Výsledky vyhledávání - "Selvi Pradeepan"

Investigating Nephrotoxicity of Polymyxin Derivatives by Mapping Renal Distribution Using Mass Spectrometry Imaging

Autor: Harish Shankaran, Abhishek G. Sathe, Jennifer C. Sasaki, Aixiang Xue, Per E. Andrén, Selvi Pradeepan, Anna Nilsson, Richard J. A. Goodwin, Natalie Keirstead, Anshul Gupta, Richard T. Gallagher, John G. Swales

Publikováno v: Chemical Research in Toxicology. 28:1823-1830

Colistin and polymyxin B are effective treatment options for Gram-negative resistant bacteria but are used as last-line therapy due to their dose-limiting nephrotoxicity. A critical factor in developing safer polymyxin analogues is understanding accu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f6815c5fe363edb205bfddb745649e05
https://doi.org/10.1021/acs.chemrestox.5b00262

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SAR of Carbon-Linked, 2-Substituted Purines: Synthesis and Characterization of AP23451 as a novel Bone-Targeted Inhibitor of Src Tyrosine Kinase With In Vivo Anti-Resorptive Activity

Publikováno v: Chemical Biology & Drug Design. 71:97-105

Targeted disruption of the pp60(src) (Src) gene has implicated this tyrosine kinase in osteoclast-mediated bone resorption and as a therapeutic target for the treatment of osteoporosis and other bone-related diseases. Here, we describe structure acti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9dcdeae0a92758c4ad04f2c1f5760a13
https://doi.org/10.1111/j.1747-0285.2007.00615.x

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Bone-Targeted pyrido[2,3-d]pyrimidin-7-ones: potent inhibitors of Src tyrosine kinase as novel antiresorptive agents

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 13:3071-3074

The design of bone-targeted pyrido[2,3-d]pyrimidin-7-ones as Src tyrosine kinase inhibitors is described. Leveraging SAR from known compounds and using structure-based methods, we were able to rapidly incorporate bone binding components, which mainta

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::557b75ac7c90bb0fb12e38e1f0a1e1cc
https://doi.org/10.1016/s0960-894x(03)00649-8

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Novel phosphate ester-linked resins: The solid-phase generation of phenyl phosphate-containing compounds for SH2 inhibition

Autor: Taylor Merry, Selvi Pradeepan, Raji Sundaramoorthi, Virginia A. Jacobsen, Mayumi Uesugi, Vaibhav Varkhedkar, Chi B. Vu, Chester A. Metcalf, Jeremy Green, Dennis A. Holt, Edgardo Laborde, Karina J. Macek, Yinka Green

Publikováno v: Tetrahedron Letters. 39:3435-3438

An efficient method for the preparation of protected phosphate ester-linked resins in high yield and purity is presented. Variation in tether length/functionality and substitution pattern of the phenol precursors, as well as mild deprotection conditi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::fa37765070d233783f49b9f5cf51fb75
https://doi.org/10.1016/s0040-4039(98)00586-3

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In vivo validation of thymidylate kinase (TMK) with a rationally designed, selective antibacterial compound

Publikováno v: ACS chemical biology. 7(11)

There is an urgent need for new antibacterials that pinpoint novel targets and thereby avoid existing resistance mechanisms. We have created novel synthetic antibacterials through structure-based drug design that specifically target bacterial thymidy

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::96acd05fda8527b11dfa95167c4cf354
https://pubmed.ncbi.nlm.nih.gov/22908966

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Bone-targeted 2,6,9-trisubstituted purines: novel inhibitors of Src tyrosine kinase for the treatment of bone diseases

Autor: Chester A. Metcalf, Ukti Mani, Shiela M. Violette, Tomi K. Sawyer, Susan Adams, Yihan Wang, Terence P. Keenan, Regine S. Bohacek, Marie Rose van Schravendijk, Mary K. Ram, David C. Dalgarno, Selvi Pradeepan, Raji Sundaramoorthi, William C. Shakespeare, Jeffrey A. Keats, Surinder S. Narula, Chad Haraldson, Manfred Weigele, Shuenn Liou

Publikováno v: Bioorganicmedicinal chemistry letters. 13(18)

Novel bone-targeted 2,6,9-trisubstituted purine template-based inhibitors of Src tyrosine kinase are described. Drug design studies of known purine compounds revealed that both positions-2 and -6 were suitable for incorporating bone-seeking moieties.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::75987963f2540aebe25650862e108230
https://pubmed.ncbi.nlm.nih.gov/12941335

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Structure-based design of an osteoclast-selective, nonpeptide Src homology 2 inhibitor with in vivo antiresorptive activity

Targeted disruption of the pp60 src (Src) gene has implicated this tyrosine kinase in osteoclast-mediated bone resorption and as a therapeutic target for the treatment of osteoporosis and other bone-related diseases. Herein we describe the discovery

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d4c5b835f12945cdcdbb7f6a31d14980
https://europepmc.org/articles/PMC16871/

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Discovery of potent and selective SH2 inhibitors of the tyrosine kinase ZAP-70

Autor: Selvi Pradeepan, Chi B. Vu, Tomi K. Sawyer, Shelia Violette, van Schravendijk Mr, Ian A. MacNeil, Catherine Bartlett, Mary K. Ram, Botfield Mc, Charles J. Eyermann, Berkley A. Lynch, Taylor Merry, Evelyn G. Corpuz, Regine S. Bohacek

Publikováno v: Journal of medicinal chemistry. 42(20)

A series of 1,2,4-oxadiazole analogues has been shown to be potent and selective SH2 inhibitors of the tyrosine kinase ZAP-70, a potential therapeutic target for immune suppression. These compounds typically are 200-400-fold more potent than the nati

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::42d84c5760ebfcd16429d81250044b98
https://pubmed.ncbi.nlm.nih.gov/10514279

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