• CC is a widespread disorder affecting up to of people

  2022-07-21

  

  CC is a widespread disorder affecting up to 20% of people worldwide, which also deteriorates the quality of life of patients and causes a substantial economic burden to society. There are 3 categories of CC: normal-transit constipation, slow-transit constipation and defecatory or rectal evacuation d

• Recently the spectrin cytoskeleton a deformable actin

  2022-07-20

  

  Recently, the spectrin cytoskeleton, a deformable actin-associated network, has been identified as a modulator of Yki function, potentially acting both apically and basally in different cell types [75•, 76•, 77•]. Several mechanisms have been proposed, including regulation via Crb/Ex tethering [], t

• Numerous strategies of cardiomyocyte protection are effectiv

  2022-07-19

  

  Numerous strategies of cardiomyocyte protection are effective in preclinical, animal models and in small clinical trials. However, most have disappointed in large clinical trials [4,5]. Failures of cyclosporine and post-conditioning to mitigate reperfusion injury are recent examples [[6], [7], [8]].

• Mice with GSTP knock out show

  2022-07-19

  

  Mice with GSTP1 knock out show increased risk of skin cancer when exposed to carcinogens like polycyclic aromatic hydrocarbons [23]. Most of the genetic association studies have focused on GSTP1 c.313G > A variant which results in isoleucine to valine substitution at amino minocycline hydrochloride

• br Introduction Excitatory pyramidal neurons are generated i

  2022-07-19

  

  Introduction Excitatory pyramidal neurons are generated in the cortical ventricular zone and migrate into the cortical plate alongside the radial glial processes (Chanas-Sacre et al., 2000, Hartfuss et al., 2001, Noctor et al., 2001, Rakic, 1972, Tan et al., 1998). Neuronal migration determines t

• R R MNF is a unique bitopic agent

  2022-07-19

  

  (R,R′)-MNF is a unique bitopic agent with selective and potent β2AR agonistic and GPR55 inhibitory properties [10], [11] that are independently associated with the drug's anti-mitotic and anti-tumorigenic actions. In 1321N1, U118MG, and melanoma cell lines, (R,R′)-MNF activation of the β2AR decrease

• br Concluding Remarks Given the increasing global incidence

  2022-07-19

  

  Concluding Remarks Given the increasing global incidence of metabolic disorders, new drugs that lower body weight and improve glucose tolerance are desperately needed. While we still have a long way to go, GPR55 might be an interesting target to explore, given its expression in numerous metabolic

• Growing evidence suggests that the glycine site seems to pla

  2022-07-19

  

  Growing evidence suggests that the glycine site seems to play a pivotal role in NMDAR-related function. For example, it lipid metabolism has been demonstrated in a hippocampal slice study that the glycine site sub-serves the spatiotemporal detection of synaptic activity (Li et al., 2009). Moreover,

• Ion dependence of mGluRs activity has been previously

  2022-07-19

  

  Ion dependence of mGluRs activity has been previously reported, notably to Ca2+ and Cl− (Kuang and Hampson, 2006). While mGlu1 and mGlu3 receptors were demonstrated to be sensitive to Ca2+, Cl− modulation was reported for all mGluRs, with a lesser extent for the mGlu2 receptor (DiRaddo et al., 2014;

• In respect of clinical development

  2022-07-19

  

  In respect of clinical development Takeda has pioneered the field with the GPR40 agonist TAK-875 or fasiglifam (Figure 2A), which in phase-II studies decreased HbA1c as efficiently as sulfonylurea without signs of hypoglycemia [24]. This was obtained with surprisingly little effect on systemic insul

• Tofacitinib Citrate Although encoded by a single gene GR dis

  2022-07-19

  

  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

• It is notable that pharmacological

  2022-07-19

  

  It is notable that pharmacological or genetic inhibition of GCGR signaling results in the engagement of a number of compensatory mechanisms that potentially impact glucose control. These include alpha-cell hyperplasia [2], [11], [12], [13] and increased beta-cell proliferation under low insulin cond

• The most ubiquitous serine threonine phosphatases

  2022-07-19

  

  The most ubiquitous serine/threonine phosphatases, such as PP1, PP2A, and PP2B are known to contribute to the majority of phosphatase activity in the heart [4]. Dysregulation of these and other PPs have been found in numerous CVDs, including heart failure (HF), and may play a critical role in reduce

• br Therapeutic approaches exploiting Cx function Due to thei

  2022-07-19

  

  Therapeutic approaches exploiting Cx43 function Due to their potential role in cancer metastasis, attempts have been made to alter connexin function to inhibit cancer growth. Therapeutic approaches include Cx43 peptide mimetics, Cx43 inhibitors, chemical agents capable of enhancing Cx43 function,

• br Introduction Alzheimer s disease AD

  2022-07-19

  

  Introduction Alzheimer's disease (AD) affects ca. 46 million people worldwide [1] and it is expected that the number will double or triple by 2030 or 2050, respectively, while no significant progress has been made in research for early diagnosis and new efficient therapies. Currently available me

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