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Application of the broad acting HTR antagonist methiothepin
2025-03-03
Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L
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The same applies also to intermediate formally obtained by e
2025-03-03
The same applies also to intermediate , formally obtained by elimination of the R substituent from compound . If compared to the thienopyrimidine derivatives (series , C), the thieno[3,2-]pyridazin-5(4H)-ones – explored herein seem to maintain similar size and shape and also analogue structural char
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That disassembling actin filaments transport chromosomes tow
2025-03-03
That disassembling 67 8 filaments transport chromosomes towards the spindle in oocytes may be surprising at first sight. On the other hand, it is well established that chromosome movement during anaphase is driven by the depolymerization of microtubules [20]. It will be interesting to investigate t
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Regarding the HT B receptors they act as
2025-03-03
Regarding the 5-HT1B receptors, they act as terminal receptors and are involved in the presynaptic regulation of the release of 5-HT. But at spinal level these receptors are principally situated post-synaptically (Sari, 2004). The ability of autoreceptors to regulate extracellular levels of 5-HT dur
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dna-pk inhibitor br COPD As in asthma also
2025-03-01
COPD As in asthma, also in COPD, increased expression of arginase has been reported, and tobacco smoke may increase expression of arginase in human subjects [46, 47]. Increased ADMA levels have also been reported in COPD, and both the increased expression of arginase and ADMA contribute to remode
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This study evaluated the anti tumor influences
2025-03-01
This study evaluated the anti-tumor influences of LA against HepG2 (Z)-4-Hydroxytamoxifen in vivro, and investigated the molecular mechanisms of inducing apoptosis. Overall, our studies suggested that LA is a promising anti-cancer drug and a possible novel therapeutic agent directed toward the mito
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Although the gene that encodes
2025-03-01
Although the gene that encodes DHFR has been strongly conserved during evolution, subtle differences in the active sites of bacterial, human and parasite Octreotide acetate have been exploited to develop DHFR inhibitors specific to particular pathogens 1, 3. For example, pyrimethamine and cycloguan
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br Nanoparticle Conjugated Topoisomerase Inhibitors The safe
2025-03-01
Nanoparticle-Conjugated Topoisomerase Inhibitors The safety and efficacy of topotecan administered as LDM or MTD have been evaluated in several preclinical studies and a few clinical trials whose results showed that there can be significant adverse effects likely precluding its use in patients [5
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Immunohistochemistry in tissue samples showed the
2025-03-01
Immunohistochemistry in tissue samples showed the expression of several nuclear receptor co-activators, including NCOA1, NCOA2, NCOA3, CREBBP, and EP300, in 85–100% of THZ1 Hydrochloride tumors even some of which lacked AR expression (Boorjian et al., 2009). Knockdown of each co-activator also resu
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br STAR Methods br Author Contributions br Acknowledgments T
2025-03-01
STAR★Methods Author Contributions Acknowledgments This study is funded by National Institutes of Health (NIH) Grants NS028901 and DC004450 (to L.O.T.); N.L. Tartar Trust Fellowship (to H.-W.L.); DC014878 to T.S.B. We thank members of the Trussell lab for helpful discussions, Dr. Stephen Dav
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br Materials and methods br Results br Discussion Prostate c
2025-03-01
Materials and methods Results Discussion Prostate cancer is the most common cancer in men in the United States and the second leading cause of cancer death. Therapeutic interventions include mainly: radical prostatectomy or radiation therapy (RT), with or without androgen deprivation therap
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Gonadotropin-releasing hormone Our studies also reveal the
2025-03-01
Our studies also reveal the normal functional roles of the MIR. Interaction between the MIR loop and the N-terminal α helix nucleates conformational maturation of AChR subunits, thereby promoting assembly of mature AChRs [52], [55]. This interaction in homologous parts of all AChR subunits appears t
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LY-2228820 Tacrine an aminoacridine derivative Fig
2025-03-01
Tacrine, an aminoacridine derivative (Fig. 1, A), was the first AChE inhibitor approved for treatment of AD [12], [13]. This compound was withdrawn from the market due to its hepatotoxicity [14]. In spite of tacrine's side effects, it is still an attractive lead compound for medicinal chemists due t
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br Antioxidative stress and anti inflammation Oxidative stre
2025-03-01
Antioxidative stress and anti-inflammation Oxidative stress is a major cause of reduced endothelial NO bioavailability in hypertension, and inflammatory response is thought to play an important role in these processes (Blake and Ridker, 2001, Landmesser et al., 2006). Reactive oxygen species (ROS
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2825 The initial observations indicating a
2025-02-28
The initial observations indicating a crucial role for 2825 transfer in 17,20 lyase activity were that the molar ratio of POR to P450c17 is three- to four-fold higher in porcine testes than in porcine adrenals, and that adding purified POR to porcine P450c17 in vitro increased 17,20 lyase more than