• Currently the computational chemical biology has been applie

  2022-07-06

  

  Currently, the computational chemical biology has been applied in hepatitis B antiviral drug discovery research [18]. Tan et al. explored oxime ethers as HBV inhibitors by docking and screening [19]. Allen et al. clarified the resistance of HBV to the nucleoside drug lamivudine [20]. The results sug

• br Discussion Using HBV transgenic mice Kim

  2022-07-06

  

  Discussion Using HBV transgenic mice, Kim, et al. first reported that the HBx gene caused HCC [34]. Since then, transgenic mice have become a useful experimental model for defining the molecular events of HBV hepatitis, and HBV-related hepatocarcinogenesis. In the present study, we first confirme

• These agents can be divided

  2022-07-06

  

  These agents can be divided into three categories based upon the therapeutic agent conjugated to the antibody; the most frequently explored are ADCs using a cytotoxic agent to be delivered directly to the tumor site. The second class has not been broadly used and consists of radionucleotides (Wong e

• br Conclusion In this report we describe the synthesis and

  2022-07-06

  

  Conclusion In this report, we describe the synthesis and evaluation of oxadiazole-based GSK3 inhibitors. Occupation of the ATP-binding pocket in its entirety led to the identification of several potent and selective compounds. These compounds are characterized by IC50 values in the low nanomolar

• br Introduction Prostate cancer is the most commonly diagnos

  2022-07-06

  

  Introduction Prostate cancer is the most commonly diagnosed cancer and the second leading cause of cancer deaths in men in the United States, accounting for about 30,000 cancer deaths annually [1]. Epidemiological studies that show geographical variations in prostate cancer incidence and mortalit

• Linezolid As a part of our continuing

  2022-07-06

  

  As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here

• The lactam compounds including ceftriaxone CEF have shown

  2022-07-06

  

  The β-lactam compounds, including ceftriaxone (CEF), have shown to attenuate drug-seeking in several drugs of abuse including methamphetamine [31], cocaine [32,33], nicotine [34] and morphine [35]. Moreover, in our laboratory, we have shown that CEF can reduce chronic alcohol drinking via upregulati

• Guanethidine Sulfate LbGlcK and the HsHxKIV d glucose comple

  2022-07-06

  

  LbGlcK and the HsHxKIV-d-glucose complex (PDB entry 3IDH) [17] were superimposed from individual subunits. The active site regions revealed the key Guanethidine Sulfate binding residues to be present for LbGlcK; also, the superposition showed that HsHxKIV had residues that were absent in LbGlcK, suc

• Immunohistochemistry analysis shown ghrelin and GHSR a

  2022-07-06

  

  Immunohistochemistry analysis shown ghrelin and GHSR-1a immunostaining was located in the epithelial cells of Fmoc-Val-OH and ducts throughout the lactation, strong immunoreactive cells were detected in L30, L60 and L120 stage. The distribution of ghrelin has been shown in many tissues, including ma

• Lenvatinib is an orally available multi targeted tyrosine ki

  2022-07-05

  

  Lenvatinib is an orally available, multi-targeted tyrosine kinase inhibitor against VEGFR1–3, FGFR1–4, PDGFRα, RET, and KIT [11,12]. In a recent phase III trial for patients with previously untreated uHCC (REFLECT study), lenvatinib showed statistical non-inferiority of overall survival compared to

• The activation of GPR FFA signaling

  2022-07-05

  

  The activation of GPR40/FFA1 signaling triggers the PLC/PIP2 signaling pathway and results in Ca2+ release from the endoplasmic reticulum (ER). Increased Ca2+ levels may lead to activation of different protein kinases, such as Ca2+/calmodulin-dependent protein kinase type IV, Akt, extracellular sign

• The IN gene of the HIV isolate from Papua

  2022-07-05

  

  The IN gene of the HIV isolate from Papua (CRF01_AE isolate) contains genetic polymorphisms (Fig. 1A) that encode for variant amino acids in the IN protein, based on the Stanford HIVdb mutation interpretation database (Fig. 1B). These variations slightly changed the three-dimensional structure of IN

• Finally worth of mention are few papers

  2022-07-04

  

  Finally, worth of mention are few papers that report on the discovery of HO-2 selective inhibitors. In 2013, starting from the screening of a Florfenicol mg library, the above-mentioned Canadian research group identified Clemizole (Table 6) as a new hit compound for the development of the first seri

• PRL-3 Inhibitor Based on pharmacophore modeling a good HDAC

  2022-07-04

  

  Based on pharmacophore modeling, a good HDAC inhibitor has at least three sides/regions: the attachment side of the Zn2+ cofactor/HDAC active site (Zn2+ binding group/ZBG), hydrophobic cap (CAP) and linker containing connecting unit (CU) with electronegative groups (Mohan et al., 2011, Rossi et al.,

• h2 agonist Recently some published studies showed that

  2022-07-04

  

  Recently, some published studies showed that HBV can induce autophagy in vitro and vivo [[19], [20], [21]]. The critical role of autophagy in HBV normal life cycle, such as HBV envelopment, has been gradually accepted by researchers from different laboratories [22,23]. HBV can trigger the autophagic

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