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First investigation of numerous membered ether linked macroc
2023-12-19
First, investigation of numerous 12-14-membered ether-linked macrocycles revealed that smaller motifs were most lipophilic efficient. Compound (3) (12-membered macrocycle) exhibited good cellular potencies (ALK IC50 = 1.0 nM; ALK-L1196 M IC50 = 20 nM) and the highest LipE (4.4) with picomolar bindin
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Pituitary adenylate cyclase activating polypeptide PACAP
2023-12-18
Pituitary adenylate cyclase-activating polypeptide (PACAP) is a member of the secretin/growth hormone-releasing hormone (GHRH)/vasoactive intestinal peptide (VIP) family, with potent anti-inflammatory and potent cytoprotective properties [[6], [7], [8], [9], [10], [11], [12], [13]]. PACAP exists as
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Based on the improved characteristics of the
2023-12-18
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 and frogs br New perspe
2023-12-18
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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Several tertiary prevention studies are currently
2023-12-18
Several tertiary prevention studies are currently underway examining the use of dutasteride for prostate cancer treatment: (1) during expectant management of prostate cancer, (2) after radical prostatectomy in men at high risk for relapse, and (3) in men with metastatic disease. The Reduction by Dut
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br Dihydrotestosterone in adult fish and
2023-12-18
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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Ch 55 The most potent compounds within the current series of
2023-12-18
The most potent compounds within the current series of compounds were therefore , , , , and , with Ch 55 possessing the best selectivity towards the lyase reaction in comparison to the hydroxylase reaction, indeed, this compound was found to possess an IC value of 1210nM against the 17α-OHase com
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eg5 br The future of cancer therapeutics with
2023-12-18
The future of cancer therapeutics with Aurora kinase inhibitors Involvement of Aurora kinases in deregulating multiple tumor suppressor and oncogenic pathways together with the preclinical findings on the efficacy of Aurora kinase inhibitors in attenuating growth of tumor eg5 suggests that these
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These results must also be addressed
2023-12-18
These results must also be addressed in light of porcine AMPKγ3R200Q (RN−) mutation. Pigs harboring this mutation produce meat with an abnormally low ultimate pH (pHML-291 mg meat (Copenhafer et al., 2006, Lundström et al., 1998, Milan et al., 2000). This extremely low pH is very close to the isoele
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In conclusion the partial sequencing and characterization of
2023-12-18
In conclusion, the partial sequencing and characterization of R. quelen cyp19a1b provides essential information about this gene and its presence in peripheral tissues outside of the central nervous system in a teleost. Furthermore, we covered sex differences in the effects of E2 on the cyp19a1b gene
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Chlorogenic acid an abundant polyphenol found in coffee and
2023-12-18
Chlorogenic L189 australia (7), an abundant polyphenol found in coffee and the human diet, has various biological activities including antioxidant and anticancer effects [54]. Jiang et al. reported that compound 7 had a selective cytotoxic activity on human oral tumor cells (HSG, HSC-2) as compared
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br The pathogenesis of AD
2023-12-18
The pathogenesis of AD and the targets of apelin Alzheimer's drugs Conclusions Introduction APJ, first identified from a human genomic library in 1993, belongs to a member of seven trans-membrane G protein-coupled receptor family. Its amino INDY sequence has 31% homology with that of th
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br APJ expression in metabolic diseases Under physiological
2023-12-18
APJ expression in metabolic diseases Under physiological conditions, APJ is present in humans as well as in mouse tissues with high metabolic activity such as muscle and adipose tissue but not in the liver. Moreover, the presence and regulation of APJ in established adipocyte or muscle cell lines
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It is worth noting that in S cerevisiae the
2023-12-18
It is worth noting that in S. cerevisiae, the control of two cell-cycle checkpoints requiring Mcm1 involves two very different mechanisms. At the G1/S transition, Mcm1 transactivation activity is inhibited by Yox1 and Yhp1 repressors, whose expression is periodically regulated through the cell cycle
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br Concluding remarks br Definition Prion diseases are fatal
2023-12-18
Concluding remarks Definition Prion diseases are fatal neurodegenerative disorders that are caused by an unconventional agent that is neither bacterial nor viral, but is in essence an infectious misfolded amyloidogenic protein, termed a prion (Prusiner, 1982). Once considered highly controvers
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