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br Modulators of the GUCY C cGMP PDEs signaling
2022-03-03
Modulators of the GUCY2C/cGMP/PDEs signaling pathways for CRC prevention and therapy (pre-clinical and clinical development) Several modulators of the GUCY2C/cGMP/PDEs signaling pathways, including GUCY2C agonists and PDEs inhibitors, have been developed and explored as chemopreventive agents for
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Paxilline Although resembling a differential symbiotic relat
2022-03-03
Although resembling a differential symbiotic relationship, interplay between prostate tumour CAFs promotes PKM2/HIF-1-driven transcriptional regulation in prostate cancer cells that exploit lactate produced by CAFs and undergo epithelial-to-mesenchymal transition (EMT) [21]. Although recent observat
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The saturated carbocyclic derivatives pyrazoles M
2022-03-03
The saturated carbocyclic derivatives, pyrazoles (2.5μM and 5.2μM) and (9.0μM and 2.5μM), provided little improvement in potency when compared to the linear alkyl derivatives, whereas the C5-phenyl derivative (0.31μM and 0.43μM) showed promise as a scaffold for further structural modifications.
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CD binding to gp causes a large scale
2022-03-03
CD4 binding to gp120 causes a large scale conformational change of gp120 which involves the gp120 core structure and the transitions of inner-domain layers (layer 1, 2 and 3), but also involves the movement of the major loops (V1, V2 and V3) [16], [17], [18], [19]. For instance, the V2-loop joins th
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br Methods and materials br Acknowledgements The authors tha
2022-03-03
Methods and materials Acknowledgements The authors thank the NIH AIDS Reagent Program for providing the materials and reagents. The HIV-1 1084i envelope gene was a generous gift from Dr. Charles Wood. This work was supported in part by grants to S.-H. X. from the Bill and Melinda Gates Foundat
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The timing and growth of follicles relative to follicle
2022-03-03
The timing and growth of follicles relative to follicle deviation was assessed in 49 cows (Fig. 4) that had NFWE following treatment onset and that had not already established dominance. Because day of deviation did not differ due to treatment, day of estrous cycle, or replicate, data are presented
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NEIL interacts with many DNA replication proteins
2022-03-03
NEIL1 interacts with many DNA replication proteins including flap-endonuclease 1 (FEN-1), proliferating cell nuclear antigen (PCNA), and Werner RecQ helicase (WRN) through its disordered C-terminal part. One study showed that in in vitro condition, NEIL1 binds to the damaged latrunculin a receptor
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Fatty acids have been repeatedly shown
2022-03-03
Fatty acids have been repeatedly shown to increase the responsiveness of pancreatic islets to glucose both in vitro and in vivo[6]. The recent identification of GPR40 as a receptor for free fatty acids that is localized to the pancreatic islet cells has therefore stimulated interest in obtaining sma
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br SMO antagonists pitfalls and limitations The first
2022-03-02
SMO antagonists: pitfalls and limitations The first Hh inhibitor discovered was cyclopamine, a naturally occurring alkaloid isolated from Veratrum californicum[21], which inactivates SMO by directly binding to its hepathelical bundle. Nevertheless, cyclopamine has shown several limitations as a d
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Here we examined whether complete ablation
2022-03-02
Here, we examined whether complete ablation of GIP production could reduce weight gain in the absence of the adipocyte hormone leptin, a condition that results in extreme hyperphagia, obesity, hyperinsulinemia, and insulin resistance, in both mice [24] and humans [25]. We found that Lepob/ob mice be
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br Contributions br Acknowledgements This research was
2022-03-02
Contributions Acknowledgements This research was supported by Natural Sciences and Engineering Research Council (NSERC) Discovery grant No. 341538 and Ontario Graduate Scholarships to HM and VS. Introduction Sexual size dimorphism describes size difference between male and female individua
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TXNIP interacts with various proteins including NLRP Yoshiha
2022-03-02
TXNIP interacts with various proteins, including NLRP3 (Yoshihara et al., 2014, Zhou et al., 2010). Emerging evidence suggests that TXNIP plays a role in ER stress-mediated cell death and in the NLRP3 inflammasome activation step (Abderrazak et al., 2015, Lerner et al., 2012, Oslowski et al., 2012,
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In addition we assessed the viability
2022-03-02
In addition, we assessed the viability of 1,2,3,4-tetrahydroquinoline (13t) and 1,2,3,4-tetrahydroisoquinoline (13u) as the tail on account of our previous SAR results. To our delight, 13t and 13u each had comparable activity to that of 13c, with 13u being slightly more potent than 13c. Further stru
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br Results br Discussion Our studies
2022-03-02
Results Discussion Our studies highlight MUFAs as key lipid modulators of both non-apoptotic and apoptotic cell death. Recent studies show that a more mesenchymal phenotype, de-differentiation, and acquired resistance to targeted inhibitors, can all promote a ferroptosis-sensitive cell state (
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SRSF is a member of Arginine Serine rich SR
2022-03-02
SRSF4 is a member of Arginine-Serine-rich (SR) protein family, that is essential for constitutive splicing and regulates alternative splicing [14]. SR proteins include one or two RNA recognition motifs (RRM) at their amino terminus and RS domains at carboxyl terminus [[15], [16], [17], [18]]. Wherea
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