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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Published:19 Nov 2019
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Special Collection: 2019 ebook collection
A. Kalyani, S. Bharath, and P. Parasuraman, in Conference on Drug Design and Discovery Technologies, ed. M. Murahari, L. Sundar, S. Chaki, V. Poongavanam, P. Bhat, and U. Y. Nayak, The Royal Society of Chemistry, 2019, pp. 64-68.
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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 being affected with osteoporosis, 34 million are at the risk of developing the disease and the number may be increases up to 1.55 million (310% in men and 240% in women) by 2050. Bisphosphonates (BP’s) like Residronate, Ibandronate, Pamidronate, Zoledronic acid and Estrogen 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.