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mecamylamine An alternative to the agonist or antagonist
2024-06-07

An alternative to the agonist or antagonist potential in drug discovery is the positive allosteric modulator (PAM) approach, which can augment the normal processes of neurotransmission as opposed to directly replacing or antagonizing them. PAMs are thought to bind to sites that are distinct from the
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Consistent with the observation that mutations in the redox
2024-06-07

Consistent with the observation that mutations in the redox-partner binding site of P450c17 that reverse charge from basic to acidic (R347H, R358Q) cause 17,20-lyase deficiency (Geller et al, 1997, Geller et al, 1999), at least one POR mutation that changes a residue in the FMN domain from neutral t
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In this paper we describe the
2024-06-07

In this paper, we describe the formation of a structure-based pharmacophore which lead to the discovery of several hydrophobic, yet non-lipid inhibitors of ATX. These compounds docked within the same volume occupied by the initial non-lipid inhibitors of ATX used to build the pharmacophore. Violatio
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On the contrary evidence also suggests that
2024-06-07

On the contrary, evidence also suggests that autophagy plays a striking protective role in cancer cells. Highly burgeoning cancer nuciferine synthesis require cellular building blocks for their metabolism and energy production. At this stage of cancer development, autophagy acts as a friend providin
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Granzyme B Inhibitor Z-AAD-CH2Cl receptor Jesus et al discov
2024-06-07

Jesus et al. discovered a new series of azaindole as Aurora inhibitors through various modification of GSK1070916 (47). They synthesized series from modification of the GSK1070916 and evaluated for in-vitro Aurora-B/INCENP and Aurora-A/TPX2 inhibition assays. Modified Granzyme B Inhibitor Z-AAD-CH2C
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br Experimental section br Acknowledgments br Introduction A
2024-06-07

Experimental section Acknowledgments Introduction Adipose is a major endocrine organ which releases a range of bioactive agents [1]. Selected adipose depots have been established as sites of sex steroid metabolism [1]. Subcutaneous and visceral adipose express high levels of aromatase, cap
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br Funding This work was supported by
2024-06-06

Funding This work was supported by the National Natural Science Foundation of China (grant No. 81573664). Thanks to Jing-xian Yang from the Pharmacology Laboratory of Liaoning University of Traditional Chinese Medicine for support with technology and experimental equipment. Disclosure Confl
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br Materials and methods br Results and discussion
2024-06-06

Materials and methods Results and discussion First, we examined whether hypothalamic Akt-mediated signaling pathways are regulated postprandially in chickens. Refeeding significantly (P Spectinomycin hydrochloride hydrate concentrations significantly increased in chicks after 1 h of refeeding
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The functional observations from the
2024-06-06

The functional observations from the present study are based on neoplastic pentylenetetrazol australia (HSY), and comparative expressions between normal salivary and pleomorphic adenoma tissues. However, there is a paucity of information on AhR expression and function in normal salivary gland, not
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In a recent series of
2024-06-06

In a recent series of studies from our laboratory, to characterize the contractile systems within the rat SecinH3 wall, three conditions were identified that led to detrusor activity: spontaneous micro-contractions, electrical field stimulated (EFS) contractions and muscarinic agonist induced contr
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br Functional consequences of ADK regulation
2024-06-06

Functional consequences of ADK regulation on astrocyte function As outlined above (see introduction), ADK critically regulates the extracellular adenosine levels in NADP/NADPH Quantitation Colorimetric Kit (Boison, 2006, Etherington et al., 2009). Changes in the levels of adenosine, as a result
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While the direct effects of ARI lead to a
2024-06-06

While the direct effects of 5-ARI lead to a dramatic Amyloid β-Peptide (1-42) in serum DHT levels, other laboratory values are also affected by 5-ARI use. Serum testosterone elevations are known to occur with both finasteride and dutasteride use, but values will typically remain within the normal la
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Drug resistance development often involves structurally
2024-06-06

Drug resistance development often involves structurally un-related drugs and, specifically both conventional and targeted agents. IGROV-1/Pt1 Trehalose are characterized by resistance to cisplatin and reduced sensitivity to inhibitors of EGF-R and MEK, the up-stream activator of ERK1/2, associated w
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Fourth non canonical sites may be targeted Classical benzodi
2024-06-05

Fourth, non-canonical sites may be targeted. Classical benzodiazepines require the presence of a γ subunit for high-affinity binding, which limits their activity to a specific large pool of receptor isoforms, leaving other isoforms unaffected. In particular, δ subunit-containing receptors, as well a
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Researchers demonstrated that mitochondria are the
2024-06-05

Researchers demonstrated that mitochondria are the main producers of ROS and are the most sensitive to the effects of ROS. Mitochondria-mediated apoptosis may not be limited to the role of cytochrome c in the activation of caspase-3 and ROS may provide an alternate mitochondrial signaling pathway (H
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