Zobrazeno 1 - 10 of 22 pro vyhledávání: '"G.D. Kishore Kumar"'
1
A mitochondria-targeted mass spectrometry probe to detect glyoxals: implications for diabetes
Autor: Angela Logan, Robin A.J. Smith, Ian M. Fearnley, Thomas Krieg, Katja E. Menger, Tracy A. Prime, Carmen Methner, G.D. Kishore Kumar, Sebastian Rogatti, Balu K. Chacko, Yvonne Collins, Pamela Boon Li Pun, Michelle S. Johnson, Andrew M. James, Michael P. Murphy, Guang W. Huang, Richard C. Hartley, David S. Larsen, Victor M. Darley-Usmar, Lesley Larsen
Publikováno v: Free Radical Biology & Medicine
The glycation of protein and nucleic acids that occurs as a consequence of hyperglycemia disrupts cell function and contributes to many pathologies, including those associated with diabetes and aging. Intracellular glycation occurs after the generati
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9ac0f1a5a64eaa512b1ceb06454cf9e7
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2
Synthesis and Biochemical Evaluation of Thiochromanone Thiosemicarbazone Analogues as Inhibitors of Cathepsin L
Autor: G.D. Kishore Kumar, Shen-En Chen, Kevin G. Pinney, Gustavo E. Chavarria, Liela Bayeh, Amanda K. Charlton-Sevcik, Lindsay M. Jones, Jiangli Song, Mary Lynn Trawick, David J. Chaplin, Elizabeth S Conner
Publikováno v: ACS Medicinal Chemistry Letters
A series of 36 thiosemicarbazone analogues containing the thiochromanone molecular scaffold functionalized primarily at the C-6 position were prepared by chemical synthesis and evaluated as inhibitors of cathepsins L and B. The most promising inhibit
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3
Synthesis and evaluation of macrocyclic diarylether heptanoid natural products and their analogs
Autor: Abijah M. Nyong, G.D. Kishore Kumar, Vashti C. Bryant, Amarnath Natarajan
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:245-248
The macrocyclic diarylether heptanoid (MDEH) natural products have been used in folk medicine for centuries. MDEHs are reported to exert anti-tumor properties by inhibiting the activation of NF-κB. Here we report the synthesis of a small MDEH librar
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https://doi.org/10.1016/j.bmcl.2011.11.025
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4
Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors
Autor: Amanda K. Charlton-Sevcik, David J. Chaplin, Tracy E. Strecker, Bronwyn G. Siim, G.D. Kishore Kumar, Shen-En Chen, Gustavo E. Chavarria, Mary Lynn Trawick, Wara M. Arispe, Matthew T. MacDonough, Kevin G. Pinney
Publikováno v: Bioorganic & Medicinal Chemistry Letters
Graphical abstract A variety of benzophenone thiosemicarbazone analogs have been designed and prepared by chemical synthesis. A sub-set of these compounds demonstrated potent inhibition of cathepsin L with minimal inhibition of cathepsin B.
A sm
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http://europepmc.org/articles/PMC7125537
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5
Design, synthesis, biochemical, and biological evaluation of nitrogen-containing trifluoro structural modifications of combretastatin A-4
Autor: Christopher J. Jelinek, George R. Pettit, Justin K. Tidmore, Tracy E. Strecker, Madhavi Sriram, G.D. Kishore Kumar, Mallinath B. Hadimani, Mary Lynn Trawick, John J. Hall, David J. Chaplin, Kevin G. Pinney
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 18:5146-5149
A new trifluorinated amino-combretastatin analogue, ( Z) -2-(4′-methoxy-3′-aminophenyl)-1-(3,4,5-trifluorophenyl)ethene, prepared by chemical synthesis, was found to be a potent inhibitor of tubulin assembly (IC 50 = 2.9 μM), and cytotoxic again
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c5888082483e93431c2388d1229fecf9
https://doi.org/10.1016/j.bmcl.2008.07.070
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6
Synthesis and biochemical evaluation of benzoylbenzophenone thiosemicarbazone analogues as potent and selective inhibitors of cathepsin L
Autor: Gustavo E. Chavarria, Dietmar W. Siemann, David J. Chaplin, Erica Parker, Kevin G. Pinney, Ashleigh L. Barnes, Samuel O. Odutola, G.D. Kishore Kumar, Mary Lynn Trawick, Dhivya R. Sudhan, Amanda K. Charlton-Sevcik, Michael R. Horsman, Thomas Wittenborn, Jiangli Song, Tracy E. Strecker
Publikováno v: Parker, E N, Song, J, Kishore Kumar, G D, Odutola, S O, Chavarria, G E, Charlton-Sevcik, A K, Strecker, T E, Barnes, A L, Sudhan, D R, Wittenborn, T R, Siemann, D W, Horsman, M R, Chaplin, D J, Trawick, M L & Pinney, K G 2015, ' Synthesis and biochemical evaluation of benzoylbenzophenone thiosemicarbazone analogues as potent and selective inhibitors of cathepsin L ', Bioorganic & Medicinal Chemistry, vol. 23, no. 21, pp. 6974-6992 . https://doi.org/10.1016/j.bmc.2015.09.036
Upregulation of cathepsin L in a variety of tumors and its ability to promote cancer cell invasion and migration through degradation of the extracellular matrix suggest that cathepsin L is a promising biological target for the development of anti-met
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https://pubmed.ncbi.nlm.nih.gov/26462052
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7
High-throughput fluorescence polarization assay to identify small molecule inhibitors of BRCT domains of breast cancer gene 1
Autor: G. L. Lokesh, Aparna Rachamallu, Amarnath Natarajan, G.D. Kishore Kumar
Publikováno v: Analytical Biochemistry. 352:135-141
The C-terminus region of the 1863 residue early onset of breast cancer gene 1 (BRCA1) nuclear protein contains a tandem globular carboxy terminus domain termed BRCT. The BRCT repeats in BRCA1 are phosphoserine- and/or phosphothreonine-specific bindin
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https://doi.org/10.1016/j.ab.2006.01.025
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8
Total synthesis of ovalifoliolatin B, acerogenins A and C
Autor: Amarnath Natarajan, G.D. Kishore Kumar
Publikováno v: Tetrahedron Letters. 49:2103-2105
A short and concise route for the synthesis of ovalifoliolatin B, a highly strained macrocyclic diaryl ether heptanoid natural product that also provides quick access to acerogenins A and C natural products has been reported.
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https://doi.org/10.1016/j.tetlet.2008.01.135
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9
Initial evaluation of the antitumour activity of KGP94, a functionalized benzophenone thiosemicarbazone inhibitor of cathepsin L
Autor: Shen-En Chen, David J. Chaplin, Michael R. Horsman, Kevin G. Pinney, Tracy E. Strecker, Wara M. Arispe, Mary Lynn Trawick, G.D. Kishore Kumar, Erica Parker, Gustavo E. Chavarria
Publikováno v: Chavarria, G E, Horsman, M R, Arispe, W M, Kumar, G D K, Chen, S-E, Strecker, T E, Parker, E N, Chaplin, D J, Pinney, K G & Trawick, M L 2012, ' Initial evaluation of the antitumour activity of KGP94, a functionalized benzophenone thiosemicarbazone inhibitor of cathepsin L ', European Journal of Medicinal Chemistry, vol. 58, pp. 568-72 . https://doi.org/10.1016/j.ejmech.2012.10.039
Kinetic analysis of the mode of inhibition of cathepsin L by KGP94, a lead compound from a privileged library of functionalized benzophenone thiosemicarbazone derivatives, demonstrated that it is a time-dependent, reversible, and competitive inhibito
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https://pubmed.ncbi.nlm.nih.gov/23168380
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