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As we previously observed in the
2023-08-18

As we previously observed in the NSFT (Fukumoto et al., 2014), the effect of LY341495 in the FST was also inhibited by a 5-HT1A receptor antagonist, indicating the role of the 5-HT1A receptor in the actions of LY341495. Among the 5-HT1A receptors, which exist both presynaptically and postsynapticall
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Given the powerful and ubiquitous nature of
2023-08-18

Given the powerful and ubiquitous nature of adenosine action within the CNS, basal levels of extracellular adenosine are carefully regulated and are estimated to be in the region of 30–300 nM (Fredholm et al., 2001). The two main pathways for the control of extracellular adenosine involve phosphoryl
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Entrectinib receptor br Discussion Mycobacterium tuberculosi
2023-08-18

Discussion Mycobacterium tuberculosis infection is a main threat to mankind, with one third of the world population being infected. [9] Over nine million new cases of tuberculosis and two million deaths from this disease occur yearly worldwide. [10] The rising incidence of tuberculosis over the l
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As a continuation of our search for a selective AChE
2023-08-18

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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dfmo Acknowledgements The work was supported
2023-08-18

Acknowledgements The work was supported by grants from Swedish Research Council (J.Z.H.) (A.R.M.). We thank Protein Science Facility (PSF), Department of Medical Biochemistry and Biophysics, Karolinska Institute, Stockholm, Sweden. We thank Prof. Ralf Morgenstern (Department for Environmental Medic
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br Funding br Introduction l Dihydroxyphenylalanine l
2023-08-18

Funding Introduction l-3,4-Dihydroxyphenylalanine (l-DOPA) is the gold-standard treatment for the motor symptoms of Parkinson's disease (PD); however, its chronic use induces severe motor complications that eventually limit its long-term efficacy (Bastide et al., 2015). The most disabling side
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The resolution cocrystal structure of ACL
2023-08-18

The 2.10Å resolution cocrystal structure of ACL in complex with citrate indicates that the carboxyl (COH) groups of citrate forms a network of H-bonds with hydrophilic residues surrounding the ACL citrate binding domain (CBD) (A). The - carboxyl group forms a salt bridge with the guanidine moiety of
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Introduction An association of elevated
2023-08-18

Introduction An association of elevated branched-chain Sulforaphane (BCAA—Leu, Val, Ile) with obesity and insulin resistance was first reported nearly 50 years ago (Felig et al., 1969). With the advent of metabolomics technologies, it has since become apparent that the association of BCAA and rela
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Thus phosphorylation of p was used to
2023-08-18

Thus, phosphorylation of p38 was used to measure the intracellular potency of ASK1 inhibitors. In this assay, HEK293/AP-1luc Cy3 RNA expressing human full-length ASK1 were incubated with compound for 18 h and then lysed and the level of phospho-p38 was quantified using the HTRF assay [33]. Resul
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We found a protective effect of the
2023-08-18

We found a protective effect of the GTCC haplotype against ED, which is reflected by its association with increased IIEF in patients with clinical ED. Further studies are required to determine the functional implications of these genetic markers combined in specific haplotypes blocks. Indeed, we fou
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The current study was designed to investigate the effects
2023-08-17

The current study was designed to investigate the effects of the 12/15-LOX inhibitor, LOXBlock-1 (LB1) in mice using a FeCl3-induced distal MCAO model, and to test its utility in conjunction with subsequent thrombolysis with tPA, which is to date the only FDA-approved drug for acute stroke treatment
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stat3 inhibitor br Neurological development and BCAAs Glutam
2023-08-17

Neurological development and BCAAs Glutamate is an important excitatory neurotransmitter in the brain, and BCAAs (especially leucine) function to synthesize glutamate in astrocytes around neurons, since leucine enters the brain from the blood more rapidly than other stat3 inhibitor and provides
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T16Ainh - A01 br Concluding remarks The past decade has seen
2023-08-17

Concluding remarks The past decade has seen rapid advances in our understanding of the metabolic reprogramming that occurs during tumorigenesis. Strategies to target specific nodes of cancer cell amino T16Ainh - A01 metabolism have progressed from preclinical studies to clinical trials, and are
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br Results and discussion br Conclusion The tyrosine kinase
2023-08-17

Results and discussion Conclusion The tyrosine kinase ALK represents one of the most successful molecular targets for the development of precise medicine to treat stratified subgroups of cancer patients. Three generations of ALK inhibitors have been awarded the FDA's approval or are being exte
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To date defining the prognostic
2023-08-17

To date, defining the prognostic impact of molecular drivers of early-stage NSCLC has been challenging due to the relative rarity of these subsets and the redefinition of comparator arms over time as understanding of the molecular drivers of NSCLC evolved. Indeed, use of molecularly heterogeneous co
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