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A variety of quinazoline or fused pyrimidine substituted dia
2024-06-17
A variety of quinazoline or fused pyrimidine-substituted diaminotriazoles showed sub-100nM inhibition of Axl (). Diaminotriazoles similarly substituted with quinolines, isoquinolines and benzothiazoles also showed potent Axl activity (data not shown), but generally exhibited potent cytotoxicity and
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IC values were obtained for an expanded version of the
2024-06-17
IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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The allosteric site of class C receptors
2024-06-17
The allosteric site of class C receptors is generally located on the extracellular side of the TM domain (Brauner-Osborne et al., 2007, Christopher et al., 2015, Dore et al., 2014, Gregory et al., 2011, Harpsoe et al., 2017, Kniazeff et al., 2011, Pin and Prezeau, 2007, Urwyler, 2011, Wu et al., 201
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br Conclusions and future direction ER PgR breast
2024-06-17
Conclusions and future direction ER(−)/PgR(+) breast cancers have a distinct clinical course, response to treatment, and molecular features when compared to other breast cancer types, however some of them are actually technical artifacts or consequences of too high definitions of positivity. Acco
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As aforementioned this study aimed to design synthesize and
2024-06-17
As aforementioned, this study aimed to design, synthesize and investigate aromatase inhibitory and anti-breast cancer activities of N,N′-disubstituted thiourea derivatives. Based on the attractive phenotypic molecule 1, the synthetic N,N′-disubstituted thioureas have been designed including monothio
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br Identification of the croaker mAR cDNA Testosterone T was
2024-06-17
Identification of the croaker mAR cDNA Testosterone (T) was observed to alter steroidogenesis through a nongenomic mechanism (not blocked by the transcription inhibitor, actinomycin D) in Atlantic croaker ovarian tissues (Braun and Thomas, 2003). This action of T was mimicked by T conjugated to B
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br Role of AR in models of neointima
2024-06-17
Role of AR in models of neointima formation Investigations into the pathogenesis of lesion formation have often used acute models of mechanical damage to assess the mechanisms regulating the fibro-proliferative response to arterial injury. Models of acute injury used for this purpose include: lig
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br Experimental Procedures br Acknowledgments br
2024-06-17
Experimental Procedures Acknowledgments Introduction Cellular and molecular mechanisms underlying synaptic plasticity in the 3-Deazaadenosine are thought to be involved in memory acquisition. Synaptic plasticity is categorised into two main types, long-term depression (LTD) and long-term p
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Fish aminopeptidases from Alaska Pollack roe and tuna pylori
2024-06-14
Fish aminopeptidases from Alaska Pollack roe and tuna pyloric caeca have been reported on [12,13]. More recently, we described the purification of a leucine aminopeptidase from the skeletal muscle of the common carp [14], red sea bream [15] and a lysine aminopeptidases from Japanese flounder [16]. T
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br Conflict of interest statement
2024-06-14
Conflict of interest statement Introduction Currently, adenocarcinoma is the most common histological subtype of lung cancer. Activating mutations and translocations with a potential for targeted therapy are reported predominantly in non-smokers. ALK rearrangement is found in less than 5% of u
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The lack of specific PARP inhibitors prevents our
2024-06-14
The lack of specific PARP inhibitors prevents our understanding of how TIPARP or perhaps other PARPs affect AHR signaling. Current inhibitors are based on NAM and were designed to inhibit PARP1 [59]. Many of them do not effectively inhibit mono-ADP-ribosyltransferases and their ability to inhibit TI
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CEP-37440 br Hypothesis The hypothesis is that AhR in
2024-06-14
Hypothesis The hypothesis is that AhR in skin diseases could be an objective of study for future dermatological therapies. Both stimulation and inhibition of the receptor might have significant influences on neoplastic or inflammatory skin diseases. However, at present the functions of AhR are un
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Introduction Glaucoma consists of a
2024-06-14
Introduction Glaucoma consists of a group of eye diseases showing a broad spectrum of clinical presentation and unknown aetiologies, that lead to a permanent loss of visual function due to the death of retinal ganglion latanoprost mg and damage of the optical nerve. It is well accepted that a crit
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Notably our preliminary results confirmed that fluoxetine SS
2024-06-14
Notably, our preliminary results confirmed that fluoxetine (SSRIs, 5–10 mg/kg) and duloxetine (SNRIs, 5–10 mg/kg) could not enhance memory function in the novel object recognition or step-down passive avoidance tasks (data not shown). In the present study, we also found that vilazodone showed had no
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br Expression of ADK in the normal brain
2024-06-14
Expression of ADK in the normal brain In adult brain, ADK is primarily expressed in astrocytes. Immunocytochemical analysis of adult rat and mouse atp enzyme revealed predominant astrocytic expression throughout the hippocampus and cortex. Two isoforms of ADK have been identified in mammals, a lo
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