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Liang R, Van L, Loebach J, Ge M, Uozumi Y, Sekanina K, Horan N, Gildersleeve J, Thompson C, Smith A, Biswas K, Still WC, Kahne D: Parallel synthesis and screening of a solid phase carbohydrate library. Science (1996) 274:1520-1522. A binary encoded library of carbohydrates was used to identify novel ligands for a lectin.
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Hwang S, Tamilarasu N, Ryan K, Huq l, Richter S, Still WC, Rana TM: Inhibition of gene expression in human ceils through small molecule - RNA interactions. Proc Natl Acad Sei USA (1999) 96:12997-13002. A binary encoded library of tripeptides was used to identify ligands for the bulge loop of HIV-1 TAR RNA. NMR analysis confirmed the binding site. One of the ligands inhibited Tat-induced trans activation in vivo.
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Burbaum JJ, Ohlmeyer MH, Reader JC, Henderson l, Dillard LW, Li G, Rändle TL, Sigal NH, Chelsky D, Baldwin JJ: A paradigm for drug discovery employing encoded combinatorial libraries. Proc Nail Acad Sei USA (1995) 92:6027-6031. Two binary encoded libraries were used to identify nanomolar inhibitors of carbonic anhydrase in an activity-based assay.
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Hortick RA, Ohlmeyer MH, Stroke IL, Strahl B, Pan G, Schilling AE, Paradkar V, Quintero JG, You M, Riviello C, Thorn MB, Damaj B, Fitzpatrick VD, Dolle RE, Webb ML, Baldwin JJ, Sigal NH: Small molecule antagonists of the bradykinin B1 receptor. Immunopharmacology (1999) 43:169-177.
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Nicolaou KC, Vourloumis D, Li T, Pastor J, Winssinger N, He Y, Ninkovic S, Sarabia F, Vallberg H, Roschangar F, King NP, Rnlay MR, Giannakakou P, Verdier-Pinard P, Hamel E: Designed epothilones: Combinatorial synthesis, tubulin assembly properties, and cytotoxic action against Taxol-resistant tumor cells. AngewChem Int Ed Engl (1997) 36:2097-2103.
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Lu AT, Solas DW, Gore MA, Maclean D, Shah NH, Coffin JM, Bhinderwala NS, Wang Y, Tsutsui KT, Look GC, Campbell DA, Hale RL, Navre M, DeLuca-Flaherty CR: 1447-1453. A novel lawn-based screening fonnat was used to identify antimicrobials from a binary encoded library of triazines.
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Silen JL, Lu AT, Solas DW, Gore MA, Maclean D, Shah NH, Coffin JM, Bhinderwala NS, Wang Y, Tsutsui KT, Look GC, Campbell DA, Hale RL, Navre M, DeLuca-Flaherty CR: Screening for novel antimicrobials from encoded combinatorial libraries by using a two-dimensional agar format. Antimicrob Agents Chemother (1998) 42:1447-1453. A novel lawn-based screening fonnat was used to identify antimicrobials from a binary encoded library of triazines.
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Adler M, Auld DS, Baldwin JJ, Blasko E, Browne LJ, Chelsky D, Davey D, Dolle RE, Eagen KA, Erickson S, Feldman Rl, Glaser CB, Mallari C, Morrissey MM, Ohlmeyer MH, Pan G, Parkinson JF, Phillips GB, Polokoff MA, Sigal NH, Vergona R, Whitlow M, Young TA, Devlin JJ: 1506-1511. A binary encoded library of pyrimidine imidazoles was used to identify selective nanomolar inhibitors of //VOS. Crystallographic analysis indicated that the inhibitors act by preventing /A/OS dimerization rather than binding in the active site.
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McMillan K, Adler M, Auld DS, Baldwin JJ, Blasko E, Browne LJ, Chelsky D, Davey D, Dolle RE, Eagen KA, Erickson S, Feldman Rl, Glaser CB, Mallari C, Morrissey MM, Ohlmeyer MH, Pan G, Parkinson JF, Phillips GB, Polokoff MA, Sigal NH, Vergona R, Whitlow M, Young TA, Devlin JJ: Allosteric inhibitors of inducible nitric oxide synthase dimerization discovered via combinatorial chemistry. Proc Natl Acad Sei USA (2000) 97:1506-1511. A binary encoded library of pyrimidine imidazoles was used to identify selective nanomolar inhibitors of //VOS. Crystallographic analysis indicated that the inhibitors act by preventing /A/OS dimerization rather than binding in the active site.
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Proc Natl Acad Sei USA
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