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In stark contrast to this study Zhang and colleagues
2022-03-09

In stark contrast to this study, Zhang and colleagues demonstrated that FFA4, along with FFA1, play roles in suppressing cell proliferation and promoting apoptosis in CRC clozapine clozaril treated with omega-3 PUFA [53]. In this study design, in vivo CRC was induced in mice upon treatment with the
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MMV s distinct mode of inhibition addresses key impediments
2022-03-09

MMV019313's distinct mode of inhibition addresses key impediments in the development of PfFPPS/GGPPS inhibitors as antimalarial drugs. First, it is the first non-bisphosphonate inhibitor of Plasmodium FPPS/GGPPS with drug-like physicochemical properties satisfying the “Rule of 5” (Van Voorhis et al.
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In conclusion we have shown that
2022-03-09

In conclusion, we have shown that the brain penetrating ability of heteroaryl piperazine and piperadine ureas can be modulated through small structural changes to the heteroarenes, the piperazine or piperidine core, and the biaryl ether tail. Compounds exhibiting / ratios ranging as high as 4.2:1 to
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We found the FAAH CC genotype only confers
2022-03-09

We found the FAAH CC genotype only confers risk for anxiety if the CRFR1 minor allele combination is also present. Additionally, the FAAH AA/AC genotype was riskier than the CC if the three CRFR1 minor Atractyloside Dipotassium Salt were not present. This result is somewhat contrary to our predictio
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The even bigger surprise was the second feature of both
2022-03-09

The even bigger surprise was the second feature of both structures. Interestingly, binding of the MRG domain hardly altered the conformation of the SET domain compared with its apo state (An et al., 2011). What did change, however, is the conformation of the ASH1L auto-inhibitory loop (Figure 1). De
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br Pharmacological anti aging approaches and the Hippo pathw
2022-03-08

Pharmacological anti-aging approaches and the Hippo pathway Aging and age-related pathologies are the main causes of disabilities and death. As Magalhañes and colleagues suggest, the challenges of developing anti-aging pharmacological therapies may, in part, be due to the complexity of aging mole
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microRNAs miRNAs of approximately nucleotides
2022-03-08

microRNAs (miRNAs) of approximately 22 nucleotides play vital roles in cancer development and progression by regulating translational repression or decay of target messenger RNAs (mRNAs) through their binding to the 3′-untranslated regions (3′-UTRs) of target mRNAs with imprecise or precise compleme
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Nazar and colleagues reported a normal HER
2022-03-08

Nazar and colleagues reported a normal HER2 gene number in 13 primary and 2 recurrent ethmoid sinus adenocarcinomas, without any histological and immunohistochemical characterization, so a comparison with the present findings is impossible [14]. More recently, 552 head and neck carcinomas have been
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FoxM a downstream target of Gli has
2022-03-08

FoxM1, a downstream target of Gli, has been mainly related to BH3I-1 australia regulation and cellular proliferation in tumor (Alvarez-Fernandez and Medema, 2013, Halasi and Gartel, 2013, Teh et al., 2002). Especially, FoxM1 is a regulator of G1/S and G2/M transitions and M-phase progression (Wonse
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br Conclusion and future perspectives
2022-03-08

Conclusion and future perspectives The nicotinic Adaptaquin receptor GPR109A and its close relatives GPR109B and GPR81 are primarily expressed in adipocytes and are coupled to Gi-type G proteins. Recently, the ketone body β-hydroxy-butyrate, the β-oxidation intermediate 3-hydroxy octanoic acid a
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br Acknowledgements br Introduction The
2022-03-08

Acknowledgements Introduction The study methods consisted of the review of articles included in the Pubmed and Medline databases and in the clinicaltrials.gov clinical trials register between 2013 and 2016, and of the preliminary results of therapies presented at international trichology confe
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br Competing interests br Introduction An effective vaccine
2022-03-08

Competing interests Introduction An effective vaccine against the Human immunodeficiency virus (HIV) is still to be created, even though many strategies have already been tried [1]. Antibodies against a vaccine antigen must be either neutralizing or inducing cellular cytotoxicity [1]. It is kn
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GnRH ant have been designed to obtain pharmacological compou
2022-03-08

GnRH-ant have been designed to obtain pharmacological compounds to block the pituitary–gonadal axis without the undesirable flare effect exerted by GnRH itself or by the GnRH-a (see Section 2.2). GnRH-ant competitively block the binding of GnRH to GnRHRs (Schally, 1999; Tan & Bukulmez, 2011); they p
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In summary we discovered azaindole substituted hydroxypyrido
2022-03-08

In summary, we discovered 7-azaindole substituted -hydroxypyridone as a potent zinc-binding GLO1 inhibitor (IC=11nM) through lead generation from HTS and structure-based inhibitor design. The X-ray cocrystal structure and the comparison of binding energies with the indole counterpart revealed that
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br Materials and methods br
2022-03-08

Materials and methods Results Discussion The redox domain that spans the region between amino tak 242 positions 35 and 127 of the major human AP endonuclease, APE1, regulates the sequence-specific DNA binding of various transcription factors [[52], [85]]. The existent crystal structures of
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