ANTINEOPLASTIC ACTIVITY;
ARTICLE;
BINDING AFFINITY;
CARBON NUCLEAR MAGNETIC RESONANCE;
CONTROLLED STUDY;
DRUG SCREENING;
DRUG SYNTHESIS;
HUMAN;
HUMAN CELL;
IC 50;
OSTEOSARCOMA CELL;
PROTEIN PROTEIN INTERACTION;
PROTON NUCLEAR MAGNETIC RESONANCE;
STRUCTURE ACTIVITY RELATION;
In Vivo Activation of the p53 Pathway by Small-Molecule Antagonists of MDM2
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Patented small molecule inhibitors of p53-MDM2 interaction
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J. Deng, R. Dayam, and N. Neamati Patented small molecule inhibitors of p53-MDM2 interaction Expert Opin. Ther. Pat 16 2006 165 188 (Pubitemid 43263239)
Terphenyl-based helical mimetics that disrupt the p53/HDM2 interaction
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H. Yin, G.I. Lee, H.S. Park, G.A. Payne, J.M. Rodriguez, S.M. Sebti, and A.D. Hamilton Terphenyl-based helical mimetics that disrupt the p53/HDM2 interaction Angew. Chem. Int. Ed. Engl. 44 2005 2704 2707 (Pubitemid 40689569)
Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells
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Structure-based design of potent non-peptide MDM2 inhibitors
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K. Ding, Y. Lu, Z. Nikolovska-Coleska, S. Qiu, Y. Ding, W. Gao, J. Stuckey, K. Krajewski, P.P. Roller, Y. Tomita, D.A. Parrish, J.R. Deschamps, and S. Wang Structure-based design of potent non-peptide MDM2 inhibitors J. Am. Chem. Soc. 127 2005 10130 10131 (Pubitemid 41045454)
A nonpeptidic sulfonamide inhibits the p53-mdm2 interaction and activates p53-dependent transcription in mdm2-overexpressing cells
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P.S. Galatin, and D.J. Abraham A nonpeptidic sulfonamide inhibits the p53-mdm2 interaction and activates p53-dependent transcription in mdm2-overexpressing cells J. Med. Chem. 47 2004 4163 4165 (Pubitemid 39045423)
Chalcone derivatives antagonize interactions between the human oncoprotein MDM2 and p53
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R. Stoll, C. Renner, S. Hansen, S. Palme, C. Klein, A. Belling, W. Zeslawski, M. Kamionka, T. Rehm, P. Muhlhahn, R. Schumacher, F. Hesse, B. Kaluza, W. Voelter, R.A. Engh, and T.A. Holak Chalcone derivatives antagonize interactions between the human oncoprotein MDM2 and p53 Biochemistry 40 2001 336 344 (Pubitemid 32061981)
High-density miniaturized thermal shift assays as a general strategy for drug discovery
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M.W. Pantoliano, E.C. Petrella, J.D. Kwasnoski, V.S. Lobanov, J. Myslik, E. Graf, T. Carver, E. Asel, B.A. Springer, P. Lane, and F.R. Salemme High-density miniaturized thermal shift assays as a general strategy for drug discovery J. Biomol. Screen. 6 2001 429 440 (Pubitemid 34052847)
Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein-protein interaction through structure-based drug design
DOI 10.1016/j.bmcl.2006.03.055, PII S0960894X06003490
D.J. Parks, L.V. LaFrance, R.R. Calvo, K.L. Milkiewicz, J.J. Marugan, P. Raboisson, C. Schubert, H.K. Koblish, S. Zhao, C.F. Franks, J. Lattanze, T.E. Carver, M.D. Cummings, D. Maguire, B.L. Grasberger, A.C. Maroney, and T. Lu Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein-protein interaction through structure-based drug design Bioorg. Med. Chem. Lett. 16 2006 3310 3314 (Pubitemid 44304453)
Benzodiazepinedione inhibitors of the Hdm2:p53 complex suppress human tumor cell proliferation in vitro and sensitize tumors to doxorubicin in vivo
H.K. Koblish, S. Zhao, C.F. Franks, R.R. Donatelli, R.M. Tominovich, L.V. LaFrance, K.A. Leonard, J.M. Gushue, D.J. Parks, R.R. Calvo, K.L. Milkiewicz, J.J. Marugan, P. Raboisson, M.D. Cummings, B.L. Grasberger, D.L. Johnson, T. Lu, C.J. Molloy, and A.C. Maroney Benzodiazepinedione inhibitors of the Hdm2:p53 complex suppress human tumor cell proliferation in vitro and sensitize tumors to doxorubicin in vivo Mol. Cancer Ther. 5 2006 160 169
1,4-Thienodiazepine-2,5-diones via MCR (I): Synthesis, virtual space and p53-Mdm2 activity
Y. Huang, S. Wolf, M. Bista, L. Meireles, C. Camacho, T.A. Holak, and A. Domling 1,4-Thienodiazepine-2,5-diones via MCR (I): synthesis, virtual space and p53-Mdm2 activity Chem. Biol. Drug Des. 76 2010 116 129
KY-109, a new bifunctional pro-drug of a cephalosporin. Chemistry, physico-chemical and biological properties
N. Kakeya, S. Nishizawa, K. Nishimura, A. Yoshimi, S. Tamaki, T. Mori, and K. Kitao KY-109, a new bifunctional pro-drug of a cephalosporin. Chemistry, physico-chemical and biological properties J. Antibiot. (Tokyo) 38 1985 380 389 (Pubitemid 15102202)
Multicomponent synthesis of novel amino acid-nucleobase chimeras: A versatile approach to PNA-monomers
DOI 10.1016/S0968-0896(00)00066-3, PII S0968089600000663
W. Maison, I. Schlemminger, O. Westerhoff, and J. Martens Multicomponent synthesis of novel amino acid-nucleobase chimeras: a versatile approach to PNA-monomers Bioorg. Med. Chem. 8 2000 1343 1360 (Pubitemid 30398455)
Structure of the MDM2 oncoprotein bound to the p53 tumor suppressor transactivation domain
DOI 10.1126/science.274.5289.948
P.H. Kussie, S. Gorina, V. Marechal, B. Elenbaas, J. Moreau, A.J. Levine, and N.P. Pavletich Structure of the MDM2 oncoprotein bound to the p53 tumor suppressor transactivation domain Science 274 1996 948 953 (Pubitemid 26398409)
Discovery of a nanomolar inhibitor of the human murine double minute 2 (MDM2)-p53 interaction through an integrated, virtual database screening strategy
DOI 10.1021/jm060023+
Y. Lu, Z. Nikolovska-Coleska, X. Fang, W. Gao, S. Shangary, S. Qiu, D. Qin, and S. Wang Discovery of a nanomolar inhibitor of the human murine double minute 2 (MDM2)-p53 interaction through an integrated, virtual database screening strategy J. Med. Chem. 49 2006 3759 3762 (Pubitemid 43967873)
