• Theoretically the majority of resistance mechanisms identifi

  2021-11-26

  

  Theoretically, the majority of resistance mechanisms identified so far could be targeted by compounds that are already available, such as inhibitors of ER, PIK3CA/mTOR or FGFR1. However, the potential therapeutic advantage of combining these agents with standard HER2-targeting treatments must be wei

• Whereas Sororin is dispensable in

  2021-11-26

  

  Whereas Sororin is dispensable in the absence of Wapl [14], overexpressed Haspin only partly supports cohesion in Sororin-depleted cells. Thus, although Haspin and Sororin have functional similarities, they are not fully redundant at the centromere. Haspin may have a mitosis-specific role in maintai

• Introduction Soluble guanylyl cyclase sGC is a key protein i

  2021-11-26

  

  Introduction Soluble guanylyl cyclase (sGC) is a key protein in the regulation of multiple physiological functions in mammalian physiology [1,2]. Upon stimulation by nitric oxide (NO) [3], sGC generates cyclic guanosine monophosphate (cGMP) from guanosine-5′ triphosphate and activates protein kina

• The gsnor ko plants contain elevated

  2021-11-26

  

  The gsnor-ko plants contain elevated amount of low and high molecular weight S-nitrosothiols (SNO) indicating that GSNOR activity controls the level of both GSNO and indirectly protein-SNOs [13], [17], [18]. GSNOR deficiency has been shown to cause pleiotropic plant growth defects, impaired plant di

• br Endogenous and synthetic ligands of GPR There are current

  2021-11-26

  

  Endogenous and synthetic ligands of GPR55 There are currently limited commercially available synthetic agonists and antagonists that are specific for GPR55. A large number of studies have investigated the pharmacology of GPR55 4, 23, 25, 30, 31, 32, 33, 34, 35, with contradictory findings reporte

• br Introduction Lichen forming fungi LFFs have evolved

  2021-11-25

  

  Introduction Lichen-forming fungi (LFFs) have evolved in various classes, including Arthoniomycetes, Coniocybomycetes, Dothideomycetes, Eurotiomycetes, Lecanoromycetes, Leotiomycetes and Lichinomycetes, in Ascomycota (James et al., 2006, Schoch et al., 2009a, Lumbsch and Rikkinen, 2017, Prieto et

• Polymerisation of HbS initiates the clinical

  2021-11-25

  

  Polymerisation of HbS initiates the clinical complications of SCD (Bunn and Forget, 1986). The resulting sequelae are multiple and diverse, and their individual impact on pathogenesis is difficult to elucidate. Early changes include altered red cell membrane permeability (Gibson and Ellory, 2002, Le

• br Concluding remarks In this small material of

  2021-11-25

  

  Concluding remarks In this small material of thirteen pituitary tumors of various kinds, we could not run statistical analysis. However, with a follow-up period of up to five years, we show that Disclosure Statement Acknowledgments Introduction Galanin is a 29/30-residue neuropeptide fo

• Somatostatin analogues are among the first

  2021-11-25

  

  Somatostatin analogues are among the first peptide-based drugs used in cancer imaging and therapy (for review see Reubi, 2003). Treatment of tumors by the use of peptide analogues labeled with cytotoxic agents acting via specific receptors is also under investigation for neuropeptide Y (Koglin and B

• Reports described a range of synthetic

  2021-11-25

  

  Reports described a range of synthetic GPR40 agonists with desirable safety and efficacy profiles, compared with existing antidiabetic therapies such as insulin and sulfonylureas [[20], [21], [22], [23], [24], [25], [26], [27], [28]]. Among them, several small molecules were tested in the clinical t

• The objective of this study is to design

  2021-11-25

  

  The objective of this study is to design and synthesize drug-like molecules with agonistic activity on both receptors; PPARγ and FFAR1. These agents would act as insulin sensitizers and insulin secretagogues through their action on PPARγ and FFAR1, respectively. The design of drugs with dual mode of

• Considering the fact that NADPH oxidase

  2021-11-25

  

  Considering the fact that NADPH oxidase is the main source for paraquat and maneb-induced oxidative stress, we hypothesized that NADPH oxidase activation might contribute to dopaminergic neurodegeneration induced by paraquat and maneb through ferroptosis. To test our hypothesis, we investigated the

• A second site of histone core domain acetylation that that

  2021-11-25

  

  A second site of histone core domain acetylation that that has been observed on newly synthesized histones is histone H4 lysine 91 [34]. H4 lysine 91 lies along the interface between the H3/H4 tetramer and the H2A/H2B dimers. In fact, H4 lysine 91 normally forms a salt bridge with an aspartic Y 134

• br Conclusion Our data allow pharmacological discrimination

  2021-11-25

  

  Conclusion Our data allow pharmacological discrimination of diverse of H3 ezh2 inhibitor antagonists that can be linked to their differential efficacy in preclinical and clinical disease settings (Fig. 6). Moreover, we identify the sigma-1 receptor as a common “off target” for H3 antagonists, and

• Importantly the regulation of the Hippo

  2021-11-25

  

  Importantly, the regulation of the Hippo pathway by metabolic networks, such as by glycolysis39, 40, hexosamine biosynthesis41, 42, and mevalonate synthesis43, 44, as well as by nutrient-sensing pathways including AMP-activated protein kinase (AMPK) 40, 45, 46 and mTOR 47, 48, 49, 50, was recently d

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