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br ACK inhibitors Since ACK activation is
2024-01-16
ACK1 inhibitors Since ACK1 activation is correlated with poor prognosis in various cancers, strong efforts are being directed by multiple groups towards developing highly potent and specific small molecule inhibitors targeting the ACK1 kinase. At least eight small molecule kinase inhibitors have
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Toxicity is the main reason for the failure at
2024-01-16
Toxicity is the main reason for the failure at all stages of the new drug development process. The major part of safety-related attrition occurs at preclinical phases while predicting preclinical safety liabilities earlier in the drug development process. This strategy enables the design and/or sele
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REM sleep is proposed to create an environment
2024-01-16
REM sleep is proposed to create an environment to facilitate plasticity processes that create a generalized downregulation of synaptic strength (Grosmark et al., 2012; Tononi and Cirelli, 2014), while synapses are upregulated specifically by the reactivation of neuronal firing sequences experienced
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br ARIs in the prevention of prostate cancer Prostate cancer
2024-01-16
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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Anti LT therapy by LO inhibition has been hampered
2024-01-16
Anti-LT therapy by 5-LO inhibition has been hampered by occurring liver toxicities by Zileuton or the clinical phase II compound Atreleuton [36], [37] However both compounds possess a thiophene as well as an N-hydroxyurea moiety. These features could be linked with reactive thiophene intermediates [
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The central problem in amnesia developing
2024-01-16
The central problem in amnesia developing following impairment of long-term memory consolidation or reconsolidation is a question of the underlying mechanisms, whether it is caused by impairment of retrieval or memory storage mechanisms [3,8,9,[15], [16], [17], [18]]. To answer this question, severa
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Since innate immune responses represent the first defense ag
2024-01-16
Since innate immune responses represent the first defense against incoming infectious microorganisms, they are particularly engaged during the early stages of viral infections. Many innate defense mechanisms rely on the engagement of pattern recognition receptors (PRRs) which are conserved, germ lin
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br Results br Discussion br Conclusion The flux of
2024-01-16
Results Discussion Conclusion The flux of glucose into cytosolic short chain acyl-CoAs was maintained in pure beta histamine receptors in the presence of inhibition of ATP citrate lyase with hydroxycitrate and also in a cell line with >90% ATP citrate lyase knockdown suggesting that a path
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br Introduction Throughout early prophase I meiotic cells
2024-01-16
Introduction Throughout early prophase I, meiotic cells intentionally generate DSBs as part of a stringently controlled process to initiate homologous recombination (HR). HR is a critical DSB repair pathway that ultimately permits the exchange of genetic information between homologous chromosomes
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br Extracellular domain architecture The extracellular regio
2024-01-16
Extracellular domain architecture The extracellular region of GABAB receptor exists in a heterodimeric configuration regardless of interactions within the rest of the protein (Geng et al., 2012, Liu et al., 2004, Nomura et al., 2008). The extracellular domains of the GABAB1 and GABAB2 subunits ar
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Maduramicin is a polyether ionophore antibiotic that
2024-01-16
Maduramicin is a polyether ionophore antibiotic that has the smallest margin of safety between the maximum authorized dosage and the minimum toxic concentration. Clinical signs of maduramicin intoxication are similar to that of other ionophores, often causing feed refusal, anorexia, respiratory dist
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br HIF Blockade in AA
2024-01-16
HIF-α Blockade in AA Therapy In lieu of the evidence supporting a central role for HIF-α signaling in tumor angiogenesis and CC pathobiology, significant efforts have focused on the discovery of small-molecule HIF-α inhibitors (for exhaustive compendia, see [28,44,45]). In brief, inhibitors vary
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br Combination Effective RAS inhibition which is
2024-01-16
Combination Effective RAS inhibition, which is important for YM 155 receptor control as well for the management of associated illnesses, can be produced through proper selection and dose maintenance and also by the combination with other antihypertensive agents along with continuous monitoring fo
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Previous studies have thus demonstrated that
2024-01-16
Previous studies have thus demonstrated that AR activation generally correlates with the promotion of urothelial carcinogenesis and cancer growth. In this article, we review available data suggesting their modulation through the AR pathway as well as correlations of AR signals with sensitivity to co
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In the present study AP
2024-01-16
In the present study, AP31-B preferentially released hydrophobic 3,4-DAA such as leucine and alanine from N-terminal of peptide (Fig. 4). The debittering ability of AP31-B seemed to depend on such substrate specificity, but additional tests against other hydrophobic amino acids are needed to confirm
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