首页> 外文会议>Conference on Drug Design and Discovery Technologies >MOLECULAR DOCKING BASED SCREENING OF'NITROGEN CONTAINING BISPHOSPHONATE CONJUGATE WITH HYDROXYAPATITE'ACTIVE CONSTITUENTS TOWARDS MEVALONATE PATHWAY IN FINDING POTENT INHIBITORS FOR ANTI-OSTEOPOROTIC ACTIVITY
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MOLECULAR DOCKING BASED SCREENING OF'NITROGEN CONTAINING BISPHOSPHONATE CONJUGATE WITH HYDROXYAPATITE'ACTIVE CONSTITUENTS TOWARDS MEVALONATE PATHWAY IN FINDING POTENT INHIBITORS FOR ANTI-OSTEOPOROTIC ACTIVITY

机译:基于分子对接的筛选“含羟基磷灰石与羟基磷酸盐”活性成分对甲氨酸途径的活性成分,寻找抗骨质疏松活性的有效抑制剂

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Osteoporosis is a skeletal disease causing bone fragility by disturbing micro architecture of the bone by decreasing Bone mineral density(BMD).Osteoporosis is seen commonly in post menopausal women and also in patients with long term use of medications like corticoids termed as glucocorticoid induced osteoporosis.Midst of the disease increases fracture risk and decreases the life expectancy and quality of life.Globally there are 323 million people above the age of fifty were beingaffected with osteoporosis,34 million are at the risk of developing the disease and the number may be increasesup to 1.55 million(310% in men and 240% in women)by 20501.Bisphosphonates(BP's)like Residronate,Ibandronate,Pamidronate,Zoledronic acid andEstrogen patchesare the choice of drugs for treatment of osteoporosis.Nitrogen containing Bisphosphonates aid in the effective treatment of osteoporosis by directly acting on osteoclasts cells by inhibiting the Farnesyl pyrophosphate synthase(FPPS)of melvonate pathway and their ability to bind with the mineral component of bone contributing to their potency of BP's.The P-C-P backbone is responsible for strong affinity towards hydroxyapatite and facilitate potent inhibitory effects.These drugs are having high affinity and strong binding sites towards Hydroxyapatite.Hydroxyapatite is the mineral component present in the bone containing calcium and phosphorus in the ratio of 1.67 and also aid in effective treatment against hypercalcemia,multiple myeloma,metastatic cancer.
机译:骨质疏松症是通过降低骨矿物密度(BMD)骨矿物质密度(BMD)骨髓症,在后绝经妇女中观察到骨骼的微观架构,骨质疏松症是骨骼脆性,并且还在长期使用皮质激素被称为糖皮质激素诱导的骨质疏松症的患者。疾病中期增加了骨折风险并降低了寿命的预期寿命和生活质量.11岁以上的人数超过50.5岁以上的人类患有骨质疏松症,3400万有发展疾病的风险,数量可能会增加。 20501年,1255万(男性310%和240%)到20501.比膦酸盐(BP)如Realtronate,IBANDronate,Pamidronate,唑酮酸和Zoletrogen and Endestrousare选择用于治疗骨质疏松症的药物。含有双膦酸盐的癸酸盐的有效治疗方法有效治疗骨质疏松症通过抑制融合叶酸盐的焦磷酸盐合成酶(FPP)直接作用于骨核苷酸细胞与骨骼矿物成分结合的方式,含有BP的效力的方式。PCP骨架对羟基磷灰石的强烈亲和力负责,促进有效的抑制作用。这些药物具有高亲和力和强的羟基磷灰石的强粘合位点。羟基磷灰石是矿物质组分存在于含钙和磷中的比例为1.67,也有助于有效治疗高钙血症,多发性骨髓瘤,转移性癌症。

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