Search Results - "Bhamidipati, Somasekhar"
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Regulation of bone homeostasis by MERTK and TYRO3
Published in Nature communications (12-12-2022)“…The fine equilibrium of bone homeostasis is maintained by bone-forming osteoblasts and bone-resorbing osteoclasts. Here, we show that TAM receptors MERTK and…”
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Metabolism of Fostamatinib, the Oral Methylene Phosphate Prodrug of the Spleen Tyrosine Kinase Inhibitor R406 in Humans: Contribution of Hepatic and Gut Bacterial Processes to the Overall Biotransformation
Published in Drug metabolism and disposition (01-07-2010)“…The metabolism of the spleen tyrosine kinase inhibitor…”
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R723, a selective JAK2 inhibitor, effectively treats JAK2V617F-induced murine myeloproliferative neoplasm
Published in Blood (23-06-2011)“…The activating mutations in JAK2 (including JAK2V617F) that have been described in patients with myeloproliferative neoplasms (MPNs) are linked directly to MPN…”
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Tuning the Reactivity of Nuclear Factor Erythroid 2‑Related Factor 2 (Nrf2) Activators for Optimal in Vivo Efficacy
Published in ACS medicinal chemistry letters (14-12-2023)“…Dimethyl fumarate 1 is approved for the treatment of multiple sclerosis but is also associated with off-target activation of the niacin receptor. By using a…”
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Blockade of Mer By the Small Molecule Inhibitor R992 Inhibits Multiple Myeloma and Its Associated Bone Disease By Restoring the Perturbed Bone Homeostasis
Published in Blood (29-11-2018)“…Despite many therapeutic advances in recent years Multiple Myeloma (MM) still remains incurable in the majority of the patients. In addition, MM patients…”
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R970, A Selective Activator of Nrf2, is Efficacious in a Murine Model of Multiple Sclerosis
Published in The Journal of immunology (1950) (01-05-2016)“…Abstract The transcription factor Nrf2 (nuclear factor erythroid-derived-2-like 2) is a key mediator of the anti-oxidant response. Nrf2 can be activated by…”
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Abstract 4869: Small molecule inhibitors of the anti-inflammatory TAM receptor MerTK
Published in Cancer research (Chicago, Ill.) (15-07-2016)“…Abstract Introduction: MerTK, a TAM (Tyro3, Axl, MerTK) family RTK, is expressed on phagocytic myeloid and epithelial cells. Its normal function is to dampen…”
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Design, synthesis of diaminopyrimidine inhibitors targeting IgE- and IgG-mediated activation of Fc receptor signaling
Published in Bioorganic & medicinal chemistry letters (15-05-2015)“…[Display omitted] Using cultured human mast cells (CHMC) the optimization of 2,4-diaminopyrimidine compounds leading to 22, R406 is described. Compound 22 is a…”
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In vitro and in vivo characterization of small molecule inhibitors of the anti-inflammatory TAM receptor MerTK
Published in The Journal of immunology (1950) (01-05-2016)“…Abstract MerTK, a TAM (Tyro3, Axl, MerTK) family RTK, is expressed on phagocytic cells. Its normal function is to dampen innate immune responses to…”
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Application of cultured human mast cells (CHMC) for the design and structure–activity relationship of IgE-mediated mast cell activation inhibitors
Published in Bioorganic & medicinal chemistry letters (15-05-2015)“…[Display omitted] Here we report the optimization of small molecule inhibitors of human mast cell degranulation via anti-IgE-mediated tryptase release…”
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Efficacy of R723, a Potent and Selective JAK2 Inhibitor, in JAK2V617F-Induced Murine MPD Model
Published in Blood (20-11-2009)“…Abstract 3897 Poster Board III-833 The V617F mutation of JAK2 (JAK2-V617F) occurs at a high frequency in Philadelphia chromosome-negative myeloproliferative…”
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In Vitro and in Vivo Inhibition of JAK2 Signaling by Potent and Selective JAK2 Inhibitor
Published in Blood (16-11-2008)“…Recent advances in understanding the role of JAK2 V617F mutation in Bcr-Abl negative myeloproliferative (MPD) diseases pathogenesis opened up a possibility to…”
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