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1
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0037416141
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The small-molecule approach to biology
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S.L. Schreiber The small-molecule approach to biology Chem Eng News 81 2003 51 61 An excellent, comprehensive report on the use of DOS-derived, small-molecule chemical probes in understanding (and dissecting) complex biological interactions.
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(2003)
Chem Eng News
, vol.81
, pp. 51-61
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Schreiber, S.L.1
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2
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0036909567
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Small molecules, big impact: A history of chemical inhibitors and the cytoskeleton
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J.R. Peterson, and T.J. Mitchison Small molecules, big impact: a history of chemical inhibitors and the cytoskeleton Chem Biol 9 2002 1275 1285
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(2002)
Chem Biol
, vol.9
, pp. 1275-1285
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Peterson, J.R.1
Mitchison, T.J.2
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3
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0141633672
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Solution-phase combinatorial libraries: Modulating cellular signaling by targeting protein-protein or protein-DNA interactions
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D.L. Boger, J. Desharnais, and K. Capps Solution-phase combinatorial libraries: Modulating cellular signaling by targeting protein-protein or protein-DNA interactions Angew Chem Int Ed Engl 42 2003 4138 4176 Several examples of bioactive small-molecule chemical probes proven to act as modulators of macromolecular interactions are nicely discussed in the review article.
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(2003)
Angew Chem Int Ed Engl
, vol.42
, pp. 4138-4176
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Boger, D.L.1
Desharnais, J.2
Capps, K.3
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4
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3142781225
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Small-molecule inhibitors of protein-protein interactions: Progressing towards the dream
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M.R. Arkin, and J.A. Wells Small-molecule inhibitors of protein-protein interactions: progressing towards the dream Nat Rev Drug Discov 3 2004 301 317 This article presents the challenges and opportunities for designing small-molecule inhibitors of protein-protein interactions. Several successful stories covered in this article provide a good overview of the current status of research in this area.
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(2004)
Nat Rev Drug Discov
, vol.3
, pp. 301-317
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Arkin, M.R.1
Wells, J.A.2
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5
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0042572312
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The completed human genome: Implications for chemical biology
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C.P. Austin The completed human genome: implications for chemical biology Curr Opin Chem Biol 7 2003 511 515
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(2003)
Curr Opin Chem Biol
, vol.7
, pp. 511-515
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Austin, C.P.1
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6
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0037432765
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From knowing to controlling: A path from genomics to drugs using small molecule probes
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R.L. Strausberg, and S.L. Schreiber From knowing to controlling: a path from genomics to drugs using small molecule probes Science 300 2003 294 295
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(2003)
Science
, vol.300
, pp. 294-295
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Strausberg, R.L.1
Schreiber, S.L.2
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7
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0031710509
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Chemical genetics resulting from a passion for synthetic organic chemistry
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S.L. Schreiber Chemical genetics resulting from a passion for synthetic organic chemistry Bioorg Med Chem 6 1998 1127 1152
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(1998)
Bioorg Med Chem
, vol.6
, pp. 1127-1152
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Schreiber, S.L.1
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8
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0038400185
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Chemical genetics: Tailoring tools for cell biology
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T.U. Mayer Chemical genetics: tailoring tools for cell biology Trends Cell Biol 13 2003 270 277
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(2003)
Trends Cell Biol
, vol.13
, pp. 270-277
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Mayer, T.U.1
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9
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0142087554
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Antibodies as therapeutic agents: Vive le renaissance!
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L. Stockwin, and S. Holmes Antibodies as therapeutic agents: vive le renaissance! Expert Opin Biol Ther 3 2003 1133 1152
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(2003)
Expert Opin Biol Ther
, vol.3
, pp. 1133-1152
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Stockwin, L.1
Holmes, S.2
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10
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3342908718
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Emerging classes of protein-protein interaction inhibitors and new tools for their development
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L. Pagliaro, J. Felding, K. Audouze, S.J. Nielsen, R.B. Terry, C. Krog-Jensen, and S. Butcher Emerging classes of protein-protein interaction inhibitors and new tools for their development Curr Opin Chem Biol 8 2004 442 449
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(2004)
Curr Opin Chem Biol
, vol.8
, pp. 442-449
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Pagliaro, L.1
Felding, J.2
Audouze, K.3
Nielsen, S.J.4
Terry, R.B.5
Krog-Jensen, C.6
Butcher, S.7
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11
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0000875480
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Chemistry, biology and medicine of selected tubulin polymerizing agents
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K.C. Nicolaou, D. Hepworth, N.P. King, and M.R.V. Finaly Chemistry, biology and medicine of selected tubulin polymerizing agents Pure & Appl Chem 71 1999 989 997
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(1999)
Pure & Appl Chem
, vol.71
, pp. 989-997
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Nicolaou, K.C.1
Hepworth, D.2
King, N.P.3
Finaly, M.R.V.4
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13
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0030779208
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Designed epothilones: Combinatorial synthesis, tubulin assembly properties, and cytotoxic action against Taxol-resistant tumor cells
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K.C. Nicolaou, D. Vourloumis, T. Li, J. Pastor, N. Winssinger, Y. He, S. Ninkovic, F. Sarabia, H. Vallberg, and F. Roschanger Designed epothilones: combinatorial synthesis, tubulin assembly properties, and cytotoxic action against Taxol-resistant tumor cells Angew Chem Int Ed Engl 36 1997 2097 2103
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(1997)
Angew Chem Int Ed Engl
, vol.36
, pp. 2097-2103
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Nicolaou, K.C.1
Vourloumis, D.2
Li, T.3
Pastor, J.4
Winssinger, N.5
He, Y.6
Ninkovic, S.7
Sarabia, F.8
Vallberg, H.9
Roschanger, F.10
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14
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0034644383
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Evolution of a gram-scale synthesis of (+)-discodermolide
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A.B. Smith, T.J. Beauchamp, M.J. LaMarche, M.D. Kaufman, Y. Qiu, H. Arimoto, D.R. Jones, and K. Kobayashi Evolution of a gram-scale synthesis of (+)-discodermolide J Am Chem Soc 122 2000 8654 8664
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(2000)
J Am Chem Soc
, vol.122
, pp. 8654-8664
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Smith, A.B.1
Beauchamp, T.J.2
Lamarche, M.J.3
Kaufman, M.D.4
Qiu, Y.5
Arimoto, H.6
Jones, D.R.7
Kobayashi, K.8
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15
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0034826406
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The relationship between Taxol and (+)-discodermolide: Synthetic analogs and modeling studies
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L.A. Martello, M.J. LaMarche, L. He, T.J. Beauchamp, A.B. Smith, and S.B. Horwitz The relationship between Taxol and (+)-discodermolide: synthetic analogs and modeling studies Chem Biol 8 2001 843 855
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(2001)
Chem Biol
, vol.8
, pp. 843-855
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Martello, L.A.1
Lamarche, M.J.2
He, L.3
Beauchamp, T.J.4
Smith, A.B.5
Horwitz, S.B.6
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16
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0030113284
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(+)-Discodermolide binds to microtubules in stoichiometric ratio to tubulin dimers, blocks Taxol binding and results in mitotic arrest
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D.T. Hung, J. Chen, and S.L. Schreiber (+)-Discodermolide binds to microtubules in stoichiometric ratio to tubulin dimers, blocks Taxol binding and results in mitotic arrest Chem Biol 3 1996 287 293
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(1996)
Chem Biol
, vol.3
, pp. 287-293
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Hung, D.T.1
Chen, J.2
Schreiber, S.L.3
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17
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0141508044
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Microtubule-stabilizing marine metabolite laulimalide and its derivatives: Synthetic approaches and antitumor activity
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J. Mulzer, and E. Ohler Microtubule-stabilizing marine metabolite laulimalide and its derivatives: Synthetic approaches and antitumor activity Chem Rev 103 2003 3753 3786
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(2003)
Chem Rev
, vol.103
, pp. 3753-3786
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Mulzer, J.1
Ohler, E.2
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18
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0032475452
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Total synthesis of eleutherobin and eleuthosides a and B
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K.C. Nicolaou, T. Ohshima, S. Hosokawa, F.L. VaDelft, D. Vourloumis, J.Y. Xu, J. Pfefferkorn, and S. Kim Total synthesis of eleutherobin and eleuthosides A and B J Am Chem Soc 120 1998 8674 8680
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(1998)
J Am Chem Soc
, vol.120
, pp. 8674-8680
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Nicolaou, K.C.1
Ohshima, T.2
Hosokawa, S.3
Vadelft, F.L.4
Vourloumis, D.5
Xu, J.Y.6
Pfefferkorn, J.7
Kim, S.8
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19
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0029842109
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Structure of the FKBP12-rapamycin complex interacting with binding domain of human FRAP
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J. Choi, J. Chen, S.L. Schreiber, and J. Clardy Structure of the FKBP12-rapamycin complex interacting with binding domain of human FRAP Science 273 1996 239 242
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(1996)
Science
, vol.273
, pp. 239-242
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Choi, J.1
Chen, J.2
Schreiber, S.L.3
Clardy, J.4
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20
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0030296634
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Three-part inventions: Intracellular signaling and induced proximity
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G.R. Crabtree, and S.L. Schreiber Three-part inventions: intracellular signaling and induced proximity Trends Biochem Sci 21 1996 418 422
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(1996)
Trends Biochem Sci
, vol.21
, pp. 418-422
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Crabtree, G.R.1
Schreiber, S.L.2
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21
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0030013607
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Controlling protein association and subcellular localization with a synthetic ligand that induces heterodimerization of proteins
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P.J. Belshaw, S.N. Ho, G.R. Crabtree, and S.L. Schreiber Controlling protein association and subcellular localization with a synthetic ligand that induces heterodimerization of proteins Proc Natl Acad Sci USA 93 1996 4604 4607
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(1996)
Proc Natl Acad Sci USA
, vol.93
, pp. 4604-4607
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Belshaw, P.J.1
Ho, S.N.2
Crabtree, G.R.3
Schreiber, S.L.4
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22
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0031892994
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Dimerization as a regulatory mechanism in signal transduction
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J.D. Klemm, S.L. Schreiber, and G.R. Crabtree Dimerization as a regulatory mechanism in signal transduction Annu Rev Immunol 16 1998 569 592
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(1998)
Annu Rev Immunol
, vol.16
, pp. 569-592
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Klemm, J.D.1
Schreiber, S.L.2
Crabtree, G.R.3
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23
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0035977612
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Isolation and structure elucidation of chlorofusin, a novel p53-MDM2 antagonist from a Fusarium sp
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S.J. Duncan, S. Gruschow, D.H. Williams, C. McNicholas, R. Purewal, M. Hajek, M. Gerlitz, S. Martin, S.K. Wrigley, and M. Moore Isolation and structure elucidation of chlorofusin, a novel p53-MDM2 antagonist from a Fusarium sp J Am Chem Soc 123 2001 554 560
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(2001)
J Am Chem Soc
, vol.123
, pp. 554-560
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Duncan, S.J.1
Gruschow, S.2
Williams, D.H.3
McNicholas, C.4
Purewal, R.5
Hajek, M.6
Gerlitz, M.7
Martin, S.8
Wrigley, S.K.9
Moore, M.10
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24
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0037398860
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Protecting p53 from degradation
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S. Lain Protecting p53 from degradation Biochem Soc Trans 31 2003 482 485
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(2003)
Biochem Soc Trans
, vol.31
, pp. 482-485
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Lain, S.1
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25
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10744221485
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In vivo activation of the p53 pathway by small-molecule antagonists of MDM2
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L.T. Vassilev, B.T. Vu, B. Graves, D. Carvajal, F. Podlaski, Z. Filipovic, N. Kong, U. Kammlott, C. Lukacs, C. Lein, N. Fotouhi, and E.A. Liu In vivo activation of the p53 pathway by small-molecule antagonists of MDM2 Science 303 2004 844 848 This article is a good example showing a rational approach (i.e. using protein structure information) leading to developing a small-molecule inhibitor of protein-protein interaction.
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(2004)
Science
, vol.303
, pp. 844-848
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Vassilev, L.T.1
Vu, B.T.2
Graves, B.3
Carvajal, D.4
Podlaski, F.5
Filipovic, Z.6
Kong, N.7
Kammlott, U.8
Lukacs, C.9
Lein, C.10
Fotouhi, N.11
Liu, E.A.12
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26
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0034678033
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Target-oriented and diversity-oriented organic synthesis in drug discovery
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S.L. Schreiber Target-oriented and diversity-oriented organic synthesis in drug discovery Science 287 2000 1964 1969
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(2000)
Science
, vol.287
, pp. 1964-1969
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Schreiber, S.L.1
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0344515366
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Diversity-oriented synthesis; A challenge for synthetic chemists
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D.R. Spring Diversity-oriented synthesis; a challenge for synthetic chemists Org Biomol Chem 1 2003 3867 3870
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(2003)
Org Biomol Chem
, vol.1
, pp. 3867-3870
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Spring, D.R.1
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28
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3042799070
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A planning strategy for diversity-oriented synthesis
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M.D. Burke, and S.L. Schreiber A planning strategy for diversity-oriented synthesis Angew Chem Int Ed Engl 43 2004 46 58
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(2004)
Angew Chem Int Ed Engl
, vol.43
, pp. 46-58
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Burke, M.D.1
Schreiber, S.L.2
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29
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0038343601
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HR22CC16: A potent small-molecule probe for the dynamics of cell division
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S. Hotha, J.C. Yarrow, J.G. Yang, S. Garrett, K.V. Renduchintala, T.U. Mayer, and T.M. Kapoor HR22CC16: a potent small-molecule probe for the dynamics of cell division Angew Chem Int Ed Engl 42 2003 2379 2382
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(2003)
Angew Chem Int Ed Engl
, vol.42
, pp. 2379-2382
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Hotha, S.1
Yarrow, J.C.2
Yang, J.G.3
Garrett, S.4
Renduchintala, K.V.5
Mayer, T.U.6
Kapoor, T.M.7
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30
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0038713943
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Discovery of an inhibitor of a transcription factor using small molecule microarrays and diversity-oriented synthesis
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A.N. Koehler, A.F. Shamji, and S.L. Schreiber Discovery of an inhibitor of a transcription factor using small molecule microarrays and diversity-oriented synthesis J Am Chem Soc 125 2003 8420 8421 The use of a small-molecule microarray containing a DOS-based library tested in high-throughput protein binding experiments is described.
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(2003)
J Am Chem Soc
, vol.125
, pp. 8420-8421
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Koehler, A.N.1
Shamji, A.F.2
Schreiber, S.L.3
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31
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0142147275
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Generating diverse skeletons of small molecules combinatorially
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M.D. Burke, E.M. Berger, and S.L. Schreiber Generating diverse skeletons of small molecules combinatorially Science 302 2003 613 618 An example of synthetic strategies (in solution and on solid phase) allowing different architectures of natural product-like compounds in a high-throughput manner.
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(2003)
Science
, vol.302
, pp. 613-618
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Burke, M.D.1
Berger, E.M.2
Schreiber, S.L.3
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32
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7444242717
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A synthesis strategy yielding skeletally diverse small molecules combinatorially
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M.D. Burke, E.M. Berger, and S.L. Schreiber A synthesis strategy yielding skeletally diverse small molecules combinatorially J Am Chem Soc 126 2004 14095 14104
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(2004)
J Am Chem Soc
, vol.126
, pp. 14095-14104
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Burke, M.D.1
Berger, E.M.2
Schreiber, S.L.3
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33
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4544326369
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Synthetic strategy toward skeletal diversity via solid-supported, otherwise unstable reactive intermediates
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S.J. Taylor, A.M. Taylor, and S.L. Schreiber Synthetic strategy toward skeletal diversity via solid-supported, otherwise unstable reactive intermediates Angew Chem Int Ed Engl 43 2004 1681 1685
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(2004)
Angew Chem Int Ed Engl
, vol.43
, pp. 1681-1685
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Taylor, S.J.1
Taylor, A.M.2
Schreiber, S.L.3
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34
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0037138650
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Diversity-oriented synthesis of biaryl-containing medium rings using a one bead/one stock solution platform
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D.R. Spring, S. Krishnan, H.E. Blackwell, and S.L. Schreiber Diversity-oriented synthesis of biaryl-containing medium rings using a one bead/one stock solution platform J Am Chem Soc 124 2002 1354 1363 The identification of few lead compounds from a DOS-based library is described.
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(2002)
J Am Chem Soc
, vol.124
, pp. 1354-1363
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Spring, D.R.1
Krishnan, S.2
Blackwell, H.E.3
Schreiber, S.L.4
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35
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4544365737
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Asymmetric solid-phase synthesis of 6,6-spiroketals
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O. Barun, S. Sommer, and H. Waldmann Asymmetric solid-phase synthesis of 6,6-spiroketals Angew Chem Int Ed 43 2004 3195 3199 An application of a stereoselective aldol reaction on solid phase to obtain chiral, functionalized, sprioketal derivatives.
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(2004)
Angew Chem Int Ed
, vol.43
, pp. 3195-3199
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Barun, O.1
Sommer, S.2
Waldmann, H.3
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36
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14844300078
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A stereocontrolled, solid phase synthesis of 90 membered library of indoline alkaloid-like polycyclics from an enantiorich aminoindoline scaffold
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G. Zhonghong, P.T. Reddy, S. Quevillon, S. Couve-Bonnaire, and P. Arya A stereocontrolled, solid phase synthesis of 90 membered library of indoline alkaloid-like polycyclics from an enantiorich aminoindoline scaffold Angew Chem Int Ed 44 2005 1366 1368 The library generation of indoline alkaloid-like, functionalized tricyclic derivatives obtained by a stereoselective aza-Michael reaction.
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(2005)
Angew Chem Int Ed
, vol.44
, pp. 1366-1368
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Zhonghong, G.1
Reddy, P.T.2
Quevillon, S.3
Couve-Bonnaire, S.4
Arya, P.5
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