Zobrazeno 1 - 10 of 55 pro vyhledávání: '"V V, Sardana"'
1
Development of thioquinazolinones, allosteric Chk1 kinase inhibitors
Autor: Marc Abrams, Laura Sepp-Lorenzino, Steve Stirdivant, Joan Zugay-Murphy, Keith W. Rickert, Xianzhi Mao, Stephen C. Beck, Mark E. Fraley, Robert M. Garbaccio, Rob Lobell, Youwei Yan, Bob Drakas, Paul Zuck, Sylvie Jezequel-Sur, Kelly Hamilton, Timothy J. Hartingh, Constantine Kreatsoulas, Edward S. Tasber, Sanjeev Munshi, Antonella Converso, Eileen S. Walsh, George D. Hartman, Carolyn A. Buser, Weikang Tao, V V Sardana
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:1240-1244
A high throughput screening campaign was designed to identify allosteric inhibitors of Chk1 kinase by testing compounds at high concentration. Activity was then observed at K(m) for ATP and at near-physiological concentrations of ATP. This strategy l
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5a164d70b45a247a3957cdbd7608b23b
https://doi.org/10.1016/j.bmcl.2008.12.076
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2
Development of 6-substituted indolylquinolinones as potent Chek1 kinase inhibitors
Autor: Eileen S. Walsh, Steve Stirdivant, George D. Hartman, Kelly Hamilton, Marc Abrams, Robert M. Garbaccio, Laura Sepp-Lorenzino, Lawrence Kuo, Steve Beck, Joan Zugay Murphy, Constantine Kreatsoulas, Justin T. Steen, Sanjeev Munshi, Carolyn A. Buser, Weikang Tao, Shaei Huang, Youwei Yan, V V Sardana, Bob Drakas, Mari Ikuta, James Hardwick, Keith W. Rickert, Mark E. Fraley, Elizabeth Mahan, Xianzhi Mao, Rob Lobell, Michael Reilly
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 16:5907-5912
Through a comparison of X-ray co-crystallographic data for 1 and 2 in the Chek1 active site, it was hypothesized that the affinity of the indolylquinolinone series (2) for Chek1 kinase would be improved via C6 substitution into the hydrophobic region
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9417e1526f4bd74048baad5244ad1fea
https://doi.org/10.1016/j.bmcl.2006.08.053
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3
A general procedure for the purification of human β-secretase expressed in Escherichia coli
Autor: Paul L. Darke, Sanjeev Munshi, Zhongguo Chen, Lawrence C. Kuo, Bei Xu, Joan Zugay-Murphy, V V Sardana, Mohinder K. Sardana
Publikováno v: Protein Expression and Purification. 34:190-196
Expression and purification of human beta-secretase (BACE1) in bacteria have been plagued with issues concerning solubility, inhomogeneous N-terminus, and lack of enzymic activity. Several forms of the mature human BACE1 have been expressed in Escher
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7fea7d6e57b22fbf50f6e9846446fc23
https://doi.org/10.1016/j.pep.2003.12.014
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4
X-ray structure of simian immunodeficiency virus integrase containing the core and C-terminal domain (residues 50-293) - an initial glance of the viral DNA binding platform 1 1Edited by I. A. Wilson
Autor: Lawrence C. Kuo, Abigail Wolfe, Emilio A. Emini, Ying Li, Bei Xu, Joan Zugay-Murphy, Peter J. Felock, Zhongguo Chen, Marc V. Witmer, Daria J. Hazuda, Sanjeev Munshi, Youwei Yan, V V Sardana
Publikováno v: Journal of Molecular Biology. 296:521-533
The crystal structure of simian immunodeficiency virus (SIV) integrase that contains in a single polypeptide the core and the C-terminal deoxyoligonucleotide binding domain has been determined at 3 A resolution with an R -value of 0.203 in the space
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::2a5c061dda24790ca652d37a70a191c2
https://doi.org/10.1006/jmbi.1999.3451
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5
Purification, solution properties and crystallization of SIV integrase containing a continuous core and C-terminal domain
Autor: Ying Li, Abigail Wolfe, Peter J. Felock, Daria J. Hazuda, Youwei Yan, V V Sardana, Joan Zugay-Murphy, Marc V. Witmer, Zhongguo Chen, Mohinder K. Sardana, Bei Xu, James L. Cole, Lawrence C. Kuo
Publikováno v: Acta Crystallographica Section D Biological Crystallography. 55:1906-1910
The C-terminal two-thirds segment of integrase derived from the simian immunodeficiency virus has been cloned, expressed in Escherichia coli, and purified to greater than 95% homogeneity. The protein encompasses amino-acid residues 50–293 and conta
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6b35be474ffa03a53718c11f2ec042ca
https://doi.org/10.1107/s0907444999009610
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6
Complex of NS3 protease and NS4A peptide of BK strain hepatitis C virus: A 2.2 Å resolution structure in a hexagonal crystal form
Autor: Youwei Yan, Mohinder K. Sardana, C. Steinkuehler, Ying Li, Lawrence Kuo, R. De Francesco, Zhongguo Chen, Licia Tomei, Sanjeev Munshi, V V Sardana, James L. Cole
Publikováno v: Protein Science. 7:837-847
The crystal structure of the NS3 protease of the hepatitis C virus (BK strain) has been determined in the space group P6(3)22 to a resolution of 2.2 A. This protease is bound with a 14-mer peptide representing the central region of the NS4A protein.
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::517d36d00d31b6aa0dc5f782e63129ac
https://doi.org/10.1002/pro.5560070402
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7
Human immunodeficiency virus 1 (HIV-1)-specific reverse transcriptase (RT) inhibitors may suppress the replication of specific drug-resistant (E138K)RT HIV-1 mutants or select for highly resistant (Y181C-->C181I)RT HIV-1 mutants
Autor: E A Emini, Anna Karlsson, E. De Clercq, V V Sardana, Jan Balzarini, M J Camarasa
Publikováno v: Scopus-Elsevier
Mutant HIV-1 that expresses a Glu138-->Lys substitution in its RT [(E138K)RT] is resistant to the HIV-1-specific RT inhibitor 2',5'-bis-O-(tert-butyldimethylsilyl)-3'-spiro-5"-(4"-amino-1",2"- oxathiole-2",2"-dioxide)pyrimidine (TSAO). However, cell
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1380f941bb215e67eade8c5863a6fa0e
https://doi.org/10.1073/pnas.91.14.6599
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8
Peptide substrate cleavage specificity of the human cytomegalovirus protease
Autor: C A Veloski, W J Long, K LeGrow, J A Wolfgang, V V Sardana, Bohdan S. Wolanski, Emilio A. Emini, Robert L. Lafemina
Publikováno v: Journal of Biological Chemistry. 269:14337-14340
The human cytomegalovirus UL80 gene encodes an 80-kDa precursor polyprotein whose N-terminal 256-amino acid domain is a protease. This enzyme cleaves a specific peptide bond that results in its own release from the precursor, as well as a peptide bon
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ac89a92ec59b0bac6179a19a109ba378
https://doi.org/10.1016/s0021-9258(17)36622-x
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10
Comprehensive mutant enzyme and viral variant assessment of human immunodeficiency virus type 1 reverse transcriptase resistance to nonnucleoside inhibitors
Autor: W J Long, J A Wolfgang, Jon H. Condra, V V Sardana, A J Schlabach, C L Schneider, J A Waterbury, B S Wolanski, William A. Schleif, V W Byrnes
Publikováno v: Antimicrobial Agents and Chemotherapy. 37:1576-1579
The nonnucleoside reverse transcriptase (RT) inhibitors comprise a class of structurally diverse compounds that are functionally related and specific for the human immunodeficiency virus type 1 RT. Viral variants resistant to these compounds arise re
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e10ad59c45dbcbae135e1ba309b31d01
https://doi.org/10.1128/aac.37.8.1576
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