• A high throughput small molecule ACK biochemical inhibition

  2024-04-26

  

  A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found sodium channel to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work w

• Loxapine br Acknowledgements br Introduction Autoantibodies

  2024-04-26

  

  Acknowledgements Introduction Autoantibodies directed at neurotransmitter receptors and ion channels are pathogenic and/or biomarkers in several autoimmune neurological diseases [1]. For example, autoantibodies directed against voltage-gated potassium channels, the P/Q-type (α1A) voltage-gated

• With the treatment options available today including a combi

  2024-04-26

  

  With the treatment options available today including a combination of symptomatic treatments and general immunosuppression, many MG patients can lead productive lives [1], [4], [20]. The frequency of death has decreased due to improved management and detection of milder cases. At present, the overal

• Compounds were profiled for their

  2024-04-26

  

  Compounds – were profiled for their inhibitory activity against dipeptidyl peptidase-IV Activity and/or Structure Homologues (DASH) [e.g. DPP2, DPP8 and DPP9] and non-DASH [eg. post-proline cleaving enzyme (PPCE), neutral endopeptidase (NEP), aminopeptidase P (APP), aminopeptidase N (APN)] enzymes.

• The gene SRD A encodes the

  2024-04-26

  

  The gene SRD5A2 encodes the 5-α-reductase enzyme, which converts testosterone into dihydrotestosterone. Although dihydrotestosterone levels are considerably lower than testosterone, dihydrotestosterone has a five-fold stronger binding capacity to the androgen receptor and, thereby, a considerably mo

• Because the V ATPase inhibitors that have

  2024-04-26

  

  Because the V-ATPase inhibitors that have been employed in these studies (including bafilomycin and concanamycin), are membrane permeant, they inhibit all the V-ATPases in the cell. This is important since it is possible that intracellular V-ATPases, in addition to those present at the plasma membra

• Acknowledgments br Introduction Prostate cancer is the first

  2024-04-26

  

  Acknowledgments Introduction Prostate cancer is the first leading cause of cancer-related deaths among males in the UK and the second in the US. Despite recent advances in surgery, radiation, medical management and screening, prostate cancer patients suffer high morbidity and mortality and signi

• Bexarotene Although apelin g kg shows negative early and

  2024-04-26

  

  Although apelin 60μg/kg shows negative (early) and positive (late) inotropic effects, since ERK1/2 phosphorylation starts at the min 5 of administration [6], ERK1/2 phosphorylation mediate positive inotropic effects of apelin 60μg/kg. After the simultaneous inhibition of KOR and APJ the phosphoryla

• Although the earlier studies focused on the antioxidant capa

  2024-04-26

  

  Although the earlier studies focused on the antioxidant capacity of tocopherols, ascorbic PAC-1 and carotenoids, then it was noticed that phenolic compounds were more powerful than others (Rice-Evans, Miller, & Paganga, 1996). Phenolic compounds, the most numerous and ubiquitous groups of plant sec

• Thiol are reduced by two major redox systems

  2024-04-26

  

  Thiol are reduced by two major redox systems, glutathione/glutaredoxin (GRX) and thioredoxin (TRX), which have been extensively studied in plants [13], [14], [15]. Glutathione, a thiol-containing tripeptide, exists in a reduced (GSH) or an oxidized form (GSSG). It has a major role as a redox buffer

• br Summary br Introduction With readily

  2024-04-26

  

  Summary Introduction With readily synthetic methods and excellent chemical/physical characteristics, coumarins have received extensive attention and show great practical values in many fields, such as medicine discovery, dye chemistry, materials chemistry and so on [[1], [2], [3]]. Actually, o

• Finally terbinafine is generally associated with a

  2024-04-26

  

  Finally, terbinafine is generally associated with a low index of toxicity and few adverse effects. In humans, only mild GI toxicity and hepatobiliary dysfunction are reported. In red-tailed hawks, oral administration of a high dose of terbinafine (120 mg/kg BW) was furthermore demonstrated to induce

• Another hypothesis is angiogenesis inhibition Angiogenesis i

  2024-04-26

  

  Another hypothesis is angiogenesis inhibition. Angiogenesis is a process that involves the growth, migration and differentiation of endothelial Nimodipine to form new blood vessels. Angiogenesis favorably influences tumor growth and also influences tumor invasion of vessels, resulting in tumor meta

• We have recently begun to

  2024-04-26

  

  We have recently begun to demonstrate this concept by reporting a novel class of β-hairpin peptidomimetics, built on a piperidine-pyrrolidine semi-rigid β-turn inducer [12] and bearing two recognition pentapeptide sequences, designed on oligomeric and fibril structures of Aβ1-42 (compound 1, Fig. 1)

• LOXs and CYPs are a series

  2024-04-25

  

  LOXs and CYPs are a series of iron-containing enzymes that metabolize arachidonic hydralazine hydrochloride to form biologically active products, such as epoxyeicosatrienoic acids (EETs) hydroperoxyeicosatetraenoic acids (HETEs), prostaglandins, leukotrienes and thromboxanes [6]. Among these mediat

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