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By promoting bundling and processive elongation of actin
2023-10-25

By promoting bundling and processive elongation of Coumarin sale filaments and inhibiting association of capping protein with filament barbed ends, Ena/VASP family proteins contribute to the dynamics of lamellipodia and filopodia [41] and maintenance of focal adhesions and tight junctions [42, 43].
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Pyrimidine is the important pharmacology
2023-10-24

Pyrimidine is the important pharmacology core in many Aurora inhibitors, such as VX-680, ENMD-2076, CYC-116 and ENMD-2076 [12]. To identify additional effective Aurora inhibitors, we designed a series of 2,4-diaminopyrimidine compounds, our modeling studies suggested that the Salmeterol xinafoate co
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map3k8 We conducted the largest drug screen to date
2023-10-24

We conducted the largest drug screen to date in HPV-positive cancers and identified Aurora kinase inhibitors as effective and understudied drugs in HNSCC and CESC. These drugs cause apoptosis and cell cycle arrest in vitro and decrease tumor size in vivo. This is the first published study to demonst
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Aurora B is also known as chromosomal
2023-10-24

Aurora-B is also known as chromosomal passenger protein and localizes at the chromosome arms and at centromeres during prophase. As cell cycle continues, Aurora-B moves towards the inner centromere region followed by the central spindle and cortex during SEA0400 and finally accumulates in the midbo
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Acknowledgments br Introduction Pulmonary fibrosis PF is a
2023-10-24

Acknowledgments Introduction Pulmonary fibrosis (PF) is a chronic, fibrosing interstitial pneumonia and a crushing disease that occurs as a result of a variety of lung injuries, including auto-immune, tuberculosis and traumatic insult [1], [2]. PF is characterized by the accumulation of extracel
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gap junction br Materials and methods br
2023-10-24

Materials and methods Results Discussion Diabetic kidney disease (DKD) is the most common cause of end-stage renal disease [15], [16]. The pathogenesis of DKD is not fully understood, and there is no effective treatment. Although previous studies suggested that early lesions of DKD are foun
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Immunohistochemistry in tissue samples showed the expression
2023-10-24

Immunohistochemistry in tissue samples showed the expression of several nuclear receptor co-activators, including NCOA1, NCOA2, NCOA3, CREBBP, and EP300, in 85–100% of L-α-Aminoadipic Acid tumors even some of which lacked AR expression (Boorjian et al., 2009). Knockdown of each co-activator also re
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Although only Leu CysAP IRAP Herbest et
2023-10-24

Although only Leu/CysAP (IRAP) (Herbest et al., 1997, Keller, 2004) and DPPIV (Alponti and Silveira, 2010, Kirino et al., 2009) had been identified and studied in adipocytes, our kinetic analysis suggested the highest physiological significance for AspAP (highest affinity) and APM and PSA (highest e
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br Introduction Psychostimulant abuse and addiction remain a
2023-10-24

Introduction Psychostimulant abuse and addiction remain a societal problem in the United States. The latest statistics from the National Survey on Drug Use and Health indicate that slightly less than one million people over the age of 12 report having a cocaine use disorder (NSDUH, 2016). Additio
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The mechanisms that control Ahr
2023-10-24

The mechanisms that control Ahr transcription are poorly understood, especially when considering cell type-specific regulation. A recent report suggested that the Ahr transcription might be directly promoted by RORγt [retinoic Dasatinib Monohydrate receptor (RAR)-related orphan receptor γt] based o
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Tamoxifen br Results br Discussion Tapinarof GSK is a natura
2023-10-24

Results Discussion Tapinarof (GSK2894512) is a naturally derived investigational topical medicine with demonstrated clinical efficacy for patients with AD and psoriasis (Bissonnette et al., 2010, Bissonnette et al., 2012a). The drug substance is a polyphenol produced by bacteria that is struct
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We aim to evaluate the AK
2023-10-24

We aim to evaluate the AK in regulating adenosine signaling in the retina. It was reported that the degree of N-(p-amylcinnamoyl) injury directly depends on expression levels of AK and the resulting extracellular levels of adenosine (Boison, 2006). Indeed, transgenic mice overexpressing AK are highl
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The first rationally designed dual mPGES
2023-10-23

The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic MRS1523 - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been synthesized
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Because activation of HT A receptor is capable of
2023-10-23

Because activation of 5-HT2A receptor is capable of facilitating dopamine cell activity and dopamine release (Bortolozzi et al., 2003), and this action of dopamine is known to mediate rat maternal behavior, especially maternal motivation (Afonso et al., 2007, Febo et al., 2010, Li and Fleming, 2003,
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PF also a dual Aurora A and
2023-10-23

PF-03814735, also a dual Aurora-A and Aurora-B inhibitor, was administered in a phase I dose escalation study in a 3-weekly zilpaterol receptor for 5 or 10 consecutive days [69], [70]. To date 25 patients have been included in 7 dose levels (5–100mg/day for 5 days). Using the 5-day schedule the MTD
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