Application of Combinatorial Libraries and Protein Engineering to the Discovery of Novel Anti-Thrombotic Drugs

• References

• 1 Lam KS, Salmon SE, Hersh EM, Hruby VJ, Kazmierski WM, Knapp RJ. A new type of synthetic peptide library for identifying ligand-binding activity. Nature 1991; 354: 82-84
• 2 Houghten RA, Pinilla C, Blondelle SE, Appel JR, Dooley CT, Cuervo JH. Generation and use of synthetic peptide combinatorial libraries for basic research and drug discovery. Nature 1991; 354: 84-86
• 3 Simon RJ, Kania RS. et al. Peptoids: a modular approach to drug discovery. Proc Natl Acad Sci USA 1992; 89: 9367-9371
• 4 Gallop MA, Barrett RW, Dower WJ, Fodor SP, Gordon EM. Applications of combinatorial technologies to drug discovery. I. Background and peptide combinatorial libraries (Perspective). J Med Chem 1994; 37: 1233-1251
• 5 Gordon EM, Barrett RW, Dower WJ, Fodor SP, Gallop MA. Applications of combinatorial technologies to drug discovery. 2. Combinatorial organic synthesis, library screening strategies, and future directions. J Med Chem 1994; 37: 1385-1401
• 6 Muller YA, Ultsch MH, Kelley RF, de Vos AM. Structure of the extracellular domain of human tissue factor: Location of the factor Vila binding site. Biochemistry 1994; 33: 10864-10870
• 7 Gibbs CS, McCurdy SN, Leung LL K, Paborsky LR. Identification of the factor Vila binding site on tissue factor by homologous loop swap and alanine scanning mutagenesis. Biochemistry 1994; 33: 14003-14010
• 8 Ellington AD, Szostak JW. In vitro selection of RNA molecules that bind specific ligands. Nature 1990; 346: 818-822
• 9 Joyce GF. Amplification, mutation, and selection of catalytic RNA. Gene 1989; 82: 83-87
• 10 Blackwell TK, Weintraub H. Differences and similarities in DNA-binding preferences of MyoD and E2A protein complexes revealed by binding site selection. Science 1990; 250: 1104-1110
• 11 Bock LC, Griffin LC, Latham JA, Vermaas EH, Toole JJ. Selection of single-stranded DNA molecules that bind and inhibit human thrombin. Nature 1992; 355: 564-566
• 12 Wang KY, McCurdy S, Shea RG, Swaminathan S, Bolton PH. A DNA aptamer which binds to and inhibits thrombin exhibits a new structural motif for DNA. Biochemistry 1993; 32: 1899-1904
• 13 Blackburn EH. Structure and function of telomeres (review). Nature 1991; 350: 569-573
• 14 Li WX, Kaplan AV, Grant GW, Toole JJ, Leung LL K. A novel nucleotide-based thrombin inhibitor inhibits clot-bound thrombin and reduces arterial thrombin formation. Blood 1994; 83: 677-682
• 15 Griffin LC, Tidmarsh GF, Bock LC, Toole JJ, Leung LL K. In vivo anticoagulant properties of a novel nucleotide-based thrombin inhibitor and demonstration of regional anticoagulation in extracorporeal circuits. Blood 1993; 81: 3271-3276
• 16 DeAnda A, Coutre SE, Moon MR. et al. Pilot study of the efficacy of a thrombin inhibitor for use during cardiopulmonary bypass. Ann Thorac Surg 1994; 58: 344-350
• 17 Paborsky LR, McCurdy SN, Griffin LC, Toole JJ, Leung LL K. The single-stranded DNA aptamer-binding site of human thrombin. J Biol Chem 1993; 268: 20808-20811
• 18 Jin L, Cohen FE, Wells JA. Structure from function: screening structural models with functional data. Proc Natl Acad Sci USA 1994; 91: 113-117
• 19 Jayawickreme CK, Graminski GF, Quillan JM, Lerner MR. Creation and functional screening of a multi-use peptide library. Proc Natl Acad Sci USA 1994; 91: 1614-1618