-
1
-
-
0033618555
-
Detecting protein function and protein-protein interactions from genome sequences
-
Marcotte E.M., Pellegrini M., Ng H.L., Rice D.W., Yeates T.O., Eisenberg D. Detecting protein function and protein-protein interactions from genome sequences. Science. 285:1999;751-753
-
(1999)
Science
, vol.285
, pp. 751-753
-
-
Marcotte, E.M.1
Pellegrini, M.2
Ng, H.L.3
Rice, D.W.4
Yeates, T.O.5
Eisenberg, D.6
-
2
-
-
0011909346
-
Macromolecular therapeutics: Emerging strategies for drug discovery in the postgenome era
-
Juliano R.L., Astriab-Fisher A., Falke D. Macromolecular therapeutics: emerging strategies for drug discovery in the postgenome era. Mol Interv. 1:2001;40-53
-
(2001)
Mol Interv
, vol.1
, pp. 40-53
-
-
Juliano, R.L.1
Astriab-Fisher, A.2
Falke, D.3
-
3
-
-
0036469060
-
Unraveling hot spots in binding interfaces: Progress and challenges
-
DeLano W.L. Unraveling hot spots in binding interfaces: progress and challenges. Curr Opin Struct Biol. 12:2002;14-20
-
(2002)
Curr Opin Struct Biol
, vol.12
, pp. 14-20
-
-
Delano, W.L.1
-
4
-
-
0041821388
-
Dehydron: A structurally encoded signal for protein interaction
-
Fernandez A., Scott R. Dehydron: a structurally encoded signal for protein interaction. Biophys J. 85:2003;1914-1928
-
(2003)
Biophys J
, vol.85
, pp. 1914-1928
-
-
Fernandez, A.1
Scott, R.2
-
5
-
-
0037388679
-
Protein-protein interactions as a target for drugs in proteomics
-
Archakov A.I., Govorun V.M., Dubanov A.V., Ivanov Y.D., Veselovsky A.V., Lewi P., Janssen P. Protein-protein interactions as a target for drugs in proteomics. Proteomics. 3:2003;380-391
-
(2003)
Proteomics
, vol.3
, pp. 380-391
-
-
Archakov, A.I.1
Govorun, V.M.2
Dubanov, A.V.3
Ivanov, Y.D.4
Veselovsky, A.V.5
Lewi, P.6
Janssen, P.7
-
6
-
-
0034644538
-
Translocation and reversible localization of signaling proteins: A dynamic future for signal transduction
-
Teruel M.N., Meyer T. Translocation and reversible localization of signaling proteins: a dynamic future for signal transduction. Cell. 103:2000;181-184
-
(2000)
Cell
, vol.103
, pp. 181-184
-
-
Teruel, M.N.1
Meyer, T.2
-
7
-
-
0034644509
-
Signaling networks: The origins of cellular multitasking
-
Jordan J.D., Landau E.M., Iyengar R. Signaling networks: the origins of cellular multitasking. Cell. 103:2000;193-200
-
(2000)
Cell
, vol.103
, pp. 193-200
-
-
Jordan, J.D.1
Landau, E.M.2
Iyengar, R.3
-
8
-
-
0037061646
-
Inhibition of protein-protein association by small molecules: Approaches and progress
-
Toogood P.L. Inhibition of protein-protein association by small molecules: approaches and progress. J Med Chem. 45:2002;1543-1558
-
(2002)
J Med Chem
, vol.45
, pp. 1543-1558
-
-
Toogood, P.L.1
-
9
-
-
0037860938
-
Modulation of protein-protein interactions with small organic molecules
-
An excellent review summarizing the different approaches used to identify small-molecule protein-protein modulators.
-
Berg T. Modulation of protein-protein interactions with small organic molecules. Angew Chem Int Ed Engl. 42:2003;2462-2481 An excellent review summarizing the different approaches used to identify small-molecule protein-protein modulators.
-
(2003)
Angew Chem Int Ed Engl
, vol.42
, pp. 2462-2481
-
-
Berg, T.1
-
10
-
-
0037439329
-
Nuclear transport as a target for cell growth
-
Kau T.R., Silver P.A. Nuclear transport as a target for cell growth. Drug Discov Today. 8:2003;78-85
-
(2003)
Drug Discov Today
, vol.8
, pp. 78-85
-
-
Kau, T.R.1
Silver, P.A.2
-
11
-
-
0345276609
-
Targeting the PI3K-AKT pathway for cancer therapy
-
Lu Y., Wang H., Mills G.B. Targeting the PI3K-AKT pathway for cancer therapy. Rev Clin Exp Hematol. 7:2003;205-228
-
(2003)
Rev Clin Exp Hematol
, vol.7
, pp. 205-228
-
-
Lu, Y.1
Wang, H.2
Mills, G.B.3
-
12
-
-
0141633672
-
Solution-phase combinatorial libraries: Modulating cellular signaling by targeting protein-protein or protein-DNA interactions
-
Boger D.L., Desharnais J., Capps K. Solution-phase combinatorial libraries: modulating cellular signaling by targeting protein-protein or protein-DNA interactions. Angew Chem Int Ed Engl. 42:2003;4138-4176
-
(2003)
Angew Chem Int Ed Engl
, vol.42
, pp. 4138-4176
-
-
Boger, D.L.1
Desharnais, J.2
Capps, K.3
-
13
-
-
0037415861
-
Design and application of an alpha-helix-mimetic scaffold based on an oligoamide-foldamer strategy: Antagonism of the Bak BH3/Bcl-xL complex
-
Ernst J.T., Becerril J., Park H.S., Yin H., Hamilton A.D. Design and application of an alpha-helix-mimetic scaffold based on an oligoamide-foldamer strategy: antagonism of the Bak BH3/Bcl-xL complex. Angew Chem Int Ed Engl. 42:2003;535-539
-
(2003)
Angew Chem Int Ed Engl
, vol.42
, pp. 535-539
-
-
Ernst, J.T.1
Becerril, J.2
Park, H.S.3
Yin, H.4
Hamilton, A.D.5
-
14
-
-
0035150803
-
Identification of small-molecule inhibitors of interaction between the BH3 domain and Bcl-xL
-
Degterev A., Lugovskoy A., Cardone M., Mulley B., Wagner G., Mitchison T., Yuan J. Identification of small-molecule inhibitors of interaction between the BH3 domain and Bcl-xL. Nat Cell Biol. 3:2001;173-182
-
(2001)
Nat Cell Biol
, vol.3
, pp. 173-182
-
-
Degterev, A.1
Lugovskoy, A.2
Cardone, M.3
Mulley, B.4
Wagner, G.5
Mitchison, T.6
Yuan, J.7
-
15
-
-
1642512639
-
Small-molecule antagonists of the oncogenic Tcf/beta-catenin protein complex
-
A study in which both a 7000-member natural product library and a 45 000 member synthetic small-molecule library were screened against a protein-protein interaction library. The only inhibitors identified in this study were from the natural product library, whereas the synthetic compound library failed to provide additional hits. This study underscores the importance of screening the appropriate chemistry, whatever the assay technology.
-
Lepourcelet M., Chen Y.N., France D.S., Wang H., Crews P., Petersen F., Bruseo C., Wood A.W., Shivdasani R.A. Small-molecule antagonists of the oncogenic Tcf/beta-catenin protein complex. Cancer Cell. 5:2004;91-102 A study in which both a 7000-member natural product library and a 45 000 member synthetic small-molecule library were screened against a protein-protein interaction library. The only inhibitors identified in this study were from the natural product library, whereas the synthetic compound library failed to provide additional hits. This study underscores the importance of screening the appropriate chemistry, whatever the assay technology.
-
(2004)
Cancer Cell
, vol.5
, pp. 91-102
-
-
Lepourcelet, M.1
Chen, Y.N.2
France, D.S.3
Wang, H.4
Crews, P.5
Petersen, F.6
Bruseo, C.7
Wood, A.W.8
Shivdasani, R.A.9
-
16
-
-
18244370299
-
Generation of an LFA-1 antagonist by the transfer of the ICAM-1 immunoregulatory epitope to a small molecule
-
Gadek T.R., Burdick D.J., McDowell R.S., Stanley M.S., Marsters J.C. Jr., Paris K.J., Oare D.A., Reynolds M.E., Ladner C., Zioncheck K.A., et al. Generation of an LFA-1 antagonist by the transfer of the ICAM-1 immunoregulatory epitope to a small molecule. Science. 295:2002;1086-1089
-
(2002)
Science
, vol.295
, pp. 1086-1089
-
-
Gadek, T.R.1
Burdick, D.J.2
McDowell, R.S.3
Stanley, M.S.4
Marsters Jr., J.C.5
Paris, K.J.6
Oare, D.A.7
Reynolds, M.E.8
Ladner, C.9
Zioncheck, K.A.10
-
17
-
-
0035818921
-
Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 4. Structure-activity relationship of substituents on the benzene ring of the cinnamide
-
Winn M., Reilly E.B., Liu G., Huth J.R., Jae H.S., Freeman J., Pei Z., Xin Z., Lynch J., Kester J., von Geldern T.W., Leitza S., DeVries P., Dickinson R., Mussatto D., Okasinski G.F. Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 4. Structure-activity relationship of substituents on the benzene ring of the cinnamide. J Med Chem. 44:2001;4393-4403
-
(2001)
J Med Chem
, vol.44
, pp. 4393-4403
-
-
Winn, M.1
Reilly, E.B.2
Liu, G.3
Huth, J.R.4
Jae, H.S.5
Freeman, J.6
Pei, Z.7
Xin, Z.8
Lynch, J.9
Kester, J.10
Von Geldern, T.W.11
Leitza, S.12
Devries, P.13
Dickinson, R.14
Mussatto, D.15
Okasinski, G.F.16
-
18
-
-
0033571626
-
Cutting edge: A small molecule antagonist of LFA-1-mediated cell adhesion
-
Kelly T.A., Jeanfavre D.D., McNeil D.W., Woska J.R. Jr., Reilly P.L., Mainolfi E.A., Kishimoto K.M., Nabozny G.H., Zinter R., Bormann B.J., Rothlein R. Cutting edge: a small molecule antagonist of LFA-1-mediated cell adhesion. J Immunol. 163:1999;5173-5177
-
(1999)
J Immunol
, vol.163
, pp. 5173-5177
-
-
Kelly, T.A.1
Jeanfavre, D.D.2
McNeil, D.W.3
Woska Jr., J.R.4
Reilly, P.L.5
Mainolfi, E.A.6
Kishimoto, K.M.7
Nabozny, G.H.8
Zinter, R.9
Bormann, B.J.10
Rothlein, R.11
-
19
-
-
0034816320
-
Binding site elucidation of hydantoin-based antagonists of LFA-1 using multidisciplinary technologies: Evidence for the allosteric inhibition of a protein-protein interaction
-
Last-Barney K., Davidson W., Cardozo M., Frye L.L., Grygon C.A., Hopkins J.L., Jeanfavre D.D., Pav S., Qian C., Stevenson J.M., Tong L., Zindell R., Kelly T.A. Binding site elucidation of hydantoin-based antagonists of LFA-1 using multidisciplinary technologies: evidence for the allosteric inhibition of a protein-protein interaction. J Am Chem Soc. 123:2001;5643-5650
-
(2001)
J Am Chem Soc
, vol.123
, pp. 5643-5650
-
-
Last-Barney, K.1
Davidson, W.2
Cardozo, M.3
Frye, L.L.4
Grygon, C.A.5
Hopkins, J.L.6
Jeanfavre, D.D.7
Pav, S.8
Qian, C.9
Stevenson, J.M.10
Tong, L.11
Zindell, R.12
Kelly, T.A.13
-
20
-
-
0037195181
-
A synthetic HIV-1 Rev inhibitor interfering with the CRM1-mediated nuclear export
-
Daelemans D., Afonina E., Nilsson J., Werner G., Kjems J., De Clercq E., Pavlakis G.N., Vandamme A.M. A synthetic HIV-1 Rev inhibitor interfering with the CRM1-mediated nuclear export. Proc Natl Acad Sci USA. 99:2002;14440-14445
-
(2002)
Proc Natl Acad Sci USA
, vol.99
, pp. 14440-14445
-
-
Daelemans, D.1
Afonina, E.2
Nilsson, J.3
Werner, G.4
Kjems, J.5
De Clercq, E.6
Pavlakis, G.N.7
Vandamme, A.M.8
-
21
-
-
0031841054
-
Design and synthesis of small molecule interleukin-1 receptor antagonists based on a benzene template
-
Sarabu R., Cooper J.P., Cook C.M., Gillespie P., Perrotta A.V., Olson G.L. Design and synthesis of small molecule interleukin-1 receptor antagonists based on a benzene template. Drug Des Discov. 15:1997;191-198
-
(1997)
Drug des Discov
, vol.15
, pp. 191-198
-
-
Sarabu, R.1
Cooper, J.P.2
Cook, C.M.3
Gillespie, P.4
Perrotta, A.V.5
Olson, G.L.6
-
22
-
-
13044262566
-
Mimicry of erythropoietin by a nonpeptide molecule
-
Qureshi S.A., Kim R.M., Konteatis Z., Biazzo D.E., Motamedi H., Rodrigues R., Boice J.A., Calaycay J.R., Bednarek M.A., Griffin P., Gao Y.D., Chapman K., Mark D.F. Mimicry of erythropoietin by a nonpeptide molecule. Proc Natl Acad Sci USA. 96:1999;12156-12161
-
(1999)
Proc Natl Acad Sci USA
, vol.96
, pp. 12156-12161
-
-
Qureshi, S.A.1
Kim, R.M.2
Konteatis, Z.3
Biazzo, D.E.4
Motamedi, H.5
Rodrigues, R.6
Boice, J.A.7
Calaycay, J.R.8
Bednarek, M.A.9
Griffin, P.10
Gao, Y.D.11
Chapman, K.12
Mark, D.F.13
-
23
-
-
13044256383
-
A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity
-
Baba M., Nishimura O., Kanzaki N., Okamoto M., Sawada H., Iizawa Y., Shiraishi M., Aramaki Y., Okonogi K., Ogawa Y., Meguro K., Fujino M. A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity. Proc Natl Acad Sci USA. 96:1999;5698-5703
-
(1999)
Proc Natl Acad Sci USA
, vol.96
, pp. 5698-5703
-
-
Baba, M.1
Nishimura, O.2
Kanzaki, N.3
Okamoto, M.4
Sawada, H.5
Iizawa, Y.6
Shiraishi, M.7
Aramaki, Y.8
Okonogi, K.9
Ogawa, Y.10
Meguro, K.11
Fujino, M.12
-
24
-
-
0033035408
-
Characterization of antiallodynic actions of ALE-0540, a novel nerve growth factor receptor antagonist, in the rat
-
Owolabi J.B., Rizkalla G., Tehim A., Ross G.M., Riopelle R.J., Kamboj R., Ossipov M., Bian D., Wegert S., Porreca F., Lee D.K. Characterization of antiallodynic actions of ALE-0540, a novel nerve growth factor receptor antagonist, in the rat. J Pharmacol Exp Ther. 289:1999;1271-1276
-
(1999)
J Pharmacol Exp Ther
, vol.289
, pp. 1271-1276
-
-
Owolabi, J.B.1
Rizkalla, G.2
Tehim, A.3
Ross, G.M.4
Riopelle, R.J.5
Kamboj, R.6
Ossipov, M.7
Bian, D.8
Wegert, S.9
Porreca, F.10
Lee, D.K.11
-
25
-
-
0034691130
-
Structure-based discovery of an organic compound that binds Bcl-2 protein and induces apoptosis of tumor cells
-
Wang J.L., Liu D., Zhang Z.J., Shan S., Han X., Srinivasula S.M., Croce C.M., Alnemri E.S., Huang Z. Structure-based discovery of an organic compound that binds Bcl-2 protein and induces apoptosis of tumor cells. Proc Natl Acad Sci USA. 97:2000;7124-7129
-
(2000)
Proc Natl Acad Sci USA
, vol.97
, pp. 7124-7129
-
-
Wang, J.L.1
Liu, D.2
Zhang, Z.J.3
Shan, S.4
Han, X.5
Srinivasula, S.M.6
Croce, C.M.7
Alnemri, E.S.8
Huang, Z.9
-
26
-
-
2442508985
-
Critical upstream signals of cytochrome c release induced by a novel Bcl-2 inhibitor
-
Feb 13 (in press).
-
An J, Chen Y, Huang Z: Critical upstream signals of cytochrome c release induced by a novel Bcl-2 inhibitor. J Biol Chem 2004 Feb 13 (in press).
-
(2004)
J Biol Chem
-
-
An, J.1
Chen, Y.2
Huang, Z.3
-
27
-
-
0035818885
-
Discovery of small-molecule inhibitors of Bcl-2 through structure-based computer screening
-
Enyedy I.J., Ling Y., Nacro K., Tomita Y., Wu X., Cao Y., Guo R., Li B., Zhu X., Huang Y., Long Y.Q., Roller P.P., Yang D., Wang S. Discovery of small-molecule inhibitors of Bcl-2 through structure-based computer screening. J Med Chem. 44:2001;4313-4324
-
(2001)
J Med Chem
, vol.44
, pp. 4313-4324
-
-
Enyedy, I.J.1
Ling, Y.2
Nacro, K.3
Tomita, Y.4
Wu, X.5
Cao, Y.6
Guo, R.7
Li, B.8
Zhu, X.9
Huang, Y.10
Long, Y.Q.11
Roller, P.P.12
Yang, D.13
Wang, S.14
-
28
-
-
0037414274
-
Discovery of a potent small molecule IL-2 inhibitor through fragment assembly
-
Braisted A.C., Oslob J.D., Delano W.L., Hyde J., McDowell R.S., Waal N., Yu C., Arkin M.R., Raimundo B.C. Discovery of a potent small molecule IL-2 inhibitor through fragment assembly. J Am Chem Soc. 125:2003;3714-3715
-
(2003)
J Am Chem Soc
, vol.125
, pp. 3714-3715
-
-
Braisted, A.C.1
Oslob, J.D.2
Delano, W.L.3
Hyde, J.4
McDowell, R.S.5
Waal, N.6
Yu, C.7
Arkin, M.R.8
Raimundo, B.C.9
-
29
-
-
0035895350
-
Chalcone derivatives antagonize interactions between the human oncoprotein MDM2 and p53
-
Stoll R., Renner C., Hansen S., Palme S., Klein C., Belling A., Zeslawski W., Kamionka M., Rehm T., Muhlhahn P., et al. Chalcone derivatives antagonize interactions between the human oncoprotein MDM2 and p53. Biochemistry. 40:2001;336-344
-
(2001)
Biochemistry
, vol.40
, pp. 336-344
-
-
Stoll, R.1
Renner, C.2
Hansen, S.3
Palme, S.4
Klein, C.5
Belling, A.6
Zeslawski, W.7
Kamionka, M.8
Rehm, T.9
Muhlhahn, P.10
-
30
-
-
10744221485
-
In vivo activation of the p53 pathway by small-molecule antagonists of MDM2
-
Identification of SMPPIIs with therapeutic potential using a structural biological approach in a pharmaceutical industrial setting.
-
Vassilev L.T., Vu B.T., Graves B., Carvajal D., Podlaski F., Filipovic Z., Kong N., Kammlott U., Lukacs C., Klein C., et al. In vivo activation of the p53 pathway by small-molecule antagonists of MDM2. Science. 303:2004;844-848 Identification of SMPPIIs with therapeutic potential using a structural biological approach in a pharmaceutical industrial setting.
-
(2004)
Science
, vol.303
, pp. 844-848
-
-
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
Klein, C.10
-
31
-
-
0036525503
-
An organic CD4 inhibitor reduces the clinical and pathological symptoms of acute experimental allergic encephalomyelitis
-
Edling A.E., Choksi S., Huang Z., Korngold R. An organic CD4 inhibitor reduces the clinical and pathological symptoms of acute experimental allergic encephalomyelitis. J Autoimmun. 18:2002;169-179
-
(2002)
J Autoimmun
, vol.18
, pp. 169-179
-
-
Edling, A.E.1
Choksi, S.2
Huang, Z.3
Korngold, R.4
-
32
-
-
0037133575
-
Small-molecule antagonists of Myc/Max dimerization inhibit Myc-induced transformation of chicken embryo fibroblasts
-
Berg T., Cohen S.B., Desharnais J., Sonderegger C., Maslyar D.J., Goldberg J., Boger D.L., Vogt P.K. Small-molecule antagonists of Myc/Max dimerization inhibit Myc-induced transformation of chicken embryo fibroblasts. Proc Natl Acad Sci USA. 99:2002;3830-3835
-
(2002)
Proc Natl Acad Sci USA
, vol.99
, pp. 3830-3835
-
-
Berg, T.1
Cohen, S.B.2
Desharnais, J.3
Sonderegger, C.4
Maslyar, D.J.5
Goldberg, J.6
Boger, D.L.7
Vogt, P.K.8
-
33
-
-
0842325666
-
Inhibition of the p53-MDM2 interaction: Targeting a protein-protein interface
-
Chene P. Inhibition of the p53-MDM2 interaction: targeting a protein-protein interface. Mol Cancer Res. 2:2004;20-28
-
(2004)
Mol Cancer Res
, vol.2
, pp. 20-28
-
-
Chene, P.1
-
35
-
-
0034266313
-
Drug-like Index: A New Approach to Measure Drug-like Compounds and Their Diversity
-
Xu J., Stevenson J. Drug-like Index: A New Approach to Measure Drug-like Compounds and Their Diversity. J Chem Inf Comput Sci. 40:2000;1177-1187
-
(2000)
J Chem Inf Comput Sci
, vol.40
, pp. 1177-1187
-
-
Xu, J.1
Stevenson, J.2
-
36
-
-
0035289779
-
Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
-
Lipinski C.A., Lombardo F., Dominy B.W., Feeney P.J. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev. 46:2001;3-26
-
(2001)
Adv Drug Deliv Rev
, vol.46
, pp. 3-26
-
-
Lipinski, C.A.1
Lombardo, F.2
Dominy, B.W.3
Feeney, P.J.4
-
37
-
-
1642581072
-
Design, synthesis, and in vitro biological evaluation of small molecule inhibitors of estrogen receptor alpha coactivator binding
-
An example in which SMPPIIs effective against estrogen receptor via a novel mode of action were developed using a rational design chemistry approach. Rather than antagonizing estrogen receptor directly, this study describes SMPPIIs that inhibit binding of co-activator to the receptor. In the absence of co-activator, the receptor lacks activity.
-
Rodriguez A.L., Tamrazi A., Collins M.L., Katzenellenbogen J.A. Design, synthesis, and in vitro biological evaluation of small molecule inhibitors of estrogen receptor alpha coactivator binding. J Med Chem. 47:2004;600-611 An example in which SMPPIIs effective against estrogen receptor via a novel mode of action were developed using a rational design chemistry approach. Rather than antagonizing estrogen receptor directly, this study describes SMPPIIs that inhibit binding of co-activator to the receptor. In the absence of co-activator, the receptor lacks activity.
-
(2004)
J Med Chem
, vol.47
, pp. 600-611
-
-
Rodriguez, A.L.1
Tamrazi, A.2
Collins, M.L.3
Katzenellenbogen, J.A.4
-
38
-
-
0037416141
-
The small-molecule approach to biology: Chemical genetics and diversity-oriented organic synthesis make possible the systematic exploration of biology
-
Schreiber S.L. The small-molecule approach to biology: Chemical genetics and diversity-oriented organic synthesis make possible the systematic exploration of biology. Chem Eng News. 81:2003;51-61
-
(2003)
Chem Eng News
, vol.81
, pp. 51-61
-
-
Schreiber, S.L.1
-
39
-
-
3042799070
-
A planning strategy for diversity-oriented synthesis
-
Burke M.D., Schreiber S.L. A planning strategy for diversity-oriented synthesis. Angew Chem Int Ed Engl. 43:2004;46-58
-
(2004)
Angew Chem Int Ed Engl
, vol.43
, pp. 46-58
-
-
Burke, M.D.1
Schreiber, S.L.2
-
40
-
-
0033556222
-
Simultaneous visualization of the translocation of protein kinase C alpha-green fluorescent protein hybrids and intracellular calcium concentrations
-
Almholt K., Arkhammar P.O., Thastrup O., Tullin S. Simultaneous visualization of the translocation of protein kinase C alpha-green fluorescent protein hybrids and intracellular calcium concentrations. Biochem J. 337:1999;211-218
-
(1999)
Biochem J
, vol.337
, pp. 211-218
-
-
Almholt, K.1
Arkhammar, P.O.2
Thastrup, O.3
Tullin, S.4
-
41
-
-
0038573885
-
Occupancy of the catalytic site of the PDE4A4 cyclic AMP phosphodiesterase by rolipram triggers the dynamic redistribution of this specific isoform in living cells tthrough a cyclic AMP independent process
-
Terry R., Cheung Y.-F., Præstegaard M., Baillie G.S., Huston E., Gall I., Adams D.R., Houslay M.D. Occupancy of the catalytic site of the PDE4A4 cyclic AMP phosphodiesterase by rolipram triggers the dynamic redistribution of this specific isoform in living cells tthrough a cyclic AMP independent process. Cell Signal. 15:2003;955-971
-
(2003)
Cell Signal
, vol.15
, pp. 955-971
-
-
Terry, R.1
Cheung, Y.-F.2
Præstegaard, M.3
Baillie, G.S.4
Huston, E.5
Gall, I.6
Adams, D.R.7
Houslay, M.D.8
-
42
-
-
2342540450
-
® screen
-
Hits with several modes of action in the p38-MAP kinase pathway were discovered in a high content cell-based translocation assay screen.
-
® screen. Assay Drug Dev Technol. 2:2004;7-20 Hits with several modes of action in the p38-MAP kinase pathway were discovered in a high content cell-based translocation assay screen.
-
(2004)
Assay Drug Dev Technol
, vol.2
, pp. 7-20
-
-
Almholt, D.L.C.1
Loechel, F.2
Nielsen, S.J.3
Krog-Jensen, C.4
Terry, R.5
Bjørn, S.P.6
Pedersen, H.C.7
Præstegaard, M.8
Møller, S.9
Heide, M.10
-
43
-
-
3342897320
-
Identification of Akt pathway inhibitors using Redistribution® screening on the FLIPR and the in Cell 3000 Analyzer
-
in press.
-
Lundholt BK, Linde, Loechel S, Pedersen HC, Møller S, Præstegaard M, Scudder K, Bjørn SP, Heide M, Arknammar POG, Terry R, Nielsen SJ: Identification of Akt pathway inhibitors using Redistribution® screening on the FLIPR and the IN Cell 3000 Analyzer. J Biomol Screen 2004, 9: in press.
-
(2004)
J Biomol Screen
, pp. 9
-
-
Lundholt, B.K.1
Linde2
Loechel, S.3
Pedersen, H.C.4
Møller, S.5
Præstegaard, M.6
Scudder, K.7
Bjørn, S.P.8
Heide, M.9
Pog, A.10
Terry, R.11
Nielsen, S.J.12
-
44
-
-
0347747970
-
A chemical genetic screen identifies inhibitors of regulated nuclear export of a Forkhead transcription factor in PTEN-deficient tumor cells
-
Kau T.R., Schroeder F., Ramaswamy S., Wojciechowski C.L., Zhao J.J., Roberts T.M., Clardy J., Sellers W.R., Silver P.A. A chemical genetic screen identifies inhibitors of regulated nuclear export of a Forkhead transcription factor in PTEN-deficient tumor cells. Cancer Cell. 4:2003;463-476
-
(2003)
Cancer Cell
, vol.4
, pp. 463-476
-
-
Kau, T.R.1
Schroeder, F.2
Ramaswamy, S.3
Wojciechowski, C.L.4
Zhao, J.J.5
Roberts, T.M.6
Clardy, J.7
Sellers, W.R.8
Silver, P.A.9
-
46
-
-
1542756081
-
Green fluorescent protein-tagged beta-arrestin translocation as a measure of G protein-coupled receptor activation
-
Ferguson S.S., Caron M.G. Green fluorescent protein-tagged beta-arrestin translocation as a measure of G protein-coupled receptor activation. Methods Mol Biol. 237:2004;121-126
-
(2004)
Methods Mol Biol
, vol.237
, pp. 121-126
-
-
Ferguson, S.S.1
Caron, M.G.2
-
47
-
-
0042476427
-
Locating a protein-protein interaction in living cells via split Renilla luciferase complementation
-
Kaihara A., Kawai Y., Sato M., Ozawa T., Umezawa Y. Locating a protein-protein interaction in living cells via split Renilla luciferase complementation. Anal Chem. 75:2003;4176-4181
-
(2003)
Anal Chem
, vol.75
, pp. 4176-4181
-
-
Kaihara, A.1
Kawai, Y.2
Sato, M.3
Ozawa, T.4
Umezawa, Y.5
-
48
-
-
3343014678
-
Measuring drug action in the cellular context using protein-fragment complementation assays
-
Yu H., West M., Keon B.H., Bilter G.K., Owens S., Lamerdin J., Westwick J.K. Measuring drug action in the cellular context using protein-fragment complementation assays. Assay Drug Dev Technol. 1:2003;811-822
-
(2003)
Assay Drug Dev Technol
, vol.1
, pp. 811-822
-
-
Yu, H.1
West, M.2
Keon, B.H.3
Bilter, G.K.4
Owens, S.5
Lamerdin, J.6
Westwick, J.K.7
-
49
-
-
2142754958
-
Allosteric inhibitors of inducible nitric oxide synthase dimerization discovered via combinatorial chemistry
-
McMillan K., Adler M., Auld D.S., Baldwin J.J., Blasko E., Browne L.J., Chelsky D., Davey D., Dolle R.E., Eagen K.A., et al. Allosteric inhibitors of inducible nitric oxide synthase dimerization discovered via combinatorial chemistry. Proc Natl Acad Sci USA. 97:2000;1506-1511
-
(2000)
Proc Natl Acad Sci USA
, vol.97
, pp. 1506-1511
-
-
McMillan, K.1
Adler, M.2
Auld, D.S.3
Baldwin, J.J.4
Blasko, E.5
Browne, L.J.6
Chelsky, D.7
Davey, D.8
Dolle, R.E.9
Eagen, K.A.10
-
50
-
-
0037016750
-
Mechanistic studies with potent and selective inducible nitric-oxide synthase dimerization inhibitors
-
An illustration of the advantages of cell-based assays for primary screening. A library screened against a cell-based iNOS assay identified potent, progressable hits not identified in a screen of the same compounds against a catalytic activity assay based on active, partially purified iNOS holo-enzyme. Functional iNOS is a dimer, and the hits identified only in the cell-based assay effectively inhibit dimerization - and thus activity.
-
Blasko E., Glaser C.B., Devlin J.J., Xia W., Feldman R.I., Polokoff M.A., Phillips G.B., Whitlow M., Auld D.S., McMillan K., et al. Mechanistic studies with potent and selective inducible nitric-oxide synthase dimerization inhibitors. J Biol Chem. 277:2002;295-302 An illustration of the advantages of cell-based assays for primary screening. A library screened against a cell-based iNOS assay identified potent, progressable hits not identified in a screen of the same compounds against a catalytic activity assay based on active, partially purified iNOS holo-enzyme. Functional iNOS is a dimer, and the hits identified only in the cell-based assay effectively inhibit dimerization - and thus activity.
-
(2002)
J Biol Chem
, vol.277
, pp. 295-302
-
-
Blasko, E.1
Glaser, C.B.2
Devlin, J.J.3
Xia, W.4
Feldman, R.I.5
Polokoff, M.A.6
Phillips, G.B.7
Whitlow, M.8
Auld, D.S.9
McMillan, K.10
-
52
-
-
3142781225
-
Small-molecule inhibitors of protein-protein interactions: Progressing towards the dream
-
Arkin M.R., Wells J.A. Small-molecule inhibitors of protein-protein interactions: progressing towards the dream. Nat Rev Drug Disc. 3:2004;301-317
-
(2004)
Nat Rev Drug Disc
, vol.3
, pp. 301-317
-
-
Arkin, M.R.1
Wells, J.A.2
-
53
-
-
2442664118
-
Rational design and characterizaton of a Rac GTPase-specific small molecule inhibitor
-
Gao Y., Dickerson J.B., Guo F., Zheng J., Zheng Y. Rational design and characterizaton of a Rac GTPase-specific small molecule inhibitor. Proc Natl Acad Sci USA. 101:2004;7618-7623
-
(2004)
Proc Natl Acad Sci USA
, vol.101
, pp. 7618-7623
-
-
Gao, Y.1
Dickerson, J.B.2
Guo, F.3
Zheng, J.4
Zheng, Y.5
-
54
-
-
2442714017
-
Selective inhibition of calcineurin-NFAT signaling by blocking protein-protein interaction with small organic molecules
-
Roehrl M.H.A., Kang S., Aramburu J., Wagner G., Rao A., Hogan P.G. Selective inhibition of calcineurin-NFAT signaling by blocking protein-protein interaction with small organic molecules. Proc Natl Acad Sci USA. 101:2004;7554-7559
-
(2004)
Proc Natl Acad Sci USA
, vol.101
, pp. 7554-7559
-
-
Roehrl, M.H.A.1
Kang, S.2
Aramburu, J.3
Wagner, G.4
Rao, A.5
Hogan, P.G.6
|