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br ARIs in the prevention of
2023-09-07

5ARIs in the prevention of prostate cancer Prostate cancer continues to be a leading cause of male deaths worldwide. In 2009, it was estimated there would be 192,280 new cases of prostate cancer with a predicted 27,360 deaths [25]. Because androgens, and specifically DHT, play a large role in bot
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Another significant group of reductase inhibitors is the ste
2023-09-07

Another significant group of 5α-reductase inhibitors is the steroidal 3-carboxylic Pam2CSK4 derivatives (relevant examples in Fig. 5), which were designed to mimic the putative enzyme-bound enolate intermediate. This was achieved by introducing sp2-hybridized centers at C3 and C4 and an anionic car
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DRiPs also contribute to formation of
2023-09-06

DRiPs also contribute to formation of protein fda approved vegf inhibitor that result from dysregulation of proteostasis, during which the proteolytic machinery is unable to process and degrade defective proteins (Tyedmers et al., 2010). Aggregation of poly-ubiquitinated proteins has been observed
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Aurora A and B are required for the
2023-09-06

Aurora A and B are required for the control of mitosis whereas Aurora C is mainly invoved in meiosis (Goldenson and Crispino, 2015). Interestingly, Aurora B is partnered with inner centromere protein (INCENP), survivin and Borealin to form a chromosomal passenger complex (CPC) that is critical for t
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After infection with Salmonella those bacteria that are not
2023-09-06

After infection with Salmonella those bacteria that are not targeted by autophagy of the complete Salmonella-containing phagosome (see above) but are living freely in the cytosol can be eliminated by xenophagy, that is direct targeting of the ‘naked’ bacteria to the autophagic pathway. The type III
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It is increasingly evident that many metabolic genes are
2023-09-06

It is increasingly evident that many metabolic genes are associated with cancer progression of various tumor cells, including NSCLC. In particular, GLUT1 overexpression has been reported in NSCLC, and correlations between GLUT1 expression and a number of clinical parameters such as gender, smoking s
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cannabinoid receptors Many naphthoquinone derivatives have b
2023-09-06

Many naphthoquinone derivatives have been previously obtained from fungi in the genus Fusarium isolated from various sources, F. oxysporum from the root of citrus (Nagia and El-Mohamedy, 2007), Fusarium sp. (No. b77) from the mangrove plant (Shao et al., 2010), F. solani and F. oxysporum from fibrou
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br Material and methods br Results Table
2023-09-06

Material and methods Results Table 1 shows that in addition to Leu/CysAP and DPPIV, genes for AspAP, ArgAP, MetAP, APM and PSA are expressed in adipocytes. The kinetic parameters of these AP are also shown in Table 1, revealing that APM has the highest Vmax and catalytic efficiency (Kcat/Km),
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Imatinib was first approved for the treatment of Philadelphi
2023-09-06

Imatinib was first approved for the treatment of Philadelphia chromosome positive chronic myelogenous leukemia in 2001 [25]. This first approved small molecule antagonist is quite unusual in that it provides a durable response that lasts for more than a decade in the majority of patients. Imatinib h
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In glaucoma the primary retinal defect appears in the GCL
2023-09-06

In glaucoma, the primary retinal defect appears in the GCL, whereas the other retinal layers appear normal (Kendell et al., 1995). In the current work, chronic elevation of IOP induced RGC apoptosis, especially in the GCL, and α2 adrenergic treatment reduced RGC apoptosis. Various studies have repor
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Further evidence for action mechanism was
2023-09-06

Further evidence for action mechanism was provided by assays using [3H]nisoxetine, a selective NET inhibitor used as standard radioligand for competitive binding experiments. The results showed dose-dependent blocking of [3H]nisoxetine binding by both xylazine and dexmedetomidine. Nisoxetine binds t
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Similar to V the temporal
2023-09-06

Similar to V1, the temporal neocortex of mammals, including the primary auditory cortex (A1), is densely innervated by 5-HT fibers originating mainly in the dorsal raphe nucleus (Campbell et al., 1987, Harding and Paxinos, 2004, Törk, 1990), and the major Tubacin of 5-HTRs are expressed throughout t
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In the late s Solvay Pharmaceuticals discontinued the
2023-09-06

In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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It is worth pointing out that phenotypes of in vivo
2023-09-06

It is worth pointing out that phenotypes of in vivo HSP90β inhibition were not identical to those observed in rapsyn mutant mice (Gautam et al., 1995). Postsynaptically, junctional AChR clusters appeared fragmented, in addition to expected reduction in AChR intensity, in muscles injected with 17-AAG
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The AChR is composed of
2023-09-06

The AChR is composed of five homologous, membrane-spanning subunits. AChRs containing two α, one β, one δ and one γ subunit (AChRγ) predominate during embryonic development and mice lacking AChRγ die at birth (Takahashi et al., 2002). After birth, the AChRγs are replaced during the first 2 postnatal
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