• The excellent potencies selectivities and improved PK associ

  2024-05-17

  

  The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This

• Adiponectin is an adipokine whose circulating level is deple

  2024-05-17

  

  Adiponectin is an adipokine whose circulating level is depleted in a number of metabolic diseases including insulin resistance, diabetes and cancer (Khan et al., 2015, Singh et al., 2014a, Singh et al., 2014b, Yamauchi et al., 2014). Despite its importance in health and pathophysiology, adiponectin

• br New AMPK activators Fenofibrate

  2024-05-17

  

  New AMPK activators Fenofibrate is a drug of the fibrate class used for the treatment of dyslipidemia [53] but is also an agent that could alleviate DN-induced alterations through AMPK activation (Fig. 2). Streptozotocin-induced diabetic rats treated with fenofibrate improved in not only renal fu

• br Introduction Myasthenia gravis MG is an autoimmune diseas

  2024-05-17

  

  Introduction Myasthenia gravis (MG) is an autoimmune disease characterised by failure of transmission at the neuromuscular junction (NMJ). In 80–85% of myasthenia gravis patients, the disease is mediated by antibodies to the nicotinic Obeticholic Acid receptor (AChR; (Lindstrom et al., 1976). Ma

• Two patients developed diffuse mesangio proliferative glomer

  2024-05-17

  

  Two patients developed diffuse mesangio-proliferative glomerulonephritis (DMPG) postoperatively, presenting as nephrotic syndrome and benign haematuria, respectively. DMPG has been reported in an adult patient with thymomatous MG following thymectomy [35], and various types of glomerulonephritis hav

• br Clinical realities br Commentary on

  2024-05-17

  

  Clinical realities Commentary on uses of selective 17,20 lyase inhibitors If continued monitoring of these same parameters along with tracking of circulating ACTH in human trials confirms these new drugs are the long sought after 17,20 lyase inhibitors, then we may for the first time be able t

• From an historical perspective ligands for

  2024-05-16

  

  From an historical perspective, ligands for GPCRs (adrenaline, serotonin, lamotrigine receptor or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenous li

• The following are the supplementary data related

  2024-05-16

  

  The following are the supplementary data related to this article. Competing interest Ethics approval and consent to participate Authors' contributions Acknowledgements The authors thank Dr. D. R. Kaplan for kind advice and materials derived from NB primary cell lines, Dr. F. D. Miller f

• Earlier studies with SERMs identified

  2024-05-16

  

  Earlier studies with SERMs identified that distinct chemical scaffolds have the ability to induce unique conformational changes in the ER, resulting in interaction with different cofactor subsets. The same has been demonstrated with SARMs, which induce distinct conformational changes compared to tes

• MAPs require divalent transition metal ions as cofactors for

  2024-05-16

  

  MAPs require divalent transition metal ions as cofactors for activity [21]. Previous studies on MAPs from different organisms indicate cobalt ions to be the most preferred divalent metal activator [22]. However, MAPs also exhibit activity with other divalent cations like Mn(II), Ca(II), Ni(II) or Fe

• To date defining the prognostic

  2024-05-16

  

  To date, defining the prognostic impact of molecular drivers of early-stage NSCLC has been challenging due to the relative rarity of these subsets and the redefinition of comparator arms over time as understanding of the molecular drivers of NSCLC evolved. Indeed, use of molecularly heterogeneous co

• br Conclusion br Conflict of interest

  2024-05-16

  

  Conclusion Conflict of interest Acknowledgments We thank Nancy Kerkvliet for helpful advice. The research in the lab of CE and THS is supported by the Deutsche Forschungsgemeinschaft (grants ES103/7-1 and 9-1, HA7346/2-1). We apologize to all authors whose work could not be cited due to lim

• To validate the identified phosphorylation sites in

  2024-05-16

  

  To validate the identified phosphorylation sites in the mouse heart, we analyzed HEK 293T monobenzone transfected with Adrb1 based on the hypothesis that protein residues phosphorylated both in vivo and in vitro are more likely to be physiologically relevant. All of the phosphorylation sites identi

• Renal cell carcinoma RCC accounts for more than cancer

  2024-05-15

  

  Renal cell carcinoma (RCC) accounts for more than 12,000 cancer deaths in the United States (Jemal et al., 2003). The current treatment includes surgical resection followed by interleukin-2 or Interferon-α treatment. Some patients experience distant metastatic lesions of RCC. In the last 5 years, re

• Starting with commercially available or nitropyrazole carbox

  2024-05-15

  

  Starting with commercially available 4- or 5-nitropyrazole-3-carboxylic acid, anilides containing nitro, amino or methylsulfonamido were synthesized. Here, manipulation of the substituents on the pyrazole ring was conducted after the anilide formation (). The rad51 of the nitro group was performed

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