• Our initial lead optimization started with

  2021-12-01

  

  Our initial lead optimization started with the modification of the indole head group as summarized in . Extensive exploration indicated that there was limited tolerance of structural change in this region of the molecule. All of the modifications to the indole moiety, including N-substitution (), li

• After initial optimization of the distances we obtained the

  2021-12-01

  

  After initial optimization of the distances we obtained the structure iG shown schematically in Fig. 1. This is the telomeric fragment of chromosome with the noncanonical structures of i-motif and G-quadruplex placed symmetrically in the middle of the duplex. Obviously, we consider the situation whe

• An important aspect of macrophage

  2021-12-01

  

  An important aspect of macrophage biology, highly influenced by HO-1 activity, is macrophage polarization. The broadest classification, based on the in vitro stimulation, surface marker expression, and inflammatory cytokines production, describes macrophages as classically activated, proinflammatory

• Introduction In the s nitric oxide NO was

  2021-12-01

  

  Introduction In the 1980s, nitric oxide (NO) was first characterized as critical to both innate immunity and endogenous signaling in animals [[1], [2], [3], [4], [5]]. NO was the first gaseous signaling molecule synthesized by animals to have its biochemical signaling pathway fully described [2]. P

• br Action of GPR in metabolically active tissues In addition

  2021-12-01

  

  Action of GPR55 in metabolically active tissues In addition to being highly expressed by discrete brain regions, as described in Section 2, GPR55 is also expressed in a wide range of peripheral tissues, including spleen, adrenals and bone (Sawzdargo et al., 1999, Ryberg et al., 2007, Whyte et al.

• br Discovery of GPR A The murine

  2021-12-01

  

  Discovery of GPR109A The murine niacin receptor, protein upregulated in macrophages by interferon-γ (PUMA-G), was identified as a G-protein-coupled receptor (GPCR) expressed in adipocytes and spleen [22], [23]. This finding suggested a role of this receptor in macrophage function [24]. In 2003, t

• So far GnRH receptors have been detected in the human

  2021-12-01

  

  So far, GnRH receptors have been detected in the human ovary, but their physiological importance is still unclear (). In particular, GnRH receptors as well as GnRH types I and II have been localized in the granulosa Torin1 of pre-ovulatory follicles, but not of follicles from the primordial to the e

• In the GLUT family glucose

  2021-11-30

  

  In the GLUT family, glucose transporter 1(GLUT1) is primarily responsible for basal glucose uptake and maintenance of glucose basal metabolism in cells (Olson and Pessin, 1996). High GLUT1 expression occurred in various types of human cancers, like brain tumor, lung cancer and esophageal cancer (Nis

• br Materials and methods br Results br Discussion Although h

  2021-11-30

  

  Materials and methods Results Discussion Although homologues of the β-galactosidase gene were known to exist in the Xenopus genome, and SA-β-gal activity has been detected in whole-mount Xenopus embryos by histochemical staining (Davaapil et al., 2017), no reports have been presented so far

• Among sensitizers tested in the previous study six test

  2021-11-30

  

  Among 22 sensitizers tested in the previous study, six test chemicals were pre- or pro-haptens (Nepal et al., 2018a). Among 6 chemicals, hydroquinone and 2-aminophenol, strong sensitizers, were falsely classified as non-sensitizers due to the lack of metabolic activation (Nepal et al., 2018a). Liter

• In the last years a plethora of studies overstepped the

  2021-11-30

  

  In the last years, a plethora of studies overstepped the classic concept of the ENS as purely modulator of GI secretion and motility, focusing on its potential as source of substances acting on immune cells and consequently involved in the control of local inflammatory events, as in the Inflammatory

• Target regulated the formation of

  2021-11-30

  

  Target-regulated the formation of G-quadruplex was used here to “kill two Nilvadipine with one stone” for the detection of melamine and I− with one probe DNA. G-quadruplexes are higher-order structures formed from G-rich oligonucleotides through the stacking of planar G-tetrads [43,44]. They have be

• The synthesis of compounds and were achieved according

  2021-11-30

  

  The synthesis of compounds and were achieved according to standard procedures. As shown in , The compound 4-methyl-1-(4-sulfobutyl)quinolonium () was prepared by alkylation reaction. Compounds and were synthesized by substitution reactions between 4-fluorobenzaldehyde and , , '-trimethylethanedi

• Another TKI used in cancer

  2021-11-30

  

  Another TKI used in cancer therapy is the Abl inhibitor imatinib mesilate which has also a beneficial effect on glucose homeostasis in diabetic humans [39], [40], [41]. Imatinib has a clear impact on NFκB activation and anti-apoptotic preconditioning of β-cells [39], attenuating islet inflammation [

• However at variance with the well studied R

  2021-11-30

  

  However, at variance with the well-studied R form of FBP1 which is flat, the R state of FBP2 is diametrically different, with a perpendicular orientation of the upper and lower dimers (Barciszewski et al., 2016). The cruciform-like R state of FBP2 is stabilized by a unique hydrophobic motif called ‘

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