Department of Pharmacy

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Author: search.filters.author.Gaikwad, Anil BhanudasSubject: search.filters.subject.Cancer

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Now showing 1 - 4 of 4
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    Natural HDAC Inhibitors: Nature’s Answer to the Cancer
    (NMIMS, 2015) Gaikwad, Anil Bhanudas
    Post translational modifications of histones play a significant role in regulation of physiological and pathological processes in the body. Acetylation is one of the most important chromatin modifying mechanisms being controlled by histone acetyl transferases and histone deacetylases. The histone deacetylases (HDAC) are basically responsible for silencing of gene transcription. Cancer involves silencing of a large number of genes. Inhibition of such gene silencing could possibly lead us to alleviatin or control of cancer progression. Natural HDAC inhibitors, a highly researched topic thus seems an attractive method to conquer the kingdom of cancer and thus prove to be the ‘bull’s eye’ like target for cancer treatment
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    Recent developments in using plant-derived natural products as tubulin inhibitors for the management of cancer
    (Elsevier, 2016) Gaikwad, Anil Bhanudas
    Defeating cancer has become a global battle calling for development of new treatment options. Better understanding of the biological processes involved in development of cancer has made it possible to screen various drugs against a wide range of targets. Targeting of microtubule dynamics has remained one of the favorite targets for researchers. Tubulin inhibitors are drugs of choice in many of the treatment strategies employed by the oncologists. Tubulin inhibitors are classified under two types as microtubule stabilizers or destabilizers. Three different sites are identified where these inhibitors binds. Natural sources have played an important role in development of modern medicines for treating various diseases including cancer. Vinca alkaloids, colchicine, and taxane are the first drugs in these categories which are named after different binding sites. Drugs binding to vinca domain and colchicine domain fall under microtubule destabilizers; and those binding to taxane domain fall under microtubule stabilizers. These drugs have served as prototypes for the development of their semisynthetic derivatives which are having wide range of anticancer activities. In present review, various aspects of the natural tubulin inhibitors and their role in development of chemotherapeutic agents for cancer treatment are discussed.
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    PARG inhibitors’ success: a long way to go!
    (Bentham Science, 2014) Gaikwad, Anil Bhanudas
    Poly(ADP-ribosyl)ation is one of the most pertinent post translational modifications involved in regulation of chromatin structure, cell cycle progression, tissue development and differentiation and other vital biological phenomena. The enzymes that catalyze the synthesis and degradation of poly(ADP) ribose polymers are PARP and PARG, respectively. The role of PARP has been implicated in development of various diseases since a long time and hence it has evolved as an important pharmacological target but a plethora of drawbacks associated with PARP inhibitors compelled the shift of focus towards PARG. Recently PARG has evolved as an alternative target to overcome the hurdles being faced in the treatment of various conditions like multiple organ failure, ischemic organ damage, diabetic nephropathy, neurodegenerative diseases and cancer. The review provides a compendium on PARG, its mode of action, inhibitors, and its therapeutic applications and also discusses the reasons due to which PARG inhibitors have not been able to reach the clinical trials. PARG inhibitors, though far from success, definitely appear as alluring topics for further research as PARG emerges out as an eminent pharmacological target in making which can shape the future of medicines to provide better therapy with reduced side effects and more efficiency.
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    Change in post-translational modifications of histone H3, heat-shock protein-27 and MAP kinase p38 expression by curcumin in streptozotocin-induced type I diabetic nephropathy
    (Wiley, 2009-01) Gaikwad, Anil Bhanudas
    Curcumin has been used to treat cancer, diabetes and other pathologies. However, little is known regarding its role in altering post-translational modifications of histone H3. A recent report suggests that acute hyperglycaemia induces a global down-regulation of gene expression in human tissues and epigenetic regulation of gene expression could be a novel mechanism underlying the pathological processes of hyperglycaemia. The present study was undertaken to examine changes in histone modification by curcumin treatment which prevents development of type I diabetic nephropathy.