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Darunavir Ethanolate synthesis br Drugs with documented pro
2024-03-16

Drugs with documented pro-apoptotic effects on platelets More than 200 drugs are reported to cause thrombocytopenia [5,42]. The concept of platelet apoptosis is relatively new and was only recently evaluated in the context of drug-induced thrombocytopenia [43]. Table 2 lists the drugs presently k
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br Epidemiology br Genetics The dominantly
2024-03-16

Epidemiology Genetics The dominantly inherited PrP cerebral amyloidoses are genetically transmitted with a penetrance of almost 100%. Early linkage analysis studies helped to established the relationship between GSS and mutations in the PRNP gene. PRNP is located on the short arm of chromosome
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Based on the improved characteristics of the mutant ECDs
2024-03-15

Based on the improved characteristics of the mutant ECDs we proceeded to crystallization trials, starting with the β1-BPloop as the most promising. We obtained rod shaped hexagonal crystals reproducibly, but with moderate diffraction ability (Fig. 5). Furthermore, the crystals were sensitive in moun
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br Dihydrotestosterone in adult fish
2024-03-15

Dihydrotestosterone in adult fish and frogs New perspectives and next directions Similar to other androgens, DHT can modulate reproductive endpoints in both fish and amphibians. However, predicting the effects of DHT can be challenging, as reproductive homeostasis is dependent upon the balance
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Drug resistance development often involves structurally
2024-03-15

Drug resistance development often involves structurally un-related drugs and, specifically both conventional and targeted agents. IGROV-1/Pt1 Zafirlukast receptor are characterized by resistance to cisplatin and reduced sensitivity to inhibitors of EGF-R and MEK, the up-stream activator of ERK1/2,
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Thirty six of the analogs
2024-03-15

Thirty-six of the analogs synthesized showed ATX inhibition greater than 50% at 10μM with FS-3, twelve of which had improved potency over the lead (Fig. 5). Of these, 22 was sub-micromolar (IC50 670nM). The 3,5-dichlorophenoxy ring of 22 is reminiscent of the 3,5-dichlorophenylthiourea ring in Hoegl
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The take home message here
2024-03-15

The take-home message here is that, although Aurora A phosphorylated on T288 is the activated isoform of Aurora A, measuring the level of phosphorylation of T288 does not reflect Aurora A kinase activity (Figure 5). What would be the most appropriate readout for an in vivo Aurora A kinase activity
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AP was originally described as a heterodimer of the
2024-03-15

AP-1 was originally described as a heterodimer of the bZIP proteins c-Jun and c-Fos. The experiments described here showed that stimulation of TRPV1 channels induced the expression of both of these classical constituents of AP-1. The essential role of both proteins was analyzed in a series of experi
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br Concluding remarks The past decade
2024-03-14

Concluding remarks The past decade has seen rapid advances in our understanding of the metabolic reprogramming that occurs during tumorigenesis. Strategies to target specific nodes of cancer cell amino herpes simplex virus type 1 metabolism have progressed from preclinical studies to clinical tr
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br Materials and Methods br Results A
2024-03-14

Materials and Methods Results A total of 28 NSCLC tumor samples from 26 patients (2 patients with paired tumor samples) were included. According to the initial FISH (Abbott Molecular probes) and IHC results, 13 samples were ALK IHC+FISH+, 5 samples were ALK IHC+FISH−, 2 samples (from the same
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To investigate further the clinical and mutational spectrum
2024-03-14

To investigate further the clinical and mutational spectrum associated with -related dyskinesia, we here performed a screen in a large series of patients affected with an unexplained hyperkinetic movement disorder, resulting in the identification of 2 pediatric patients presenting with a novel pheno
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Previous studies suggest that TGF
2024-03-14

Previous studies suggest that TGF-β contributes to the pathogenesis of diabetic renal injury [47]. TGF-β stimulates matrix production and prevents matrix degradation, which leads to increase collagen deposition and glomerulosclerosis [48]. In the current study ABT702 significantly reduced renal coll
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Encouraged by this observation a systematic SAR study
2024-03-14

Encouraged by this observation, a systematic SAR study on the A ring -alkoxy was conducted as summarized in . The A ring methoxy-containing KRCA-0008 was proven an optimal substituent in terms of potency after all and its bigger size derivatives were detrimental in both biochemical and H3122 cellula
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The myasthenia scale of Millichap and Dodge
2024-03-14

The myasthenia scale of Millichap and Dodge was used in our study for ease of comparison of our retrospective data with previous paediatric studies. Our results, with 30% achieving complete remission and 95% achieving at least some degree of clinical improvement following thymectomy, are comparable
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PF also a dual Aurora
2024-03-14

PF-03814735, also a dual Aurora-A and Aurora-B inhibitor, was administered in a phase I dose escalation study in a 3-weekly cisapride 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 was define
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