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We have previously reported that interfering with actin
2024-12-09

We have previously reported that interfering with Serdemetan assembly dynamics by knocking down cofilin-1 in hMSCs increased polymerized actin that promoted osteoblast cell differentiation through a mechanism of enhancing focal adhesion kinase (FAK), p38 and c-Jun N-terminal kinase (JNK) signaling
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ACK has been clearly implicated in cancer progression
2024-12-09

ACK1 has been clearly implicated in cancer progression in recent years. A strong correlation between ACK1 gene copy number, protein level and activity have been demonstrated in tumors of different tissue types (Mahajan et al., 2007; van der Horst et al., 2005; Wang et al., 2006). Our western blot an
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Acknowledgments br Introduction Prostate cancer is
2024-12-09

Acknowledgments Introduction Prostate cancer is the first leading cause of cancer-related deaths among males in the UK and the second in the US. Despite recent advances in surgery, radiation, medical management and screening, prostate cancer patients suffer high morbidity and mortality and signi
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In the case of DIA CN the docking results
2024-12-07

In the case of DIA-4CN the docking results do not show any interaction between the iron atom and the inhibitor, presumably due to the reduced ability to form a complex involving the -CONN- moiety versus the bidentate -CONHNH- central group of HYD-4Me. This results in a considerable gap between the
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The allosteric site of class C
2024-12-07

The allosteric site of class C receptors is generally located on the extracellular side of the TM domain (Brauner-Osborne et al., 2007, Christopher et al., 2015, Dore et al., 2014, Gregory et al., 2011, Harpsoe et al., 2017, Kniazeff et al., 2011, Pin and Prezeau, 2007, Urwyler, 2011, Wu et al., 201
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br Material and methods br
2024-12-07

Material and methods Results Discussion This study explores the hypothesis that ASK1, via transcriptional upregulation by E2F1, molecularly defines AT that supports a dys-metabolic obese phenotype in humans. We demonstrate associations between increased visceral-AT ASK1 expression and multi
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br In vivo visualization of aromatase with positron emission
2024-12-07

In vivo visualization of aromatase with positron emission tomography (PET) Positron emission tomography (PET) utilizes the high LY83583 photons formed during the annihilation of positrons to detect the changes in the amount and localization of injected radiopharmaceuticals in the living body (rec
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br Asthma The chronic airway inflammatory disease
2024-12-07

Asthma The chronic airway inflammatory disease Saracatinib is associated with enhanced levels of exhaled NO generated by iNOS in the airway epithelium [12]. In asthmatic patients local and systemic changes in iNOS, peroxynitrite, arginase, ADMA and arginine levels have been observed and are assoc
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This study evaluated the anti tumor influences of LA
2024-12-07

This study evaluated the anti-tumor influences of LA against HepG2 molecular weight marker in vivro, and investigated the molecular mechanisms of inducing apoptosis. Overall, our studies suggested that LA is a promising anti-cancer drug and a possible novel therapeutic agent directed toward the mit
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Available data thus indicate that there are
2024-12-07

Available data thus indicate that there are at least two ways that HMGA proteins can induce localized changes in the chromatin structure of inducible gene promoters, both of which involve positioned nucleosomes that must be “remodeled” before gene transcription can occur. The first mechanism is exem
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Interestingly metabolic dysfunction is also observed in amyo
2024-12-07

Interestingly, metabolic dysfunction is also observed in amyotrophic lateral sclerosis (ALS). Patients and mouse models of familial ALS exhibit higher levels of resting bromophenol blue expenditure and lower fat-free mass, indicating a hypermetabolic phenotype. Lim et al. (2012) found that reducing
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In this study we designed and synthesized two ALK PROTACs
2024-12-07

In this study, we designed and synthesized two ALK PROTACs (degraders), 5 (MS4077) and 6 (MS4078), by linking ceritinib and pomalidomide [45] through two different linkers. Using human ALCL and NSCLC cells, we characterized both compounds in a battery of assays to demonstrate their effects on reduci
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Similarly compound was prepared from aldehyde
2024-12-07

Similarly, TAK-715 13 was prepared from aldehyde 8d by following similar procedures (Scheme 3). Condensation of 13 with 7b or 7e provided the corresponding amides 9j or 9k, which then went through O-debenzylation by BCl3 to deliver the final compounds 10j and 10k in 37% and 32% overall yields, respe
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Introduction Aldose reductase ALR is the
2024-12-07

Introduction Aldose reductase (ALR2) is the first enzyme of the polyol pathway that catalyzes the reduction of glucose to sorbitol utilizing NADPH as a cofactor. The intracellular accumulation of sorbitol, due to increased aldose reductase activity at high blood glucose levels, such as those occurr
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br AhR Modulators It is now well recognized
2024-12-07

AhR Modulators It is now well recognized that ligand-activated AhR induces an immune tolerance response by acting directly on the antigen-presenting DCs and indirectly by increasing the population of immunosuppressive Tregs 24, 95, 96. In addition to inhibiting the formation or depleting the AhR
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