References

	Bachand, B., DiMaio, J., Siddiqui, M.A. (1999) Synthesis and structure-activity relationship of potent bicyclic lactam thrombin inhibitors. Bioorg Med Chem Lett, 9, 913-918.
	Boatman, P.D., Ogbu, C.O., Eguchi, M., Kim, H.O., Nakanishi, H., Cao, B., Shea, J.P., Kahn, M. (1999)Secondary structure peptide mimetics: design, synthesis, and evaluation of beta-strand mimetic thrombin inhibitors.J Med Chem, 42, 1367-1375.
	Borkakoti, N., Winkler, F.K., Williams, D.H., D'Arcy, A., Broadhurst, M.J., Brown, P.A., Johnson, W.H., Murray, E.J. (1994) Structure of the catalytic domain of human fibroblast collagenase complexed with an inhibitor. Nat Struct Biol, 1, 106-110.
	Brickmann, K., Yuan, Z., Sethson, I., Somfai, P. and Kihlberg, J. (1999) Synthesis of Conformationally Restricted Mimetics of y-Turns and Incorporation into Desmopressin, an Analogue of the Peptide Hormone Vasopressin. Chemistry - A European Journal, 5, 2241-2253 .
	Callahan, J. F., Newlander, K. A., Burgess, J. L., Eggleston, D. S., Nichols, A., Wong, A. and Huffman, W. F. (1993) The use of y-turn mimetics to define peptide secondary structure. Tetrahedron, 49, 3479-3488.
	Callahan, J.F., Bean, J.W., Burgess, J.L., Eggleston, D.S., Hwang, S.M., Kopple, K.D., Koster, P.F., Nichols, A., Peishoff, C.E., Samanen, J.M. et al. (1992) Design and synthesis of a C7 mimetic for the predicted gamma-turn conformation found in several constrained RGD antagonists. J Med Chem, 35, 3970-3972.
	Coburn, C.A., Rush, D.M., Williams, P.D., Homnick, C., Lyle, E.A., Lewis, S.D., Lucas, B.J. Jr, Di Muzio-Mower, J.M., Juliano, M., Krueger, J.A., Vastag, K., Chen, I.W.and Vacca, J.P. (2000) Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors. Bioorg Med Chem Lett, 10, 1069-1072.
	Cossy, J. and Belotti, D. (2001) A short synthesis of argatroban. a potent selective thrombin inhibitor. Bioorg Med Chem Lett, 11, 1989-1992.
	de Laszlo, S.E., Allen, E.E., Li, B., Ondeyka, D., Rivero, R., Malkowitz, L., Molineaux, C., Siciliano, S.J., Springer, M.S., Greenlee, W.J. and Mantlo, N. (1997) A nonpeptidic agonist ligand of the human C5a receptor: Synthesis, binding affinity optimization and functional characterization. Bioorg Med Chem Lett, 7, 213-218.
	Ding, C.Z., Batorsky, R., Bhide, R., Chao, H.J., Cho, Y., Chong, S., Gullo-Brown, J., Guo, P., Kim, S.H., Lee, F., Leftheris, K., Miller, A., Mitt, T., Patel, M., Penhallow, B.A., Ricca, C., Rose, W.C., Schmidt, R., Slusarchyk, W.A., Vite, G., Yan, N., Manne, V. and Hunt, J.T. (1999) Discovery and structure-activity relationships of imidazole-containing tetrahydrobenzodiazepine inhibitors of farnesyltransferase. J Med Chem, 42, 5241-5253.
	Ernst, J.T., Becerril, J., Park, H.S., Yin, H. and Hamilton, A.D. (2003) 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, 535-539.
	Estiarte, M.A., Rubiralta, M., Diez, A., Thormann, M. and Giralt, E. (2000) Oxazolopiperidin-2-ones as type II' beta-turn mimetics: synthesis and conformational analysis. J Org Chem, 65, 6992-6999.
	Ferguson, M.D., Meara, J.P., Nakanishia, H., Lee, M.S. and Kahn, M. (1997) The Development of Hydrazide y-Turn Mimetics. Tetrahedron Lett, 38, 6961-6964.
	Fink, B.E., Kym, P.R. and Katzenellenbogen, J.A. (1998) Design, Synthesis, and Conformational Analysis of a Proposed Type I ß-Turn Mimic. J Am Chem Soc, 120, 4334-4344.
	Flynn, G.A., Beight, D.W., Mehdi, S., Koehl, J.R., Giroux, E.L., French, J.F., Hake, P.W.and Dage, R.C. (1993) Application of a conformationally restricted Phe-Leu dipeptide mimetic to the design of a combined inhibitor of angiotensin I-converting enzyme and neutral endopeptidase 24.11. J Med Chem, 36, 2420-2423.
	Freidinger, R.M. (2003) Design and synthesis of novel bioactive peptides and peptidomimetics. J Med Chem, 46, 5553-5566.
	Freidinger, R.M., Schwenk Perlow, D., Veber, D.F. (1982) Protected lactam-bridged dipeptides for use as conformational constraints in peptides. J Org Chem, 47, 104-109.
	Genin, M.J., Ojala, W.H., Gleason, W.B. and Johnson, R.L. (1993) Synthesis and crystal structure of a peptidomimetic containing the (R)-4.4-spiro lactam type-II .beta.-turn mimic. J Org Chem, 58, 2334-2337.
	Hay, B.A., Cole, B.M., DiCapua, F.M., Kirk, G.W., Murray, M.C., Nardone, R.A., Pelletier, D.J., Ricketts, A.P., Robertson, A.S. and Siegel, T.W. (2001) Small molecule somatostatin receptor subtype-2 antagonists. Bioorg Med Chem Lett, 11, 2731-2734.
	Henke, B.R., Aquino, C.J., Birkemo, L.S., Croom, D.K., Dougherty, R.W. Jr, Ervin, G.N., Grizzle, M.K., Hirst, G.C., James, M.K., Johnson, M.F., Queen, K.L., Sherrill, R.G., Sugg, E.E., Suh, E.M., Szewczyk, J.W., Unwalla, R.J., Yingling, J. and Willson, T.M. (1997) Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists. J Med Chem, 40, 2706-2725.
	Henke, B.R., Willson, T.M., Sugg, E.E., Croom, D.K., Dougherty, R.W. Jr, Queen, K.L., Birkemo, L.S., Ervin, G.N., Grizzle, M.K., Johnson, M.F. and James, M.K. (1996) 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines: CCK-A agonists that demonstrate oral activity as satiety agents. J Med Chem, 39, 2655-2658.
	Hinds, M.G., Welsh, J.H., Brennand, D.M., Fisher, J., Glennie, M.J., Richards, N.G., Turner, D.L. and Robinson, J.A. (1991) Synthesis, conformational properties, and antibody recognition of peptides containing beta-turn mimetics based on alpha-alkylproline derivatives. J Med Chem, 34, 1777-1789.
	Horwell, D.C., Howson, W., Ratcliffe, G.S. and Willems, H.M. (1996) The design of dipeptide helical mimetics: the synthesis, tachykinin receptor affinity and conformational analysis of 1,1,6-trisubstituted indanes. Bioorg Med Chem, 4, 33-42.
	Hunt, J.T., Ding, C.Z., Batorsky, R., Bednarz, M., Bhide, R., Cho, Y., Chong, S., Chao, S., Gullo-Brown, J., Guo, P., Kim, S.H., Lee, F.Y., Leftheris, K., Miller, A., Mitt, T., Patel, M., Penhallow, B.A., Ricca, C., Rose, W.C., Schmidt, R., Slusarchyk, W.A., Vite, G. and Manne, V. (2000) Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity. J Med Chem, 43, 3587-3595.
	Jacoby, E. (2002) Biphenyls as potential mimetics of protein alpha-helix. Bioorg Med Chem Lett, 12, 891-893.
	James, G.L., Goldstein, J.L., Brown, M.S., Rawson, T.E., Somers, T.C., McDowell, R.S., Crowley, C.W., Lucas, B.K., Levinson, A.D., Marsters, J.C. Jr. (1993) Benzodiazepine peptidomimetics: potent inhibitors of Ras farnesylation in animal cells. Science, 260, 1937-1942.
	Johannesson, P., Lindeberg, G., Tong, W., Gogoll, A., Synnergren, B., Nyberg, F., Karlen, A. and Hallberg, A. (1999) Angiotensin II analogues encompassing 5,9- and 5,10-fused thiazabicycloalkane tripeptide mimetics. J Med Chem, 42, 4524-437.
	Kahn, M. (2000) ß-Sheet mimetics and use thereof as protease inhibitors. US Patent, No. 6 020 331.
	Keenan, R.M., Callahan, J.F., Samanen, J.M., Bondinell, W.E., Calvo, R.R., Chen, L., DeBrosse, C., Eggleston, D.S., Haltiwanger, R.C., Hwang, S.M., Jakas, D.R., Ku, T.W., Miller, W.H., Newlander, K.A., Nichols, A., Parker, M.F., Southhall, L.S., Uzinskas, I., Vasko-Moser, J.A., Venslavsky, J.W., Wong, A.S., Huffman, W.F. (1999) Conformational preferences in a benzodiazepine series of potent nonpeptide fibrinogen receptor antagonists. J Med Chem, 42, 545-559.
	Kemp, D.S. and Stites, W.E. (1988) A convenient preparation of derivatives of 3(s)-amino-10(r)-carboxy-1,6-diaza-cyclodeca-2,7-dione the dilactam of L-small alpha, small y-diaminobutyric acid and d-glutamic acid: A small ß-turn template. Tetrahedron Lett, 29, 5057-5060.
	Kikelj, D. (2003) Peptidomimetic thrombin inhibitors.Pathophysiol Haemost Thromb, 33, 487-491.
	Kishore, R. and Balaram, P. (1985) Stabilization of gamma-turn conformations in peptides by disulfide bridging. Biopolymers, 24, 2041-2043.
	Lauffer, D.J.and Mullican, M.D. (2002) A practical synthesis of (S) 3-tert-butoxycarbonylamino-2-oxo-2,3,4,5-tetrahydro-1,5-benzodiazepine-1-acetic acid methyl ester as a conformationally restricted dipeptido-mimetic for caspase-1 (ICE) inhibitors. Bioorg Med Chem Lett, 12, 1225-1227.
	Lindvall, M.K., Rissanen, K., Hakala, J.M.L. and Koskinen, A.M.P. (1999) Novel y-turn mimetics with a reinforced hydrogen bond.Tetrahedron Lett, 40, 7427-7430.
	Liu, M., Bryant, M.S., Chen, J., Lee, S., Yaremko, B., Lipari, P., Malkowski, M., Ferrari, E., Nielsen, L., Prioli, N., Dell, J., Sinha, D., Syed, J., Korfmacher, W.A., Nomeir, A.A., Lin, C.C., Wang, L., Taveras, A.G., Doll, R.J., Njoroge, F.G., Mallams, A.K., Remiszewski, S., Catino, J.J., Girijavallabhan, V.M., Bishop, W.R., et al. (1998) Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and wap-ras transgenic mice. Cancer Res, 58, 4947-4956.
	Low, C.M. R., Black, J.W., Broughton, H.B., Buck, I.M., Davies, J.M.R., Dunstone, D.J., Hull, R.A.D., Kalindjian, S.B., McDonald, I.M., Pether, M.J., Shankley, N.P.and Steel, K.I.M. (2000) Development of Peptide 3D Structure Mimetics: Rational Design of Novel Peptoid Cholecystokinin Receptor Antagonists. J Med Chem, 43, 3505-3517.
	Lu, T., Tomczuk, B., Bone, R., Murphy, L., Salemme, F.R.and Soll, R.M. (2000) Non-peptidic phenyl-based thrombin inhibitors: exploring structural requirements of the S1 specificity pocket with amidines. Bioorg Med Chem Lett, 10, 83-85 .
	Mitchell, J.B.O. and Smith, J. (2003)D-Amino Acid Residues in Peptides and Proteins.PROTEINS: Structure, Function, and Genetics, 50 , 563-571.
	Ogbu, C.O., Qabar, M.N., Boatman, P.D., Urban, J., Meara, J.P., Ferguson, M.D., Tulinsky, J., Lum, C., Babu, S., Blaskovich, M.A., Nakanishi, H., Ruan, F., Cao, B., Minarik, R., Little, T., Nelson, S., Nguyen, M., Gall, A. and Kahn, M. (1998) Highly efficient and versatile synthesis of libraries of constrained beta-strand mimetics. Bioorg Med Chem Lett, 8, 2321-2326.
	Orner, B.P., Ernst, J.T. and Hamilton, A.D. (2001) Toward proteomimetics: terphenyl derivatives as structural and functional mimics of extended regions of an alpha-helix.J Am Chem Soc, 123, 5382-5383.
	Palucki, B.L., Feighner, S.D., Pong, S., McKee, K.K., Hreniuk, D.L., Tan, C., Howard, A.D., Van der Ploeg, L.H., Patchett, A.A. and Nargund, R.P. (2001) Spiro(indoline-3,4'-piperidine) growth hormone secretagogues as ghrelin mimetics. Bioorg Med Chem Lett, 11, 1955-1957.
	Pan, L.C., Carpino, P.A., Lefker, B.A., Ragan, J.A., Toler, S.M., Pettersen, J.C., Nettleton, D.O., Ng, O., Pirie, C.M., Chidsey-Frink, K., Lu, B., Nickerson, D.F., Tess, D.A., Mullins, M.A., MacLean, D.B., DaSilva-Jardine, P.A. and Thompson, D.D. (2001) Preclinical pharmacology of CP-424,391, an orally active pyrazolinone-piperidine [correction of pyrazolidinone-piperidine] growth hormone secretagogue. Endocrine, 14, 121-132.
	Patchett, A.A., Nargund, R.P., Tata, J.R., Chen, M.H., Barakat, K.J., Johnston, D.B., Cheng, K., Chan, W.W., Butler, B., Hickey, G., et al. (1995) Design and biological activities of L-163,191 (MK-0677): a potent, orally active growth hormone secretagogue. Proc Natl Acad Sci U S A, 92, 7001-7005.
	Plummer, J.S., Berryman, K.A., Cai, C., Cody, W.L., DiMaio, J., Doherty, A.M., Eaton, S., Edmunds, J.J., Holland, D.R., Lafleur, D., Levesque, S., Narasimhan, L.S., Rubin, J.R., Rapundalo, S.T., Siddiqui, M.A., Susser, A., St-Denis, Y. and Winocour, P. (1999) Potent and selective bicyclic lactam inhibitors of thrombin: Part 3: P1' modifications. Bioorg Med Chem Lett, 9, 835-840.
	Rose, W.C., Lee, F.Y., Fairchild, C.R., Lynch, M., Monticello, T., Kramer, R.A. and Manne, V. (2001) Preclinical antitumor activity of BMS-214662, a highly apoptotic and novel farnesyltransferase inhibitor. Cancer Res, 61, 7507-7517 .
	Salimbeni, A., Paleari, F., Canevotti, R., Criscuoli, M., Lippi, A., Angiolini, M., Belvisi, L., Scolastico, C. and Colombo, L. (1997) Design and synthesis of conformationally constrained arginal thrombin inhibitors. Bioorg Med Chem Lett, 7, 2205-2210.
	Sanderson, P.E., Lyle, T.A., Cutrona, K.J., Dyer, D.L., Dorsey, B.D., McDonough, C.M., Naylor-Olsen, A.M., Chen, I.W., Chen, Z., Cook, J.J., Cooper, C.M., Gardell, S.J., Hare, T.R., Krueger, J.A., Lewis, S.D., Lin, J.H., Lucas, B.J. Jr, Lyle, E.A., Lynch, J.J. Jr, Stranieri, M.T., Vastag, K., Yan, Y., Shafer, J.A. and Vacca, J.P. (1998) Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates. J Med Chem, 41, 4466-4474.
	Sato, M., Lee, J.Y., Nakanishi, H., Johnson, M.E., Chrusciel, R.A. and Kahn, M. (1992) Design, synthesis and conformational analysis of gamma-turn peptide mimetics of bradykinin. Biochem Biophys Res Commun, 187, 999-1006.
	Schmidt, B., Lindman, S., Tong, W., Lindeberg, G., Gogoll, A., Lai, Z., Thornwall, M., Synnergren, B., Nilsson, A., Welch, C.J., Sohtell, M., Westerlund, C., Nyberg, F., Karlen, A., Hallberg, A. (1997) Design, synthesis, and biological activities of four angiotensin II receptor ligands with gamma-turn mimetics replacing amino acid residues 3-5. J Med Chem, 40, 903-919.
	Semple, J.E., Rowley, D.C., Owens, T.D., Minami, N.K., Uong, T.H. and Brunck, T.K. (1998) Potent and selective thrombin inhibitors featuring hydrophobic, basic P3-P4-aminoalkyllactam moieties. Bioorg Med Chem Lett, 8, 3525-3530.
	Soll, R.M., Lu, T., Tomczuk, B., Illig, C.R., Fedde, C., Eisennagel, S., Bone, R., Murphy, L., Spurlino, J. and Salemme, F.R. (2000) Amidinohydrazones as guanidine bioisosteres: application to a new class of potent, selective and orally bioavailable, non-amide-based small-molecule thrombin inhibitors. Bioorg Med Chem Lett, 10, 1-4.
	Stachel, S.J., Hu, H., Van, Q.N., Shaka, A.J. and Van Vranken, D.L. (1998) Stabilization of a C7 equatorial gamma turn in DMSO-d6 by a ditryptophan crosslink. Bioorg Med Chem, 6, 1439-1446.
	St-Denis, Y., Augelli-Szafran, C.E., Bachand, B., Berryman, K.A., DiMaio, J., Doherty, A.M., Edmunds, J.J., Leblond, L., Levesque, S., Narasimhan, L.S., Penvose-Yi, J.R., Rubin, J.R., Tarazi, M., Winocour, P.D. and Siddiqui, M.A. (1998) Potent bicyclic lactam inhibitors of thrombin: Part I: P3 modifications. Bioorg Med Chem Lett, 8, 3193-3198.
	Tamura, S.Y., Semple, J.E., Reiner, J.E., Goldman, E.A., Brunck, T.K., Lim-Wilby, M.S., Carpenter, S.H., Rote, W.E. Oldeshulte, G.L., Richard, B.M. et al. (1997) Design and synthesis of a novel class of thrombin inhibitors incorporating heterocyclic dipeptide surrogates. Bioorg Med Chem Lett, 7, 1543-1548.
	Tamura, S.Y., Shamblin, B.M., Brunck, T.K. and Ripka, W.C. (1997) RATIONAL DESIGN, SYNTHESIS, AND SERINE PROTEASE INHIBITORY ACTIVITY OF NOVEL P1-ARGININOYL HETEROCYCLES. Bioorg Med Chem Lett, 7, 1359-1364.
	Tokunaga, T., Hume, W.E., Umezome, T., Okazaki, K., Ueki, Y., Kumagai, K., Hourai, S., Nagamine, J., Seki, H., Taiji, M., Noguchi, H., Nagata, R. (2001) Oxindole derivatives as orally active potent growth hormone secretagogues. J Med Chem, 44, 4641-4649.
	Wagner, J., Kallen, J., Ehrhardt, C., Evenou, J.P. and Wagner, D. (1998) Rational design, synthesis, and X-ray structure of selective noncovalent thrombin inhibitors. J Med Chem, 41, 3664-3674.
	Wang, W., Xiong, C. and Hruby, V.J. (2001) An efficient approach to asymmetric synthesis of dipeptide small ß-turn mimetics: indolizidinone amino acids. Tetrahedron Lett, 42, 3159-3161.
	Weber, I.R., Neidlein, R., von der Saal, W., Grams, F., Leinert, H., Strein, K., Engh, R.A.and Kucznierz, R. (1998) Diarylsulfonamides as selective, non-peptidic thrombin inhibitors. Bioorg Med Chem Lett, 8, 1613-1618.
	Willson, T.M., Henke, B.R., Momtahen, T.M., Myers, P.L., Sugg, E.E., Unwalla, R.J., Croom, D.K., Dougherty, R.W., Grizzle, M.K., Johnson, M.F., Queen, K.L., Rimele, T.J., Yingling, J.D. and James, M.K. (1996) 3-[2-(N-phenylacetamide)]-1,5-benzodiazepines: orally active, binding selective CCK-A agonists. J Med Chem, 39, 3030-3034.
	WO 00/74679
	WO 99/64002
	WO09619483
	WO09705160
	WO09828326
	Yang, L., Berk, S.C., Rohrer, S.P., Mosley, R.T., Guo, L., Underwood, D.J., Arison, B.H., Birzin, E.T., Hayes, E.C., Mitra, S.W., Parmar, R.M., Cheng, K., Wu, T.J., Butler, B.S., Foor, F., Pasternak, A., Pan, Y., Silva, M., Freidinger, R.M., Smith, R.G., Chapman, K., Schaeffer, J.M. and Patchett, A.A. (1998) Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2. Proc Natl Acad Sci U S A, 95, 10836-10841.
	1A46 Thrombin complexed with Hirugen and a ß-strand mimetic inhibitor., Chain: R.
	1A5G Human Thrombin Complexed With Novel Synthetic Peptide Mimetic Inhibitor and Hirugen., Chain: R.
	1A61 Thrombin Complexed With A ß-Mimetic Thiazole-Containing Inhibitor., Chain: R.
	1B5G Human Thrombin Complexed With Novel Synthetic Peptide Mimetic Inhibitor and Hirugen., Chain: R.
	1B6J HIV-1 Protease Complexed With Macrocyclic Peptidomimetic Inhibitor 1., .
	1D5X X-Ray Crystal Structure Of Hla-Dr4 Complexed With Dipeptide Mimetic and Seb., Chain: D.
	1D5Z X-Ray Crystal Structure Of Hla-Dr4 Complexed With Peptidomimetic and Seb., Chain: D.
	1D6E Crystal Structure Of Hla-Dr4 Complex With Peptidomimetic and Seb., Chain: D.
	1FPC Active-Site Mimetic Inhibition Of Thrombin., Chain: R.
	1IIQ Crystal Structure Of HIV-1 Protease Complexed With A Hydroxyethylamine Peptidomimetic Inhibitor., Chain: I.
	1JCR Crystal Structure Of Rat Protein Farnesyltransferase Complexed With The Non-Substrate Tetrapeptide Inhibitor Cvfm and Farnesyl Diphosphate Substrate., .
	1MTR HIV-1 Protease Complexed With A Cyclic Phe-Ile-Val Peptidomimetic Inhibitor., Chain: C.
	1NJT Complex Structure Of Hcmv Protease and A Peptidomimetic Inhibitor., Chain: H.
	1NJU Complex Structure Of Hcmv Protease and A Peptidomimetic Inhibitor., Chain: H.
	1NKM Complex Structure Of Hcmv Protease and A Peptidomimetic Inhibitor., Chain: C.
	1RHU Crystal Structure Of The Complex Of Caspase-3 With A 5,6,7 Tricyclic Peptidomimetic Inhibitor., Chain: A.
	1W3C Crystal Structure Of The Hepatitis C Virus Ns3 Protease In Complex With A Peptidomimetic Inhibitor., Chain: A.
	1W3C Crystal Structure Of The Hepatitis C Virus Ns3 Protease In Complex With A Peptidomimetic Inhibitor., Chain: B.
	2AIG Adamalysin II With Peptidomimetic Inhibitor Pol647., Chain: I.
	3AIG Adamalysin II With Peptidomimetic Inhibitor Pol656., Chain: I.