• Finally we find that in the absence

  2022-08-04

  

  Finally, we find that in the absence of Aurora B, Sgo1 is delocalized from centromeres and found along chromosome arms, as reported after depletion of Bub1 (Kitajima et al., 2005, Riedel et al., 2006). The increased arm cohesion observed in the absence of Aurora B activity is dependent on the presen

• Protein structures determined in high resolution by X

  2022-08-04

  

  Protein structures determined in high resolution by X-ray crystallography and NMR techniques provide wealth of structural information on intra-domain and inter-domain protein interactions of small sized proteins. In addition, cryo-EM often provides low resolution structures of multi-component protei

• Accessibility and physico chemical features

  2022-08-04

  

  Accessibility and physico-chemical features of cysteine residues define their redox-reactivity and the 3-dimensional structure of GSNOR allows to identifying such surface-exposed, redox-sensitive cysteine residues. GSNOR crystal structures are available from human (Protein Data Bank code: 1MP0), tom

• br Brief overview of GSK inhibitors We

  2022-08-04

  

  Brief overview of GSK-3 inhibitors We will briefly summarize some of the key aspects about GSK-3 inhibitors. Additional details of GSK-3 inhibitors in clinical trials have been recently reviewed [5]. GSK-3 is a complicated target as it is involved in many biological processes from neurology, diab

• BAPTA-AM Starting from commercially available dioxaspiro dec

  2022-08-04

  

  Starting from commercially available 1,4-dioxaspiro[4.5]decan-8-ol, was prepared by the synthetic sequence illustrated in . Aromatic nucleophilic substitution of 1,4-dioxaspiro[4.5]decan-8-ol, followed by an BAPTA-AM catalyzed deprotection efficiently gave . A - enriched mixture of (/=∼3/2) was o

• Consistent with previous reports of

  2022-08-04

  

  Consistent with previous reports of an association between increased accumulation of cAMP and GLP-1 secretion [25, 44, 45], we hypothesized that Oleoyl-LPI may regulate GPR119 activation and secretion of GLP-1 secretion through the cAMP/PKA/CREB pathway. Pharmacological inhibition of PKA by H-89 was

• Of the patients that presented a CD dip with no

  2022-08-04

  

  Of the 11 patients that presented a CD4 dip with no cause identified other than HIV-infection, 9 had CD4 counts >200 cells/μL in the next measurement and all experienced the event during the first 24 months of follow-up. Intra-laboratory measurements and individual patient physiologic factors also i

• Compared to methadone or morphine buprenorphine

  2022-08-04

  

  Compared to methadone or morphine, buprenorphine is a partial mu-opioid agonist, which shows high affinity for, and slow dissociation from, mu-opioid receptors. This maintenance of homeostasis may help to counter the development of an overt withdrawal syndrome, and may explain the lower risk of deve

• In vertebrates three cognate receptors or receptor like

  2022-08-04

  

  In vertebrates, three cognate receptors or receptor-like sequences have been identified with distinct distributions and functions (Millar, 2005, Neill et al., 2001). Only two types of GnRHR occur in mammals, though (Morgan and Millar, 2004). The mammalian type I GnRHR shares over 80% amino Silodosin

• Based on the role of NMDA receptors in

  2022-08-04

  

  Based on the role of NMDA receptors in initiation and propagation of epileptic seizures and on potentiation of NMDA function by glycine, it has been hypothesized that glycine will have proconvulsant activity (Foster and Kemp, 1989). Indeed, there is some evidence that human epileptogenic foci, remov

• Based on work from our

  2022-08-04

  

  Based on work from our labs with mGlu NAMs, and the ability of [3.3.0] systems, such as the octahydropyrrolo[3,4-]pyrrole, to effectively mimic piperazines, we focused our attention on the potential bioisoteric replacement of the [3.1.0] system of and , as well as the piperidine of , with a [3.3.0]

• Although encoded by a single gene

  2022-08-03

  

  Although encoded by a single gene, GR displays considerable heterogeneity through the combined effects of alternative mRNA splicing, alternative translation initiation, and complex post-translational modification. Differential expression of the various GR isoforms may contribute to tissue-specific f

• br The GLI code The

  2022-08-03

  

  The GLI code The GLI code model [21], [22] considers the total GLI function as a balance of positive activator (GLIA) and negative repressive (GLIR) activities with GLI1 being mostly a positive transcription factor and GLI3 mostly a transcriptional repressor. The GLIA:GLIR ratio is thus critical,

• Herein we describe the design

  2022-08-03

  

  Herein, we describe the design and optimization of fused-ring phenyl propanoic acids as novel GPR40 agonists, leading to the discovery of compound 40a which exhibits excellent pharmacokinetic properties, improved hepatobiliary transporter inhibition, and significant glucose-lowering efficacy during

• Contrary to the transient nature

  2022-08-03

  

  Contrary to the transient nature of signal transmission through PLCβ, genome-wide RNAi screens revealed that the signaling events driven by Gαq that result in aberrant cell proliferation depends on highly specific protein-protein interactions, rather than solely on diffusible second messenger system

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