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SU11274 br Conclusion We have identified potential inhibitor
2024-11-14
Conclusion We have identified potential inhibitors of C. albicans fungus specific nuclear target outer kinetochore Dam1 complex subunit Ask1, virtually screened through the PubChem compounds database (NCBI, USA) by utilizing state-of-art in silico methods in a pipeline. The 3D protein structure o
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Apamin Second the choice of the PAABD is critical
2024-11-14
Second, the choice of the PAABD is critical for an efficient and sensitive biosensor. The sequence of the PAABD should present high affinity and efficient recognition of the phosphorylated substrate, as opposed to poor affinity for the unphosphorylated substrate, and should display a fully reversibl
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The excellent safety profile of solanezumab and
2024-11-14
The excellent safety profile of solanezumab and encouraging trends in the exploratory analyses in mild AD led to its inclusion in two secondary prevention trials, which are continuing in the hope that earlier intervention may yield more substantial benefit. The A4 study (NCT02008357) started in Febr
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br AKT signaling is essential during early dorsal
2024-11-13
AKT signaling is essential during early dorsal patterning, neural crest induction and maturation AKT signaling modulates EMT and migration of the neural crest cells The defining feature of NC cells is their delamination from the dorsal neural epithelium. At the end of neurulation, mature premi
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Active SI behavior was dose dependently affected by PACAP tr
2024-11-13
Active SI behavior was dose-dependently affected by PACAP treatment (F3,25 = 14.42, p likely reflects anxiety-like behavior because 1.0 μg PACAP did not affect maximum ICSS rates. Importantly, the PACAP dose administered to the treatment rat did not affect SI behaviors of the partner rat (Figure 2D
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Beside activation of adenosine receptors
2024-11-13
Beside activation of adenosine receptors (A2a.1, A2a.2, A2b) by FSK treatment, the expression of adenosine receptors was also upregulated, when embryos were exposed to inhibitors (SU5416 and DAPT) alone and also combined with FSK. Our data imply that adenosine receptor was associated with a positive
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During the course of our ACK
2024-11-13
During the course of our ACK1 inhibitor program, a high-throughput screening (HTS) campaign of our internal sample collection was conducted. A series of -aryl pyrimidine-5-carboxamides of the general structure () was identified. Earlier studies of the structure–activity relationship (SAR) of ident
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Finasteride has been shown to be
2024-11-13
Finasteride has been shown to be a mechanism-based inhibitor of 5AR-2 [9]. Finasteride acts as an alternate substrate for 5AR-2 and is initially bound in an extremely stable enzyme-bound NADP-dihydrofinasteride adduct which is ultimately processed to dihydrofinasteride. The NADP-dihydrofinasteride a
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PNU 37883 hydrochloride br Cytochrome b br Cytochrome P hydr
2024-11-13
Cytochrome b5 Cytochrome P450 17α-hydroxylase/17,20-lyase (P450 17A1) A number of P450s involved in steroid biosynthesis are multifunctional as they carry out two or more sequential hydroxylation reactions on the same substrate(s). P450 17A1 is a dual function endoplasmic reticulum enzyme enco
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Matsuzaki et al attempted fertility therapy in a year
2024-11-13
Matsuzaki et al. attempted fertility therapy in a 26-year-old female with secondary amenorrhea and 17OHD who was a bungarotoxin mg heterozygote for delF53/54 and the missense mutation H373L, which has aromatizable substrates might account for anovulation-related infertility in females with 17OHD, a
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br Dual role of autophagy
2024-11-13
Dual role of autophagy in human diseases Emerging evidence suggests that autophagy serves as a double-edged sword in several human diseases, such as CNS diseases (Rubinsztein et al., 2015), arteriosclerosis (Schrijvers et al., 2011) and cancer (Ozpolat and Benbrook, 2015). Likewise, currently the
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SIN-1 chloride Jesus et al discovered a new series of
2024-11-13
Jesus et al. discovered a new series of azaindole as Aurora inhibitors through various modification of GSK1070916 (47). They synthesized series from modification of the GSK1070916 and evaluated for in-vitro Aurora-B/INCENP and Aurora-A/TPX2 inhibition assays. Modified SIN-1 chloride 48 and 49 showe
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We next sought to determine the kinase
2024-11-13
We next sought to determine the kinase responsible for IR-induced phosphorylation of 53BP1. Because the sites under investigation all lie in a consensus sequence for ATM, ATR and DNA-PK, that are all activated by IR, the involvement of each of these kinases was investigated. Preincubation of Gambogi
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br Apelin The APJ receptor ligand
2024-11-12
Apelin The APJ receptor ligand apelin firstly in 1998 was segregated from bovine stomach tissue. Human preproapelin gene located on chromosome Xq25–26.1. The apelin preproproteins consist of 77 amino 4 mu mg residues that are cleaved into biologically active C-terminal fragments of various sizes
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Interestingly metabolic dysfunction is also observed in
2024-11-12
Interestingly, metabolic dysfunction is also observed in amyotrophic lateral sclerosis (ALS). Patients and mouse models of familial ALS exhibit higher levels of resting Epoxomicin expenditure and lower fat-free mass, indicating a hypermetabolic phenotype. Lim et al. (2012) found that reducing AMPK
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