Small molecule-dependent genetic selection in stochastic nanodroplets as a means of detecting protein-ligand interactions on a large scale

Chemistry and Biology

Volumn 4, Issue 12, 1997, Pages 961-968

  Borchardt, Allen ^a   Liberles, Stephen D ^a   Biggar, Stephen R ^b   Crabtree, Gerald R ^b   Schreiber, Stuart L ^a  

^a HARVARD UNIVERSITY   (United States)

^b STANFORD UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

Chemical genetics; Combinatorial chemistry; High throughput screening; Nanodroplets

Indexed keywords

EID: 0031444011     PISSN: 10745521     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1074-5521(97)90304-5     Document Type: Article

References (17)

1. Schena, M., Shalon, D., Heller, R., Chai, A. & Brown, P.O. (1996). Parallel human genome analysis: microarray-based expression monitoring of 1000 genes. Proc. Natl Acad. Sci. USA 93, 10614-10619.
2. Crabtree, G.R. & Schreiber, S.L. (1996). Three-part inventions: intracellular signaling and induced proximity. Trends Biochem. Sci. 21, 418-422.
3. Austin, D.J., Crabtree, G.R. & Schreiber, S.L. (1994). Proximity versus allostery: the role of regulated protein dimerization in biology. Chem. Biol. 1, 131-136.
4. Crews, C.M. (1996). Deciphering isozyme function: exploring cell biology with chemistry in the post-genomic era. Chem. Biol. 3, 961-965.
5. Hung, D.T., Jamison, T.F. & Schreiber, S.L. (1996). Understanding and controlling the cell cycle with natural products. Chem. Biol. 3, 623-639.
6. Furka, A., Sebestyen, M., Asgedom, M. & Dibo, G. (1991). General method for rapid synthesis of multicomponent peptide mixtures. Int. J. Peptide Prot. Res. 37, 487-493.
7. Lam, K.S., Salmon, S.E., Hersh, E.M., Hruby, V.J., Kazmierski, W.M. & Knapp, R.J. (1991). A new type of synthetic peptide library for identifying ligand-binding activity. Nature 354, 82-84.
8. Quillan, J.M., Jayawickreme, C.K. & Lerner, M.R., (1995). Combinatorial diffusion assay used to identify topically active melanocyte-stimulating hormone receptor antagonists. Proc. Natl Acad. Sci. USA 92, 2894-2898.
9. Schullek, J.R., Butler, J.H., Ni, Z.-J., Chen, D. & Yuan, Z. (1997). A high density screening format for encoded combinatorial libraries: Assay miniaturization and its application to enzymatic reactions. Anal. Biochem. 246, 20-29.
10. Motamedi, H., Cai, S.J., Shafiee, A. & Elliston, K.O. (1997). Structural organization of a multifunctional polyketide synthase involved in the biosynthesis of the macrolide immunosuppressant FK506. Euro. J. Biochem. 244, 74-80.
11. Aparicio, J.F., Molnar, I., Schwecke, T., Konig, A., Haydock, S.F., Khaw, LE., Staunton, J. & Leadlay, P.F. (1996). Organization of the biosynthetic gene cluster for rapamycin in Streptomyces hygroscopicus: analysis of the enzymatic domains in the modular polyketide synthase. Gene 169, 9-16.
12. You, A.J., Jackman, R.J., Whitesides, G.M. & Schreiber, S.L. (1997). Miniaturized arrayed assay format for detecting small molecule-protein interactions in cells. Chem. Biol. 4, 969-975.
13. Heitman, J., Movva, N.R., Hiestand, P.C. & Hall, M.N. (1991). Targets for cell cycle arrest by the immunosuppressant rapamycin in yeast. Science 253, 905-909.
14. Chen, J., Zheng, X.F., Brown, E.J. & Schreiber, S.L. (1995). Identification of an 11 kDa FKBP12-rapamycin-binding domain within the 289-kDa FKBP12-rapamycin-associated protein and characterization of a critical serine residue. Proc. Natl Acad. Sci. USA 92, 4947-4951.
15. Ho, S.N., Biggar, S.R., Spencer, D.M., Schreiber, S.L. & Crabtree, G.R. (1996). Dimeric ligands define a role for transcriptional activation domains in reinitiation. Nature 382, 822-826.
16. Belshaw, P.J., Ho, S.N., Crabtree, G.R. & Schreiber, S.L. (1996). Controlling protein association and subcellular localization with a synthetic ligand that induces heterodimerization of proteins. Proc. Natl Acad. Sci. USA 93, 4604-4607.
17. Licitra, E.J. & Liu, J.O. (1996). A three-hybrid system for detecting small ligand-protein receptor interactions. Proc. Natl Acad. Sci. USA 93, 12817-12821.