9], [10] with either no changes [6] or increments [9] in cell shortening, suggesting an e

• Furan analogs and N methylpyrrole analogs had completely

  2021-06-18

  

  Furan analogs and N-methylpyrrole analogs had completely different SARs. For example, replacement of the furan-2-sulfonyl moiety of 6 with the furan-3-sulfonyl moiety resulted in 8 with a decreased EP1 Ubenimex affinity and an increased antagonist activity, while the corresponding chemical modifica

• br Introduction The protein Epidermal Growth Factor Receptor

  2021-06-18

  

  Introduction The protein Epidermal Growth Factor Receptor Tyrosine Kinase (EGFR-TK) play important role in non small-cell lung carcinoma (NSCLC) and vital therapeutic progress withinin the treatment of this ailment has revamped the past ten years through the exploitation of this insight (Mok et a

• Itch also known as astrophin interacting protein

  2021-06-18

  

  Itch, also known as astrophin-1 interacting protein-4 (AIP4), is a HECT domain-E3 ligase. It was discovered in 1998 in mouse coat color genetic studies which displayed the disruption caused by the Itch gene inducing a lethal autoimmune inflammatory condition. The substrates of Itch are transmembrane

• Modulating protein stability specifically inhibiting ubiquit

  2021-06-18

  

  Modulating protein stability, specifically inhibiting ubiquitin E3 ligases, provides potential advantages over other druggable targets given the presence of biochemically multiple, unique pharmacophores within complexes that can bind a variety of small molecules [12]. The FBXO3 inhibitors used here

• br Chemistry A total of new ThDP analogs in

  2021-06-18

  

  Chemistry A total of 35 new ThDP analogs in the series of 7, 12, 15, and 19 were designed and synthesized (Scheme 1). The synthetic route is simple and convenient. In this synthetic route, 4-amino-2-methylpyrimidine-5-carbaldehyde 3 is a key intermediate for the synthesis of title compounds 7, 1

• galactoside Dihydrofolate reductase DHFR is an excellent mol

  2021-06-17

  

  Dihydrofolate reductase (DHFR) is an excellent molecular target for this study because it has been and is currently studied by using different molecular modeling techniques [6], [7], [8], [9]. Kerrigan et al. have reported an interesting review about recent progress in molecular dynamics simulations

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