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br Conclusions In summary aromatase mRNA
2023-03-27
Conclusions In summary, aromatase mRNA expression in the cid calculator receptor of A. leptorhynchus shows a similar distribution pattern as seen in other teleosts with expression detected in the forebrain and the pituitary gland. The lack of aromatase mRNA expression in the midbrain and hindbra
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Recently two distinct small molecule inhibitors of PHGDH wer
2023-03-22
Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer Urolithin A with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces the gro
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br Mechanisms for regulation of intracellular cholesterol ho
2023-03-22
Mechanisms for regulation of intracellular cholesterol homeostasis Cells maintain intracellular free cholesterol levels and distribution within stringent tolerances by several mechanisms [55]: (1) uptake of native LDL (the major extracellular carrier of cholesterol) by LDL receptors and modified
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Sphingolipids such as ceramides and glucosylceramides are an
2023-03-22
Sphingolipids, such as ceramides and glucosylceramides, are an important class of bioactive lipids. The levels of these lipids change as a function of adipose tissue mass and functionality, and are partially driven by cellular availability of palmitoyl-CoA. Aberrant accumulation of ceramide, glucosy
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ADOR immunoreactivity was high in parasympathetically innerv
2023-03-22
ADOR immunoreactivity was high in parasympathetically-innervated smooth muscle, namely the iris sphincter muscle and the ciliary muscle. No ADOR immunoreactivity was noted in the sympathetically-innervated iris dilator muscle. Immunoreactivity against all four ADORs was noted in the ciliary epitheli
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In conclusion two novel series of furo pyrimidin
2023-03-22
In conclusion, two novel series of furo[2,3-]pyrimidin4-amines and 7-pyrrolo[2,3-]pyrimidin-4-amines which exhibit potent in vitro inhibitor activity against ACK1 have been identified and evaluated. 1,3-Dithiolane-substituted pyrrolopyrimidine displays excellent ACK1 cellular inhibition, good kinas
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Although effects of low concentrations of agonist were not
2023-03-22
Although effects of low concentrations of agonist were not as thoroughly documented for heteromeric receptors such as the major naloxone hydrochloride α4β2 nAChR, a similar mechanism of action was described to explain the potentiation of these receptors with low concentrations of acetylcholine-este
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fty720 Cancer cells manifest characteristic abnormal growth
2023-03-22
Cancer fty720 manifest characteristic abnormal growth properties accompanying clonal evolution of cells displaying progressively increasing genomic instability capable of invasion and metastasis to distant organ sites. With the emerging knowledge about the role of known oncogene and tumor suppressor
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Significant reductions in GYN cancer patient mortality and m
2023-03-22
Significant reductions in GYN cancer patient mortality and morbidity rates require treatments that proactively prevent and reverse resistance to chemotherapy and radiation. Combining chemotherapy and radiation with inhibitors of key DDR proteins targets is likely to enhance the ability of genotoxic
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Bikinin sale Since ARBs strongly reduce inflammation it was
2023-03-20
Since ARBs strongly reduce inflammation, it was hypothesized that the protective effects on cognition were the result of reduction of inflammation and amelioration of neurogenic decrease. However, ARB treatment did not normalize increased inflammation and neurogenic loss. For this reason, the protec
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br AR expression in breast tissue Although
2023-03-20
AR expression in breast tissue Although androgenic signalling is chiefly associated with the development and maintenance of primary and secondary male characteristics, especially during puberty when the testes are by far the major source of testosterone, the AR also plays important functions in f
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The increased occurrence of ARIA
2023-03-20
The increased occurrence of ARIA-E in APOE ε4 carriers in phase 2 studies resulted in separate protocols for carriers and noncarriers in the subsequent phase 3 studies. Two 18-month trials comprising 1121 carriers and 1331 noncarriers with mild to moderate AD tested doses of bapineuzumab that varied
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ALK fusion positive NSCLC is clinically
2023-03-20
ALK fusion-positive NSCLC is clinically actionable because it can be targeted by several FDA-approved drugs, including the first generation TKI crizotinib, which is a dual inhibitor to MET and ALK [15], and the second generation inhibitors, alectinib and ceritinib, both of which are highly-selective
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The aldehyde reductase AKR A and aldose reductase AKR
2023-03-20
The aldehyde reductase (AKR1A1) and aldose reductase (AKR1B1) belong to aldo-ketoreductase (AKR) superfamily catalyzing the reduction of corresponding aldehydes and ketones involved. Both the closely related enzymes AKR1A1 and AKR1B1 have 65% structural similarity and differ only at the active site.
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Interestingly intermittent high doses of AKT inhibitors have
2023-03-20
Interestingly, intermittent high doses of AKT inhibitors have been shown to be a more effective strategy both clinically and pre-clinically. High doses appear to be required for induction of apoptosis and intermittent schedules overcome the low therapeutic index of these compounds. This is particula
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