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The Type A series contains
2023-05-15

The Type-A series contains 6 of the 11 confirmed hits, making it a highly attractive lead template. Seven (7) out of 8 Type-A series of 3-substituted-2-furoic acids are highly active (84–100% inhibition) at the high concentration of 100μM. We could deduce some interesting, albeit preliminary structu
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Many ruthenium complexes were tested
2023-05-15

Many ruthenium complexes were tested as potential anticancer agents and two complexes, namely NAMI-A (trans-[imH] [RuCl4(dmso-S)(im)]; im, imidazole) and KP1019 (trans-[indH][RuCl4(ind)2]; ind, indazole) have successfully entered clinical trials [27], [28]. NAMI-A is selectively active against metas
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The allosteric site of class C receptors
2023-05-15

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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Why do glutamate and glycine bind to the receptor in
2023-05-15

Why do glutamate and glycine bind to the Antagonist G mg in such different ways? Given the overall structural similarity between the GluN2A and GluN1 LBDs, one might conclude that the LBDs also bind ligands via similar processes. NMDA receptors with engineered disulfide linkages that lock the GluN1
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Kidney contributes importantly to the
2023-05-15

Kidney contributes importantly to the long-term blood pressure control via regulating sodium homeostasis. Renal proximal tubule (RPT) is one of the most critical segments for sodium reabsorption within kidney and therefore involved in blood pressure adjustment. This process is regulated by numerous
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br Materials and Methods br Author Contributions br Conflict
2023-05-15

Materials and Methods Author Contributions Conflicts of Interest Acknowledgments We thank Francine Jodelka for technical assistance and Gopal Thinakaran for the CTM-1 antibody. This work was financially supported by RFUMS internal research funding and NIHS10 OD 010662. Introduction A
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Several ceritinib resistant mutations following the second l
2023-05-15

Several ceritinib-resistant mutations following the second-line treatment of ALK+-NSCLC have been discovered [64]. These mutations include C1156Y, F1174L, and L1152R, which were first observed in crizotinib-resistant tumor samples. The G1202R ceritinib-resistant mutation occurs within the hinge and
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In addition to it we also
2023-05-15

In addition to it, we also showed that glycine increases miR-301a expression which directly binds to PTEN 3′UTR target sites [13]. Glycine confers neuroprotection through microRNA-301a/PTEN signaling in rats cortical neurons in oxygen deprivation model [13]. Substantial studies indicate that inhibit
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The mechanisms that control Ahr transcription are poorly und
2023-05-15

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 ZSTK474 australia receptor (RAR)-related orphan receptor γt] based on Ch
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Two cell surface trans membrane receptors have been identifi
2023-05-15

Two cell-surface trans-membrane receptors have been identified for adiponectin, AdipoR1 and AdipoR2 [21], and adiponectin action is known to signal through these receptors and the docking protein APPL1 [22]. In muscle and liver cells, signal transduction involves the phosphorylation and activation o
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The gene SRD A encodes the reductase enzyme
2023-05-10

The gene SRD5A2 encodes the 5-α-reductase enzyme, which converts testosterone into dihydrotestosterone. Although dihydrotestosterone levels are considerably lower than testosterone, dihydrotestosterone has a five-fold stronger binding capacity to the androgen receptor and, thereby, a considerably mo
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br Discussion The measurement of gonadotropins FSH LH is
2023-05-09

Discussion The measurement of Eribulin mg (FSH, LH) is critical in the evaluation and assessment of 46,XX females presenting with primary amenorrhea and lack of pubertal development. A serum level of FSH higher than 40 U/L is diagnostic of ovarian failure (6), as seen in the present case. The mo
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br Acknowledgements We thank Dr Stefan Schulte Merker and
2023-05-09

Acknowledgements We thank Dr. Stefan Schulte-Merker and his group members at the Hubrecht Institute (Utrecht, the Netherlands) for their invaluable support of the zebrafish studies. Our work is supported by grants from the Dutch Cancer Society (KWF) and the Netherlands Organisation for Scientific
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Acknowledgments br Introduction Prostate cancer is the first
2023-05-09

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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br Antibiotic drug discovery approaches Traditionally novel
2023-05-06

Antibiotic drug discovery approaches Traditionally, novel 5-Methoxy-CTP were largely discovered by phenotypic screening approaches of various sources of compounds, such as natural products isolated from extracts of soil microbes and semi-synthetic or fully synthetic compound libraries derived fro
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