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br Experimental section br Abbreviations PSA puromycin
2024-12-17

Experimental section Abbreviations PSA, puromycin–sensitive aminopeptidase; APN, aminopeptidase N; AML, acute myeloid Leukemia; ALL, acute lymphoblastic leukemia; AADR, amino AICAR deprivation response; PAN, puromycin aminonucleoside; DCC, dicyclohexyl carbodiimide; NHS, N–hydroxy succinimide;
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In summary we suggest that both cofilin and gelsolin
2024-12-17

In summary, we suggest that both cofilin and gelsolin are essential factors that regulate sperm capacitation and the acrosomal exocytosis by modulating actin. The relationships between activation/inactivation of cofilin and gelsolin suggest that inhibition of cofilin is important for allowing F-acti
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As a continuation of our search for
2024-12-17

As a continuation of our search for a selective AChE radioligand bearing a meta-F substituted N-benzyl moiety, we designed and synthesized a novel meta-F-CP-118,954 analog along with a meta-18F-labeled form via diaryliodonium salt-based precursor (Fig. 1). For comparative purposes, we incorporate th
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It has been recognized for decades that neurons in the
2024-12-17

It has been recognized for decades that neurons in the mammalian central nervous system may release both a fast-acting, typically amino acid derived neurotransmitter such as glutamate or GABA, and a second peptidergic neuromodulatory molecule such as neuropeptide Y, substance P, or cholecystokinin.
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MafB a member of the
2024-12-17

MafB, a member of the Maf protein family, is essential for terminal differentiation of macrophages (Kelly et al., 2000). The phagocytic activity of polystyrene beads was found to be enhanced in AICAR phosphate with exogenous expression of MafB (Tillmanns et al., 2007). However, in alveolar macropha
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Our data indicate that the D domain only
2024-12-16

Our data indicate that the D1 domain only needs to hydrolyze ATP a few times, or perhaps even just once, during the processing of a given substrate molecule, whereas the D2 domain hydrolyzes ATP many times. Consistent with this model, only D2 contains the canonical aromatic pore loop residues implic
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In HepG cells compound showed
2024-12-16

In HepG2 cells, glucokinase showed inhibition of total lipid syntheses with an IC of 8μM. A cell based Alamar Blue cytotoxicity assay was used in parallel to differentiate the effect on the inhibition of lipid synthesis versus potential cytotoxicity. Under identical incubation conditions, compound s
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Bioavailability has been defined as the amount of a
2024-12-16

Bioavailability has been defined as the amount of a drug given by any route, other than intravenously, that reaches general circulation and is available at the site of action [86]. The low bioavailability observed with the initial intravaginal devices (16%) was attributed to the melting point of the
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Introduction It has long been
2024-12-16

Introduction It has long been recognized that angiogenesis is critical to the growth, progression, and metastasis of many solid tumor types [1], and thus, drugs targeting the angiogenic pathway have been a topic of clinical investigation in the oncology community for many years. Angiogenesis is reg
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Since natural and recombinant glycoprotein hormones exhibit
2024-12-16

Since natural and recombinant glycoprotein hormones exhibit some differences in their carbohydrate structures, we checked whether this could affect the permissive effect on FSK-induced cyclic AMP response in MLTC-1 cells. Fig. 6 shows that the same sensitizing effect to FSK is observed with pituitar
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5-Ethynyl-2'-deoxyuridine The most widely recognized eff
2024-12-16

The most widely recognized effects of adenosine are operated through inhibiting A1R, one of the most abundant G protein-coupled receptors in 5-Ethynyl-2'-deoxyuridine tissue [53]. A1R are located presynaptically, postsynaptically and nonsynaptically [54]. Effect of adenosine in neuronal circuits of
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At the last follow up nine patients had discontinued
2024-12-13

At the last follow-up, nine patients had discontinued pyridostigmine within the first year postoperatively. Only one patient required pyridostigmine at a higher dose, but this was accompanied by successful weaning of prednisolone. None of the 5 patients who were on pyridostigmine treatment alone pri
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br ARIs in the prevention of
2024-12-13

5ARIs in the prevention of prostate cancer Prostate cancer continues to be a leading cause of male deaths worldwide. In 2009, it was estimated there would be 192,280 new cases of prostate cancer with a predicted 27,360 deaths [25]. Because androgens, and specifically DHT, play a large role in bot
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Finasteride was the first steroidal
2024-12-13

Finasteride (13) was the first steroidal 5α-reductase inhibitor approved by the US Food and Drug Administration (FDA) in 1992 for treatment of BPH. In fact, long term clinical studies with this drug demonstrated a sustained reduction of the prostatic specific antigen and an overall improvement in B
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Aurora A and B are required
2024-12-13

Aurora A and B are required for the control of mitosis whereas Aurora C is mainly invoved in meiosis (Goldenson and Crispino, 2015). Interestingly, Aurora B is partnered with inner centromere protein (INCENP), survivin and Borealin to form a chromosomal passenger complex (CPC) that is critical for
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