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br Conclusion Biotransformation of trachyloban
2023-09-22
Conclusion Biotransformation of trachyloban-19-oic CBR-5884 by S. racemosum provided three products. Oxidation of compound 1 at C-17 (2–3), as well as rearrangement of 1 into a kaurane diterpene hydroxylated in C-16 and C-17 (4) were crucial for increasing AChE inhibitory activity. Compound 3 wa
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The lanthanide series of chemical elements comprises the
2023-09-22
The lanthanide series of chemical elements comprises the fifteen metallic chemical elements with atomic numbers 57 through 71, from lanthanum to lutetium. Though originally described as ‘‘rare earths’’ because of their natural occurrence as metal oxides, they are not particularly rare. The lanthanid
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In the U S surveillance
2023-09-22
In the U.S., surveillance of ACEs has garnered traction at the state level through administration of the ACE Optional Module in CDC’s Behavioral Risk Factor Surveillance System (BRFSS) (Centers for Disease Control & Prevention, 2003). Since 2009, select states have implemented the ACEs optional modu
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To date more than different mutations in the gene
2023-09-22
To date, more than 50 different mutations in the gene have been described (Human Gene Mutation Database at the Institute of Medical Genetics in Cardiff: SRD5A2 Gene: http://www.hgmd.cf.ac.uk). Most of them are missense mutations but premature stop codons and deletions leading to non-functional or su
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During the year study period of men in
2023-09-22
During the 4-year study period, 19.9% of men in the dutasteride group developed prostate cancer as compared to 25.1% in the placebo group, which represents an absolute risk Z-WEHD-FMK of 5.1% for men taking dutasteride (Pe weighed against the prospect of undesirable sexual side effects and decrease
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At present drugs that specifically
2023-09-22
At present, drugs that specifically inhibit YAP activity are not available. In fact, verteporfin, which was originally described as a specific inhibitor of YAP-TEAD interaction, has been recently shown to exert its activity through selective induction of proteotoxicity rather than through YAP inhibi
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Compound was docked into the active site of
2023-09-22
Compound was docked into the active site of Aurora B kinase using Tripos sybyl-X ver. 2.1.1. The crystal structure of human Aurora B kinase cocrystallized with its potent inhibitor VX-680 was used for the docking analysis (PDB ID: ). The most likely binding conformations were selected based on the
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After infection with Salmonella those
2023-09-22
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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Consistent with a damaging role for
2023-09-22
Consistent with a damaging role for increased 12/15-LOX activity in stroke, systemic administration of the 12/15-LOX inhibitor, LB1, 2 h after permanent focal cerebral ischemia significantly reduced infarct size 24 h after the ischemia, and the treatment group demonstrated improved behavioral and he
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TLX may promote survival and prevent apoptosis in
2023-09-22
TLX may promote survival and prevent apoptosis in NB GSK2118436 [12]. Here, we ask whether the survival-promoting effects of TLX are mediated by Apoptosis Signal-regulating Kinase-1 (ASK1, MAP3K5). ASK1 is a member of the Mitogen-Activated Protein (MAP) kinase family and it preferentially activates
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In previous years evidence emerged that inferred
2023-09-22
In previous years, evidence emerged that inferred secondary metabolites in plants might exhibit a potential arginase inhibition [36]. In a recent study, Pham and co-workers showed the inhibitory activity of chlorogenic e 64 (7) and piceatannol (8) (Fig. 3b) on mammalian arginase with IC50s of 10.6
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The accumulation of oxidized low density
2023-09-22
The accumulation of oxidized low-density lipoprotein (oxLDL) is one of the many causes of the initiation and progression of atherosclerosis (Virmani et al., 2002; Pirillo et al., 2013; Sun et al., 2016; Huang et al., 2016; Tabas, 2010). oxLDL-induced apoptosis of macrophages contributes to the forma
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Gratifyingly compound also demonstrated improved physicochem
2023-09-21
Gratifyingly, compound also demonstrated improved physicochemical properties with significant improvement in aqueous solubility. Compound was sufficiently potent to determine its pharmacokinetic (PK) and pharmacodynamics (PD); data is summarized in . shows ADME characteristics for compound and
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br HIF HIF signaling in cancer cells contributes
2023-09-21
HIF-1α HIF-1α signaling in cancer cells contributes to tumor progression by promoting angiogenesis, invasion, metastasis, and the recruitment of immunosuppressive cells via secreted modulators 36, 37. One example of a HIF-1α immunosuppressive pathway is through increased expression of inducible n
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KL 001 receptor br Conclusions br Acknowledgments The author
2023-09-21
Conclusions Acknowledgments The authors are thankful to Hugo Santos, Olga Martinez and Ricardo Lacerda for the technical assistance provided in the maintenance of the aquaria. This work was supported by national funds, through FCT and co-funded by the European Regional Development Fund (ERDF)
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