• As illustrated in Table monocyclic acid analogs were synthes

  2020-06-11

  

  As illustrated in Table 3, monocyclic 5(S),6(R)-7-trihydroxymethyl Heptanoate analogs were synthesized and evaluated. 2-Oxido-3H-1,2,3,5-oxathiadiazol analog 8 showed 15-fold less potent EP1 receptor affinity relative to 2b, while it showed 2.2-fold more potent antagonist activity. Oxadiazole-5-one

• Our previous work has demonstrated that two glutamate

  2020-06-11

  

  Our previous work has demonstrated that two glutamate residues (Glu-305 and Glu-331 in murine and human TPP II) in the active site are important for exopeptidase activity in mTPP II [17]. At least one of these, Glu-331, seems to form a salt bridge to the N-terminal amino group of the substrate, posi

• Herein in continuation of our

  2020-06-11

  

  Herein, in continuation of our interest in designing new DNA photocleavage agents [18], we report the synthesis, characterization and DNA binding and cleaving properties of a novel compound: trans-N,N-dimethyl-10,11-di(pyridin-4-ium)-10,11-dihydro-9,12-dioxobenzo[e]phenanthrene tetrafluoroborate (1)

• C598-0466 mg br Introduction br Sphingolipid metabolism Sphi

  2020-06-11

  

  Introduction Sphingolipid metabolism Sphingolipids, are fundamental constituents of all eukaryotic membranes and their metabolism is carried out by a broad array of anabolic and C598-0466 mg with ceramide as their hub (for a review, (Hannun and Obeid, 2018)). Ceramide can be formed by multiple

• br Criteria for ER targeted fluorescent probes

  2020-06-10

  

  Criteria for ER-targeted fluorescent probes Survey of fluorescent probes Proposed approach to high affinity fluorescent steroidal ER probes Our proposed approach to the development of a new generation of fluorescent estrogen receptor imaging agents employs many of the elements present in th

• In our previous research we have focused

  2020-06-10

  

  In our previous research, we have focused on the discovery of novel VEGFR-2 inhibitors as anti-angiogenesis agents. Numbers of biphenyl-aryl urea incorporated with salicylaldoxime including BPS-7 have been developed as potent and selective VEGFR-2 inhibitors (Fig. 3) [12], [13], [14], [15], [16], [1

• For the current studies we used the selective

  2020-06-10

  

  For the current studies, we used the selective Epac agonist 8CPT-AM to directly activate the proteins. We chose this pharmacological approach since it allows a direct activation of Epacs rather than using receptor agonists such as PGE2 which could introduce confounding variables. One potential conce

• While showing that deletion of EP

  2020-06-10

  

  While showing that deletion of EP1 maintains femur bone volume fraction and trabecular bone parameters during aging, perhaps more importantly we have also demonstrated that increased initial BV/TV in EP1 is protective against OVX-induced bone loss. That is, while mice lose an approximately equal pe

• Although DP technologies are convenient for users to

  2020-06-10

  

  Although 3DP technologies are convenient for users to manufacture devices automatically, the printing materials are inevitably limited by the manufacturers of 3D printers. Strategies are increasingly being developed to functionalize the raw printing materials or their printed devices with other phys

• Currently two approaches can be used individually or combine

  2020-06-10

  

  Currently, two approaches can be used individually or combinedly to overcome weak immunogenicity of subunit AKT inhibitor VIII (Bookstaver et al., 2018; Moyle, 2017; Vartak and Sucheck, 2016). The first is to design particulate antigens. Virus-like particles (VLPs), for example—mainly derived from

• br Molecular modeling simulation study Molecular modeling st

  2020-06-10

  

  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

• DDR is characterized by an N

  2020-06-10

  

  DDR2 is characterized by an N-terminal discoidin domain and a C-terminal kinase domain [7]. Characteristics of DDR1, which is a homologue of DDR2, have been extensively investigated in terms of expression level in cancer tissues and biological functions in normal and cancer cell conditions, but char

• In a recent study Tomkins et al analyzed

  2020-06-10

  

  In a recent study, Tomkins et al. [7] analyzed the protein-protein interaction network of ROCO proteins. Based on a database analysis, and only taking into account interactions reported in at least two peer-reviewed papers and/or confirmed by two different methods, 113 interactors were revealed for

• Of note CS associated lung injury is

  2020-06-10

  

  Of note, CS-associated lung injury is closely linked with augmented influx of macrophages that subsequently intensify the lung injury [34,47] while macrophage depletion alleviates CS-induced pulmonary inflammation via reducing cytokines and chemokine production in BALF [48]. Similar effect has been

• br Are incretins the only mediators of the

  2020-06-09

  

  Are incretins the only mediators of the anti-hyperglycaemic effects of DPP-4 inhibitors? Even though both GLP-1 and GIP were identified as substrates for DPP-4 early on [17], [19], [20], [22], and DPP-4 inhibition in vivo raises levels of the intact endogenous forms of both of them [43], [44], fr

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