• br STAR Methods br AMPK A Therapeutic Target

  2023-08-21

  

  STAR★Methods AMPK: A Therapeutic Target in the β Cell? Loss of pancreatic β cell function is a hallmark of the transition to a diagnosis of T2DM (see Glossary) 1, 2, 3, 4. AMPK activation has gained attention for the treatment of hyperglycemia in prediabetes as an insulin-sensitizing agent bec

• Last decade has provided a number of studies indicating that

  2023-08-18

  

  Last decade has provided a number of studies indicating that AhR signaling could play a role both in the development and in progression of multiple cancer types, with potential implications for cancer therapy (for review see (Kolluri et al., 2017; Murray et al., 2014)). Activation of AhR is consider

• br Mechanisms for regulation of intracellular cholesterol ho

  2023-08-18

  

  Mechanisms for regulation of intracellular cholesterol homeostasis Cells maintain intracellular free cholesterol levels and distribution within stringent tolerances by several mechanisms [55]: (1) uptake of native LDL (the major extracellular carrier of cholesterol) by LDL receptors and modified

• br Adiponectin receptors in colorectal cancer development AP

  2023-08-18

  

  Adiponectin receptors in colorectal cancer development APN receptors expressed in CRC tissue may mediate its effects on cell expansion and cell death (Byeon et al., 2010). It was observed that the expression of AdipoR1 and 2 is higher in CRC tissue than in counterpart healthy tissues (Williams et

• As an alternative to chronic receptor blockade we

  2023-08-18

  

  As an alternative to chronic receptor blockade, we have been targeting adenosine kinase (ADK) – an astrocyte-based enzyme that catalyses the phosphorylation of adenosine, as a means to modify 6656 synthesis adenosinergic signalling (Boison, 2006, Etherington et al., 2009). Up-regulating ADK facilita

• Since the introduction of zebrafish into the

  2023-08-18

  

  Since the introduction of zebrafish into the laboratory, many milestones have been achieved that firmly establish this organism as a prominent genetic model for biology and medicine. Many features make this species an organism of easy maintenance in laboratory which provides advantages to understand

• In conclusion we have demonstrated that diaryl pyrazolo

  2023-08-18

  

  In conclusion, we have demonstrated that ,-diaryl-1-pyrazolo[3,4-]pyrimidine-3,6-diamines represent a novel class of ACK1 inhibitors. The presence of a polar substituent at C-4 of the N-6 aryl ring was shown to be unnecessary for maintaining high levels of inhibitory activity. Furthermore, selectivi

• Anti LT therapy by LO inhibition has been

  2023-08-18

  

  Anti-LT therapy by 5-LO inhibition has been hampered by occurring liver toxicities by Zileuton or the clinical phase II compound Atreleuton [36], [37] However both compounds possess a thiophene as well as an N-hydroxyurea moiety. These features could be linked with reactive thiophene intermediates [

• Having established the structural requirements for potency

  2023-08-18

  

  Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vitr

• In our studies of leucine and BCH in pancreatic

  2023-08-18

  

  In our studies of leucine and BCH in pancreatic islets and clonal insulin cell lines, we noticed that leucine was a slightly stronger stimulant of insulin release. Previous studies showed that leucine can be metabolized to CO2[11], [12], [13], [14] and can increase acetoacetate in pancreatic islets

• Whole body loss of ACLY is early embryonic

  2023-08-18

  

  Whole-body loss of ACLY is early embryonic lethal, indicating that it serves non-redundant roles during development (Beigneux et al., 2004). Silencing or inhibition of ACLY suppresses the proliferation of many cancer cell lines and impairs tumor growth (Bauer et al., 2005, Hanai et al., 2012, Hatziv

• The evidence points toward a role

  2023-08-18

  

  The evidence points toward a role for 12/15-LO activity in WAT in modulating chronic local inflammation and subsequent systemic metabolic decline in the obese state. However, little is known as to the role of 12- and 15-LOs in BAT. Indeed, in addition to WAT, platelet- and leukocyte-type 12-LO are e

• Previous studies have demonstrated ATR inhibition is effecti

  2023-08-18

  

  Previous studies have demonstrated ATR inhibition is effective for treating cancers combining with chemotherapies in lung adenocarcinoma, gastric cancer, HER2 positive breast cancer and chronic lymphocytic leukemia Oleamide to enhance chemotherapy sensitivity [[16], [17], [18],[20], [21], [22]]. VE

• br Conclusion This is the first report to

  2023-08-18

  

  Conclusion This is the first report to show that treatment of lung cancer cell lines, A549 and H1299, with ovatodiolid stimulates intracellular reactive oxygen species generation and induces DNA damage. Subsequently activates ATM/ATR and CHK1/2 signaling pathway, inhibits CDC25C and p21WAF1/CIP1,

• As aforementioned this study aimed to

  2023-08-18

  

  As aforementioned, this study aimed to design, synthesize and investigate aromatase inhibitory and anti-breast cancer activities of N,N′-disubstituted thiourea derivatives. Based on the attractive phenotypic molecule 1, the synthetic N,N′-disubstituted thioureas have been designed including monothio

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