加拿大代写被抓:P-gp在MDR中发挥的作用

加拿大代写被抓:P-gp在MDR中发挥的作用

P-gp在MDR中发挥的作用导致了对P-gp活性的调节。为解决这一问题,合成了几种已知具有P-gp抑制活性的化合物。第一代抑制剂是一种具有药理活性的化合物,尽管研究的目的不同,但仍提供了抑制P-gp的证据。然而,显著的肾毒性和免疫抑制作用,心脏毒性,较差的特异性和低效力的转运药物流出最终限制了他们的临床应用。


加拿大代写被抓:P-gp在MDR中发挥的作用

化疗可作为治疗转移性和局限性癌症的主流方法。然而,由于肿瘤药物在无肿瘤区域的定位不明确,导致肿瘤细胞对多种药物产生耐药性,并伴有全身毒性副作用,是目前面临的主要挑战。MDR的发生可能是由于药物外排的转运体在药物外排中起作用。这导致细胞内药物积累减少,治疗效果降低。


加拿大代写被抓:P-gp在MDR中发挥的作用

The role played by P-gp within MDR has resulted in efforts for modulating the activity of P-gp. Several compounds known for possessing the inhibitory activities of P-gp are synthesized specifically for addressing this problem. Inhibitors of first generation are compounds active pharmacologically which provided evidence of inhibiting P-gp even though being researched for different purposes. However, significant nephrotoxic and immunosuppressive effects, cardiac toxicities, poor specificity and low potencies for transporters of drug efflux end up limiting their clinical application.

加拿大代写被抓:P-gp在MDR中发挥的作用

Chemotherapy can be identified as the mainstream approach for treating metastasized and localized cancers. However, the establishment of resistance from multiple drugs by cancer cells along with side effects of systemic toxic take place due to unspecific localization of such drugs to areas without tumor is major challenges. There can be occurrence of MDR by transporters of drug efflux which are active in effluxing out drug. This results in reducing the accumulation of intracellular drugs and decreasing the level of therapeutic efficacy.

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