Spatial screening for the identification of the bioactive conformation of integrin ligands

Topics in Current Chemistry

Volumn 272, Issue , 2007, Pages 1-50

  Weide, Timo ^a   Modlinger, Armin ^a   Kessler, Horst ^a  

^a TECHNICAL UNIVERSITY OF MUNICH   (Germany)

Author keywords

Bioactive conformation; Cyclic peptides; LDT and RGD mimetics; Ligand based drug design; Spatial screening

Indexed keywords

EID: 68249117645     PISSN: 03401022     EISSN: None     Source Type: Book Series    
DOI: 10.1007/128_052     Document Type: Article

References (277)

1. Arkin MR, Wells JA (2004) Nat Rev Drug Discov 3:301
2. Ball LJ, Kühne R, Schneider-Mergener J, Oschkinat H (2005) Angew Chem Int Ed 44:2852
3. Berg T (2003) Angew Chem Int Ed 42:2462
4. Gadek TR, Nicholas JB (2003) Biochem Pharmacol 65:1
5. Toogood PL (2002) J Med Chem 45:1543
6. Lo Conte L, Chothia C, Janin J (1999) J Mol Biol 285:2177
7. Heinz DW, Schubert WD, Höfle G (2005) Angew Chem Int Ed 44:1298
8. Bollag DM, McQueney PA, Zhu J, Hensens O, Koupal L, Liesch J, Goetz M, Lazarides E, Woods CM (1995) Cancer Res 55:2325
9. Hynes RO (2002) Cell 110:673
10. Arndt T, Arndt U, Reuning U, Kessler H (2004) In: Weber GF (ed) Cancer Therapy: Molecular Tumor. Horizon Bioscience, Wymondham, pp 93-141
11. Li RH, Hoess RH, Bennett JS, DeGrado WF (2003) Protein Eng 16:65
12. Dubree NJP, Artis DR, Castanedo G, Marsters J, Sutherlin D, Caris L, Clark K, Keating SM, Beresini MH, Chiu H, Fong S, Lowman HB, Skelton NJ, Jackson DY (2002) J Med Chem 45:3451
13. DuVigneaud V, Denning GS Jr, Drabarek S, Chan WY (1964) J Biol Chem 239:472
14. Rothemund S, Beyermann M, Krause E, Krause G, Bienert M, Hodges RS, Sykes BD, Sonnichsen FD (1995) Biochemistry 34:12 954
15. Kessler H (1982) Angew Chem Int Ed 21:512
16. Hruby VJ (1982) Life Sci 31:189
17. Freidinger RM (2003) J Med Chem 46:5553
18. Kessler H, Kutscher B, Klein A (1986) Liebigs Ann Chem, p 893
19. Kessler H, Gratias R, Hessler G, Gurrath M, Müller G (1996) Pure Appl Chem 68:1201
20. Hruby VJ, Balse PM (2000) Curr Med Chem 7:945
21. Payne JW, Marshall NJ, Grail BM, Gupta S (2002) Curr Org Chem 6:1221
22. Gilon C, Mang C, Lohof E, Friedler A, Kessler H (2003) In: Goodman M, Felix L, Moroder L, Toniolo C (eds) Houben-Weyl: Methods of Organic Chemistry, vol E 22b. Thieme, Stuttgart, p 461
23. Li P, Roller PP (2002) Curr Top Med Chem 2:325
24. Davidson JP, Lubman O, Rose T, Waksman G, Martin SF (2002) J Am Chem Soc 124:205
25. Rose GD, Gierasch LM, Smith JA (1985) Adv Protein Chem 37:1
26. Saudek V, Atkinson RA, Pelton JT (1991) Biochemistry 30:7369
27. Chorev M (2002) Chim Oggi 20:81
28. Giannis A (1993) Angew Chem Int Ed 32:1244
29. Bisang C, Jiang L, Freund E, Emery F, Bauch C, Matile H, Pluschke G, Robinson JA (1998) J Am Chem Soc 120:7439
30. Hölzemann G (1991) Kontakte (Darmstadt), p 55
31. Hölzemann G (1991) Kontakte (Darmstadt), p 3
32. Gante J (1994) Angew Chem Int Ed 33:1699
33. Souers AJ, Ellman JA (2001) Tetrahedron 57:7431
34. Kee KS, Jois SD (2003) Curr Pharm Des 9:1209
35. Cluzeau J, Lubell WD (2005) Biopolymers 80:98
36. Matter H, Kessler H (1995) J Am Chem Soc 117:3347
37. Veber DF, Holly FW, Nutt RF, Bergstrand SJ, Brady SF, Hirschmann R, Glitzer MS, Saperstein R (1979) Nature 280:512
38. Malicka J, Czaplewski C, Groth M, Wiczk W, Oldziej S, Lankiewicz L, Ciarkowski J, Liwo A (2004) Curr Top Med Chem 4:123
39. Rew Y, Malkmus S, Svensson C, Yaksh TL, Chung NN, Schiller PW, Cassel JA, De-Haven RN, Taulane JP, Goodman M (2002) J Med Chem 45:5414
40. Fasan R, Dias RLA, Moehle K, Zerbe O, Vrijbloed JW, Obrecht D, Robinson JA (2004) Angew Chem Int Ed 43:2109
41. Wipf P (1995) Chem Rev 95:2115
42. Pierschbacher MD, Ruoslahti E (1984) Nature 309:30
43. Ruoslahti E, Pierschbacher MD (1987) Science 238:491
44. Aumailley M, Gurrath M, Müller G, Calvete J, Timpl R, Kessler H (1991) FEBS Lett 291:50
45. Haubner R, Finsinger D, Kessler H (1997) Angew Chem Int Ed 36:1375
46. Komoriya A, Green LJ, Mervio MM, Yamada SS, Yamada KM, Humphries MJ (1991) Faseb J 5:A1617
47. Viney JL, Jones S, Chiu HH, Lagrimas B, Renz ME, Presta LG, Jackson D, Hillan KJ, Lew S, Fong S (1996) J Immunol 157:2488
48. Weisshoff H, Frost K, Brandt W, Henklein P, Mugge C, Frommel C (1995) FEBS Lett 372:203
49. Hruby VJ (2002) Nat Rev Drug Discov 1:847
50. Veber DF, Johnson SR, Cheng HY, Smith BR, Ward KW, Kopple KD (2002) J Med Chem 45:2615
51. Laskowski RA, MacArthur MW, Moss DS, Thornton JM (1993) J Appl Crystallogr 26:283
52. Balaram H, Uma K, Balaram P (1990) Int J Peptide Protein Res 35:495
53. Hutchinson EG, Thornton JM (1994) Protein Sci 3:2207
54. Ramirez-Alvarado M, Kortemme T, Blanco FJ, Serrano L (1999) Bioorg Med Chem 7:93
55. Dyson HJ, Wright PE (1991) Annu Rev Biophys Biophys Chem 20:519
56. Yao J, Bruschweiler R, Dyson HJ, Wright PE (1994) J Am Chem Soc 116:12 051
57. Kussie PH, Gorina S, Marechal V, Elenbaas B, Moreau J, Levine AJ, Pavletich NP (1996) Science 274:948
58. Kritzer JA, Hodsdon ME, Schepartz A (2005) J Am Chem Soc 127:4118
59. Scherer G, Kramer ML, Schutkowski M, Reimer U, Fischer G (1998) J Am Chem Soc 120:5568
60. Fischer G (2000) Chem Soc Rev 29:119
61. Schiene-Fischer C, Fischer G (2001) J Am Chem Soc 123:6227
62. Kessler H, Anders U, Schudok M (1990) J Am Chem Soc 112:5908
63. Gierasch LM, Deber CM, Madison V, Niu CH, Blout ER (1981) Biochemistry 20:4730
64. Kofron JL, Kuzmic P, Kishore V, Gemmecker G, Fesik SW, Rich DH (1992) J Am Chem Soc 114:2670
65. Bara YA, Friedrich A, Hehlein W, Kessler H, Kondor P, Molter M, Veith HJ (1978) Chem Ber 111:1029
66. Manjula G, Ramakrishnan C (1979) Int J Peptide Protein Res 13:353
67. Ramakrishnan C, Rao BNN (1980) Int J Peptide Protein Res 15:81
68. Bewley CA, He H, Williams DH, Faulkner DJ (1996) J Am Chem Soc 118:4314
69. Kurz M (1991) Cyclische Modellpeptide als Template für ein konformationell orientiertes Peptiddesign. Dissertation, Technische Universität München
70. Mierke DF, Kurz M, Kessler H (1994) J Am Chem Soc 116:1042
71. Haubner R, Gratias R, Diefenbach B, Goodman SL, Jonczyk A, Kessler H (1996) J Am Chem Soc 118:7461
72. Rodriguez AM, Baldoni HA, Suvire F, Vazquez RN, Zamarbide G, Enriz RD, Farkas O, Perczel A, McAllister MA, Torday LL, Papp JG, Csizmadia IG (1998) J Mol Struct Theochem 455:275
73. Weisshoff H, Prasang C, Henklein P, Frommel C, Zschunke A, Mügge C (1999) Eur J Biochem 259:776
74. Nikiforovich GV, Kover KE, Zhang WJ, Marshall GR (2000) J Am Chem Soc 122:3262
75. Schwyzer R, Ludescher U (1969) Helv Chim Acta 52:2033
76. Gurrath M, Müller G, Kessler H, Aumailley M, Timpl R (1992) Eur J Biochem 210:911
77. Pfaff M, Tangemann K, Müller B, Gurrath M, Müller G, Kessler H, Timpl R, Engel J (1994) J Biol Chem 269:20 233
78. Kessler H, Kutscher B, Kerssebaum R, Klein A, Lautz J, Obermeier R, Muellner H, Van Gunsteren WF, Boelens R, Kaptein R (1985) In: Peptides: Structure and Function, Proc 9th Am Pept Symp, p83
79. Kessler H, Kutscher B (1985) Tetrahedron Lett 26:177
80. Fujii N, Oishi S, Hiramatsu K, Araki T, Ueda S, Tamamura H, Otaka A, Kusano S, Terakubo S, Nakashima H, Broach JA, Trent JO, Wang ZX, Peiper SC (2003) Angew Chem Int Ed 42:3251
81. Tamamura H, Mizumoto M, Hiramatsu K, Kusano S, Terakubo S, Yamamoto N, Trent JO, Wang ZX, Peiper SC, Nakashima H, Otaka A, Fujii N (2004) Org Biomol Chem 2:1255
82. Fukami T, Nagase T, Fujita K, Hayama T, Niiyama K, Mase T, Nakajima S, Fukuroda T, Saeki T, Nishikibe M, Ihara M, Yano M, Ishikawa K (1995) J Med Chem 38:4309
83. Spatola AF, Crozet Y, DeWit D, Yanagisawa M (1996) J Med Chem 39:3842
84. Gao XM, Ye YH, Bernd M, Kutscher B (2002) J Peptide Sci 8:418
85. Thurieau C, Feletou M, Hennig P, Raimbaud E, Canet E, Fauchere JL (1996) J Med Chem 39:2095
86. Monteagudo ES, Calvani F, Catrambone F, Fincham CI, Madami A, Meini S, Terracciano R (2001) J Peptide Sci 7:270
87. Etzkorn FA, Guo T, Lipton MA, Goldberg SD, Bartlett PA (1994) J Am Chem Soc 116:10 412
88. Boer J, Gottschling D, Schuster A, Semmrich M, Holzmann B, Kessler H (2001) J Med Chem 44:2586
89. Elbe JA, Kühn K (1997) Integrin-Ligand Interaction. Springer, Heidelberg
90. Plow EF, Haas TK, Zhang L, Loftus J, Smith JW (2000) J Biol Chem 275:21785
91. Arnaout MA, Goodman SL, Xiong JP (2002) Curr Opin Cell Biol 14:641
92. Shimaoka M, Springer TA (2003) Nat Rev Drug Discov 2:703
93. Albelda SM, Buck CA (1990) Faseb J 4:2868
94. Hynes RO, Lander AD (1992) Cell 68:303
95. Collins TL, Kassner PD, Bierer BE, Burakoff SJ (1994) Curr Opin Immunol 6:385
96. Humphries MJ (2000) Biochem Soc Trans 28:311
97. Adler M, Lazarus RA, Dennis MS, Wagner G (1991) Science 253:445
98. Ruoslahti E, Pierschbacher MD (1986) Cell 44:517
99. D'Souza SE, Ginsberg MH, Plow EF (1991) Trends Biochem Sci 16:246
100. Calvete JJ, Schafer W, Soszka T, Lu WQ, Cook JJ, Jameson BA, Niewiarowski S (1991) Biochemistry 30:5225
101. Smith KJ, Jaseja M, Lu XJ, Williams JA, Hyde EI, Trayer IP (1996) Int J Peptide Protein Res 48:220
102. Scarborough RM, Gretler DD (2000) J Med Chem 43:3453
103. Strömblad S, Cheresh DA (1996) Chem Biol 3:881
104. Strömblad S, Cheresh DA (1996) Trends Cell Biol 6:462
105. Schaffner P, Dard MM (2003) Cell Mol Life Sci 60:119
106. Müller G, Gurrath M, Kessler H (1994) J Comput Aided Mol Des 8:709
107. Calvete JJ, Moreno-Murciano MP, Theakston RDG, Kisiel DG, Marcinkiewicz C (2003) Biochem J 372:725
108. Dechantsreiter MA, Planker E, Mathä B, Lohof E, Hölzemann G, Jonczyk A, Goodman SL, Kessler H (1999) J Med Chem 42:3033
109. Xiong JP, Stehle T, Zhang RG, Joachimiak A, Frech M, Goodman SL, Arnaout MA (2002) Science 296:151
110. Xiong JP, Stehle T, Diefenbach B, Zhang RG, Dunker R, Scott DL, Joachimiak A, Goodman SL, Arnaout MA (2001) Science 294:339
111. Xiao T, Takagi J, Coller BS, Wang JH, Springer TA (2004) Nature 432:59
112. Marinelli L, Lavecchia A, Gottschalk KE, Novellino E, Kessler H (2003) J Med Chem 46:4393
113. Gottschalk KE, Kessler H (2002) Angew Chem Int Ed 41:3767
114. Gottschalk KE, Günther R, Kessler H (2002) Chem Bio Chem 3:470
115. Cheng S, Craig WS, Mullen D, Tschopp JF, Dixon D, Pierschbacher MD (1994) J Med Chem 37:1
116. Craig WS, Cheng S, Mullen DG, Blevitt J, Pierschbacher MD (1995) Biopolymers 37:157
117. Scarborough RM, Kleiman NS, Phillips DR (1999) Circulation 100:437
118. Heller M, Mierke DF, Reif B, Kessler H (2006) J Am Chem Soc, in press
119. Lohof E, Planker E, Mang C, Burkhart F, Dechantsreiter MA, Haubner R, Wester HJ, Schwaiger M, Hölzemann G, Goodman SL, Kessler H (2000) Angew Chem Int Ed 39:2761
120. Bean JW, Kopple KD, Peishoff CE (1992) J Am Chem Soc 114:5328
121. Peishoff CE, Ali FE, Bean JW, Calvo R, Dambrosio CA, Eggleston DS, Hwang SM, Kline TP, Koster PF, Nichols A, Powers D, Romoff T, Samanen JM, Stadel J, Vasko JA, Kopple KD (1992) J Med Chem 35:3962
122. Goodman SL, Hölzemann G, Sulyok GAG, Kessler H (2002) J Med Chem 45:1045
123. Seebach D, Kimmerlin T, Sebesta R, Campo MA, Beck AK (2004) Tetrahedron 60:7455
124. Seebach D, Beck AK, Bierbaum DJ (2004) Chem Biodiversity 1:1111
125. Pierschbacher MD, Ruoslahti E (1987) J Biol Chem 262:17 294
126. Schumann F, Müller A, Koksch M, Müller G, Sewald N (2000) J Am Chem Soc 122:12 009
127. Zimmermann D, Guthohrlein EW, Malesevic M, Sewald K, Wobbe L, Heggemann C, Sewald N (2005) Chem Bio Chem 6:272
128. Ron D, Gilon C, Hanani M, Vromen A, Selinger Z, Chorev M (1992) J Med Chem 35:2806
129. Bach AC, Eyermann CJ, Gross JD, Bower MJ, Harlow RL, Weber PC, Degrado WF (1994) J Am Chem Soc 116:3207
130. Bach AC, Espina JR, Jackson SA, Stouten PFW, Duke JL, Mousa SA, DeGrado WF (1996) J Am Chem Soc 118:293
131. Tyndall JDA, Nall T, Fairlie DP (2005) Chem Rev 105:973
132. Chorev M, Goodman M (1993) Acc Chem Res 26:266
133. Freidinger RM, Veber DF (1979) J Am Chem Soc 101:6129
134. Wermuth J, Goodman SL, Jonczyk A, Kessler H (1997) J Am Chem Soc 119:1328
135. Geyer A, Müller G, Kessler H (1994) J Am Chem Soc 116:7735
136. Suguna K, Padlan EA, Smith CW, Carlson WD, Davies DR (1987) Proc Natl Acad Sci 84:7009
137. Miller M, Schneider J, Sathyanarayana BK, Toth MV, Marshall GR, Clawson L, Selk L, Kent SBH, Wlodawer A (1989) Science 246:1149
138. Ma SG, Spatola AF (1993) Int J Peptide Protein Res 41:204
139. Haubner R, Schmitt W, Hölzemann G, Goodman SL, Jonczyk A, Kessler H (1996) J Am Chem Soc 118:7881
140. Finsinger D (1997) Peptidische und peptidanaloge Antagonisten des alpha Vbeta 3-integrins. Dissertation, Technische Universität München
141. Davies DE, Doyle PM, Farrant RD, Hill RD, Hitchcock PB, Sanderson PN, Young DW (2003) Tetrahedron Lett 44:8887
142. Belvisi L, Bernardi A, Checchia A, Manzoni L, Potenza D, Scolastico C, Castorina M, Cupelli A, Giannini G, Carminati P, Pisano C (2001) Org Lett 3:1001
143. Hirschmann R, Nicolaou KC, Pietranico S, Leahy EM, Salvino J, Arison B, Cichy MA, Spoors PG, Shakespeare WC, Sprengeler PA, Hamley P, Smith AB, Reisine T, Raynor K, Maechler L, Donaldson C, Vale W, Freidinger RM, Cascieri MR, Strader CD (1993) J Am Chem Soc 115:12 550
144. von Roedern E, Kessler H (1994) Angew Chem Int Ed 33:687
145. von Roedern E, Lohof E, Hessler G, Hoffmann M, Kessler H (1996) J Am Chem Soc 118:10 156
146. Gruner SAW, Locardi E, Lohof E, Kessler H (2002) Chem Rev 102:491
147. Scarborough RM, Rose JW, Hsu MA, Phillips DR, Fried VA, Campbell AM, Nannizzi L, Charo IF (1991) J Biol Chem 266:9359
148. Scarborough RM, Naughton MA, Teng W, Rose JW, Phillips DR, Nannizzi L, Arfsten A, Campbell AM, Charo IF (1993) J Biol Chem 268:1066
149. Fisher MJ, Gunn B, Harms CS, Kline AD, Mullaney JT, Nunes A, Scarborough RM, Arfsten AE, Skelton MA, Um SL, Utterback BG, Jakubowski JA (1997) J Med Chem 40:2085
150. Samanen J, Ali F, Romoff T, Calvo R, Sorenson E, Vasko J, Storer B, Berry D, Bennett D, Strohsacker M, Powers D, Stadel J, Nichols A (1991) J Med Chem 34:3114
151. Kopple KD, Baures PW, Bean JW, Dambrosio CA, Hughes JL, Peishoff CE, Eggleston DS (1992) J Am Chem Soc 114:9615
152. Ali FE, Bennett DB, Calvo RR, Elliott JD, Hwang SM, Ku TW, Lago MA, Nichols AJ, Romoff TT, Shah DH, Vasko JA, Wong AS, Yellin TO, Yuan CK, Samanen JM (1994) J Med Chem 37:769
153. Xue CB, DeGrado WF (1995) J Org Chem 60:946
154. Jackson S, DeGrado W, Dwivedi A, Parthasarathy A, Higley A, Krywko J, Rockwell A, Markwalder J, Wells G, Wexler R, Mousa S, Harlow R (1994) J Am Chem Soc 116:3220
155. Müller G (1996) Angew Chem Int Ed 35:2767
156. Greenspoon N, Hershkoviz R, Alon R, Varon D, Shenkman B, Marx G, Federman S, Kapustina G, Lider O (1993) Biochemistry 32:1001
157. Corbett JW, Graciani NR, Mousa SA, DeGrado WF (1997) Bioorg Med Chem Lett 7:1371
158. Xue CB, Wityak J, Sielecki TM, Pinto DJ, Batt DG, Cain GA, Sworin M, Rockwell AL, Roderick JJ, Wang SG, Orwat MJ, Frietze WE, Bostrom LL, Liu J, Higley CA, Rankin FW, Tobin AE, Emmett G, Lalka GK, Sze JY, DiMeo SV, Mousa SA, Thoolen MJ, Racanelli AL, Hausner EA, Reilly TM, DeGrado WF, Wexler RR, Olson RE (1997) J Med Chem 40:2064
159. Blackburn BK, Lee A, Baier M, Kohl B, Olivero AG, Matamoros R, Robarge KD, McDowell RS (1997) J Med Chem 40:717
160. Rockwell AL, Rafalski M, Pitts WJ, Batt DG, Petraitis JJ, DeGrado WF, Mousa S, Jadhav PK (1999) Bioorg Med Chem Lett 9:937
161. Olson RE, Sielecki TM, Wityak J, Pinto DJ, Batt DG, Frietze WE, Liu J, Tobin AE, Orwat MJ, Di Meo SV, Houghton GC, Lalka GK, Mousa SA, Racanelli AL, Hausner EA, Kapil RP, Rabel HR, Thoolen MJ, Reilly TM, Anderson PS, Wexler RR (1999) J Med Chem 42:1178
162. Batt DG, Petraitis JJ, Houghton GC, Modi DP, Cain GA, Corjay MH, Mousa SA, Bouchard PJ, Forsythe MS, Harlow PP, Barbera FA, Spitz SM, Wexler RR, Jadhav PK (2000) J Med Chem 43:41
163. Pitts WJ, Wityak J, Smallheer JM, Tobin AE, Jetter JW, Buynitsky JS, Harlow PP, Solomon KA, Corjay MH, Mousa SA, Wexler RR, Jadhav PK (2000) J Med Chem 43:27
164. Gibson C, Sulyok GAG, Hahn D, Goodman SL, Hölzemann G, Kessler H (2001) Angew Chem Int Ed 40:165
165. Duggan ME, Hutchinson JH (2000) Expert Opin Ther Pat 10:1367
166. Biltresse S, Attolini M, Dive G, Cordi A, Tucker GC, Marchand-Brynaert J (2004) Bioorg Med Chem 12:5379
167. Keenan RM, Miller WH, Lago MA, Ali FE, Bondinell WE, Callahan JF, Calvo RR, Cousins RD, Hwang SM, Jakas DR, Ku TW, Kwon C, Nguyen TT, Reader VA, Rieman DJ, Ross ST, Takata DT, Uzinskas IN, Yuan CCK, Smith BR (1998) Bioorg Med Chem Lett 8:3165
168. Keenan RM, Lago MA, Miller WH, Ali FE, Cousins RD, Hall LB, Hwang SM, Jakas DR, Kwon C, Louden C, Nguyen TT, Ohlstein EH, Rieman DJ, Ross ST, Samanen JM, Smith BR, Stadel J, Takata DT, Vickery L, Yuan CCK, Yue TL (1998) Bioorg Med Chem Lett 8:3171
169. Keenan RM, Miller WH, Barton LS, Bondinell WE, Cousins RD, Eppley DF, Hwang SM, Kwon C, Lago MA, Nguyen TT, Smith BR, Uzinskas IN, Yuan CCK (1999) Bioorg Med Chem Lett 9:1801
170. Miller WH, Bondinell WE, Cousins RD, Erhard KF, Jakas DR, Keenan RM, Ku TW, Newlander KA, Ross ST, Haltiwanger RC, Bradbeer J, Drake FH, Gowen M, Hoffman SJ, Hwang SM, James IE, Lark MW, Lechowska B, Rieman DJ, Stroup GB, Vasko-Moser JA, Zembryki DL, Azzarano LM, Adams PC, Salyers KL, Smith BR, Ward KW, Johanson KO, Huffman WF (1999) Bioorg Med Chem Lett 9:1807
171. Miller WH, Alberts DP, Bhatnagar PK, Bondinell WE, Callahan JF, Calvo RR, Cousins RD, Erhard KF, Heerding DA, Keenan RM, Kwon C, Manley PJ, Newlander KA, Ross ST, Samanen JM, Uzinskas IN, Venslavsky JW, Yuan CCK, Haltiwanger RC, Gowen M, Hwang SM, James IE, Lark MW, Rieman DJ, Stroup GB, Azzarano LM, Salyers KL, Smith BR, Ward KW, Johanson KO, Huffman WF (2000) J Med Chem 43:22
172. Sulyok GAG, Gibson C, Goodman SL, Hölzemann G, Wiesner M, Kessler H (2001) J Med Chem 44:1938
173. Miller WH, Manley PJ, Cousins RD, Erhard KF, Heerding DA, Kwon C, Ross ST, Samanen JM, Takata DT, Uzinskas IN, Yuan CCK, Haltiwanger RC, Gress CJ, Lark MW, Hwang SM, James IE, Rieman DJ, Willette RN, Yue TL, Azzarano LM, Salyers KL, Smith BR, Ward KW, Johanson KO, Huffman WF (2003) Bioorg Med Chem Lett 13:1483
174. Scarborough RM (1999) Curr Med Chem 6:971
175. Yasuda N, Hsiao Y, Jensen MS, Rivera NR, Yang CH, Wells KM, Yau J, Palucki M, Tan LS, Dormer PG, Volante RP, Hughes DL, Reider PJ (2004) J Org Chem 69:1959
176. Wityak J, Sielecki TM, Pinto DJ, Emmett G, Sze JY, Liu J, Tobin AE, Wang SG, Jiang B, Ma P, Mousa SA, Olson RE, Wexler RR (1997) J Med Chem 40:1292
177. Ku TW, Ali FE, Barton LS, Bean JW, Bondinell WE, Burgess JL, Callahan JF, Calvo RR, Chen LC, Eggleston DS, Gleason JG, Huffman WF, Hwang SM, Jakas DR, Karash CB, Keenan RM, Kopple KD, Miller WH, Newlander KA, Nichols A, Parker MF, Peishoff CE, Samanen JM, Uzinskas I, Venslavsky JW (1993) J Am Chem Soc 115:8861
178. Ku TW, Miller WH, Bondinell WE, Erhard KF, Keenan RM, Nichols AJ, Peishoff CE, Samanen JM, Wong AS, Huffman WF (1995) J Med Chem 38:9
179. Samanen JM, Ali FE, Barton LS, Bondinell WE, Burgess JL, Callahan JF, Calvo RR, Chen WT, Chen LC, Erhard K, Feuerstein G, Heys R, Hwang SM, Jakas DR, Keenan RM, Ku TW, Kwon C, Lee CP, Miller WH, Newlander KA, Nichols A, Parker M, Peishoff CE, Rhodes G, Ross S, Shu A, Simpson R, Takata D, Yellin TO, Uzsinskas I, Venslavsky JW, Yuan CK, Huffman WF (1996) J Med Chem 39:4867
180. Davis HM, Hwang SM, Freed MI (1997) Blood 90:1322
181. Wong A, Hwang SM, Johanson K, Samanen J, Bennett D, Landvatter SW, Chen WT, Heys JR, Ali FE, Ku TW, Bondinell W, Nichols AJ, Powers DA, Stadel JM (1998) J Pharmacol Exp Ther 285:228
182. Okumura K, Shimazaki T, Aoki Y, Yamashita H, Tanaka E, Banba S, Yazawa K, Kibayashi K, Banno H (1998) J Med Chem 41:4036
183. Fisher MJ, Arfstan AE, Giese U, Gunn BP, Harms CS, Khau V, Kinnick MD, Lindstrom TD, Martinelli MJ, Mest HJ, Mohr M, Morin JM, Mullaney JT, Nunes A, Paal M, Rapp A, Ruhter G, Ruterbories KJ, Sall DJ, Scarborough RM, Schotten T, Sommer B, Stenzel W, Towner RD, Um SL, Utterback BG, Vasileff RT, Voelkers S, Wyss VL, Jakubowski JA (1999) J Med Chem 42:4875
184. Fisher MJ, Giese U, Harms CS, Kinnick MD, Lindstrom TD, McCowan JR, Mest HJ, Morin JM, Mullaney JT, Paal M, Rapp A, Ruhter G, Ruterbories KJ, Sall DJ, Scarborough RM, Schotten T, Stenzel W, Towner RD, Um SL, Utterback BG, Wyss VL, Jakubowski JA (2000) Bioorg Med Chem Lett 10:385
185. Miller WH, Keenan RM, Willette RN, Lark MW (2000) Drug Discov Today 5:397
186. Duggan ME, Duong LT, Fisher JE, Hamill TG, Hoffman WF, Huff JR, Ihle NC, Leu CT, Nagy RM, Perkins JJ, Rodan SB, Wesolowski G, Whitman DB, Zartman AE, Rodan GA, Hartman GD (2000) J Med Chem 43:3736
187. Kling A, Backfisch G, Delzer J, Geneste H, Graef C, Hornberger W, Lange UEW, Lauterbach A, Seitz W, Subkowski T (2003) Bioorg Med Chem 11:1319
188. Keenan RM, Miller WH, Kwon C, Ali FE, Callahan JF, Calvo RR, Hwang SM, Kopple KD, Peishoff CE, Samanen JM, Wong AS, Yuan CK, Huffman WF (1997) J Med Chem 40:2289
189. Marinelli L, Gottschalk K-E, Meyer A, Novellino E, Kessler H (2004) J Med Chem 47:4166
190. Marinelli L, Meyer A, Heckmann D, Lavecchia A, Novellino E, Kessler H (2005) J Med Chem 48:4204
191. Gottschalk K-E, Kessler H (2004) FEBS Lett 557:253
192. Li R, Mitra N, Gratkowski H, Vilaire G, Litvinov R, Nagasami C, Weisel JW, Lear JD, DeGrado WF, Bennett JS (2003) Science 300:795
193. Gottschalk KE, Adams PD, Brunger AT, Kessler H (2002) Protein Sci 11:1800
194. Schneider D, Engelman DM (2004) J Biol Chem 279:9840
195. Wester HJ, Kessler H (2005) J Nucl Med 46:1940
196. Tilley JW, Sidduri A (2001) Drug Future 26:985
197. Tilley JW (2002) Expert Opin Ther Pat 12:991
198. Hemler ME (1990) Annu Rev Immunol 8:365
199. Postigo AA, Sanchezmateos P, Lazarovits AI, Sanchezmadrid F, Delandazuri MO (1993) J Immunol 151:2471
200. Berlin C, Berg EL, Briskin MJ, Andrew DP, Kilshaw PJ, Holzmann B, Weissman IL, Hamann A, Butcher EC (1993) Cell 74:185
201. Kilger G, Holzmann B (1995) J Mol Med 73:347
202. Yusuf-Makagiansar H, Anderson ME, Yakovleva TV, Murray JS, Siahaan TJ (2002) Med Res Rev 22:146
203. von Andrian UH, Engelhardt B (2003) New Engl J Med 348:68
204. Holzmann B, McIntyre BW, Weissman IL (1989) Cell 56:37
205. Picarella D, Hurlbut P, Rottman J, Shi XJ, Butcher E, Ringler DJ (1997) J Immunol 158:2099
206. Elices MJ (2003) Curr Opin Invest Drugs 4:1354
207. Noseworthy JH, Kirkpatrick P (2005) Nat Rev Drug Discov 4:101
208. Steinman L (2005) Nat Rev Drug Discov 4:510
209. Renz ME, Chin HH, Jones S, Fox J, Kim KJ, Presta LG, Fong S (1994) J Cell Biol 125:1395
210. Jones EY, Harlos K, Bottomley MJ, Robinson RC, Driscoll PC, Edwards RM, Clements JM, Dudgeon TJ, Stuart DI (1995) Nature 373:539
211. Shroff HN, Schwender CF, Dottavio D, Yang LL, Briskin MJ (1996) Bioorg Med Chem Lett 6:2495
212. Newham P, Craig SE, Seddon GN, Schofield NR, Rees A, Edwards RM, Jones EY, Humphries MJ (1997) J Biol Chem 272:19 429
213. Dando J, Wilkinson KW, Ortlepp S, King DJ, Brady RL (2002) Acta Crystallogr D 58:233
214. Tan K, Casasnovas JM, Liu JH, Briskin MJ, Springer TA, Wang JH (1998) Structure 6:793
215. Singh J, Adams S, Carter MB, Cuervo H, Lee WC, Lobb RR, Pepinsky RB, Petter R, Scott D (2004) Curr Top Med Chem 4:1497
216. Singh J, van Vlijmen H, Liao YS, Lee WC, Cornebise M, Harris M, Shu IH, Gill A, Cuervo JH, Abraham WM, Adams SP (2002) J Med Chem 45:2988
217. Jackson DY (2002) Curr Pharm Des 8:1229
218. Yang GX, Hagmann WK (2003) Med Res Rev 23:369
219. Tilley JW, Chen L, Sidduri A, Fotouhi N (2004) Curr Top Med Chem 4:1509
220. Hagmann WK (2004) Curr Top Med Chem 4:1461
221. Huryn DM, Konradi AW, Ashwell S, Freedman SB, Lombardo LJ, Pleiss MA, Thorsett ED, Yednock T, Kennedy JD (2004) Curr Top Med Chem 4:1473
222. Gottschling D, Boer J, Marinelli L, Voll G, Haupt M, Schuster A, Holzmann B, Kessler H (2002) Chem Bio Chem 3:575
223. Shroff HN, Schwender CF, Baxter AD, Brookfield F, Payne LJ, Cochran NA, Gallant DL, Briskin MJ (1998) Bioorg Med Chem Lett 8:1601
224. Rockwell A, Melden M, Copeland RA, Hardman K, Decicco CP, DeGrado WF (1996) J Am Chem Soc 118:10 337
225. Gottschling D, Boer E, Schuster A, Holzmann B, Kessler H (2001) Bioorg Med Chem Lett 11:2997
226. Gottschling D, Boer J, Schuster A, Holzmann B, Kessler H (2002) Angew Chem Int Ed 41:3007
227. Belanger PC, Dufresne C (1986) Can J Chem 64:1514
228. Farmer PS (1980) Drug Design. Academic, New York
229. Papageorgiou C, Haltiner R, Bruns C, Petcher TJ (1992) Bioorg Med Chem Lett 2:135
230. Hirschmann R, Sprengeler PA, Kawasaki T, Leahy JW, Shakespeare WC, Smith AB (1993) Tetrahedron 49:3665
231. Olson GL, Bolin DR, Bonner MP, Bos M, Cook CM, Fry DC, Graves BJ, Hatada M, Hill DE, Kahn M, Madison VS, Rusiecki VK, Sarabu R, Sepinwall J, Vincent GP, Voss ME (1993) J Med Chem 36:3039
232. Hirschmann R, Hynes J, Cichy-Knight MA, van Rijn RD, Sprengeler PA, Spoors PG, Shakespeare WC, Pietranico-Cole S, Barbosa J, Liu J, Yao WQ, Rohrer S, Smith AB (1998) J Med Chem 41:1382
233. Le GT, Abbenante G, Becker B, Grathwohl M, Halliday J, Tometzki G, Zuegg J, Meutermans W (2003) Drug Discov Today 8:701
234. Boer J, Gottschling D, Schuster A, Holzmann B, Kessler H (2001) Angew Chem Int Ed 40:3870
235. Chen L, Tilley JW, Huang TN, Miklowski D, Trilles R, Guthrie RW, Luk K, Hanglow A, Rowan K, Schwinge V, Wolitzky B (2000) Bioorg Med Chem Lett 10:725
236. Chen L, Tilley JW, Guthrie RW, Mennona F, Huang TN, Kaplan G, Trilles R, Miklowski D, Huby N, Schwinge V, Wolitzky B, Rowan K (2000) Bioorg Med Chem Lett 10:729
237. Harriman GCB, Schwender CF, Gallant D, Cochran NA, Briskin MJ (2000) Bioorg Med Chem Lett 10:1497
238. Hagmann WK, Durette PL, Lanza T, Kevin NJ, de Laszlo SE, Kopka HE, Young D, Magriotis PA, Li B, Lin LS, Yang G, Kamenecka T, Chang LL, Wilson J, MacCoss M, Mills SG, Van Riper G, McCauley E, Egger LA, Kidambi U, Lyons K, Vincent S, Stearns R, Colletti A, Teffera J, Tong S, Fenyk-Melody J, Owens K, Levorse D, Kim P, Schmidt JA, Mumford RA (2001) Bioorg Med Chem Lett 11:2709
239. Tilley JW, Kaplan G, Rowan K, Schwinge V, Wolitzky B (2001) Bioorg Med Chem Lett 11:1
240. Locardi E, Boer J, Modlinger A, Schuster A, Holzmann B, Kessler H (2003) J Med Chem 46:5752
241. Yun Z, Menter DG, Nicolson GL (1996) Cancer Res 56:3103
242. Chorev M, Dresnerpollak R, Eshel Y, Rosenblatt M (1995) Biopolymers 37:367
243. Engleman VW, Nickols GA, Ross FP, Horton MA, Griggs DW, Settle SL, Ruminski PG, Teitelbaum SL (1997) J Clin Invest 99:2284
244. Friedlander M, Theesfeld CL, Sugita M, Fruttiger M, Thomas MA, Chang S, Cheresh DA (1996) Proc Natl Acad Sci USA 93:9764
245. Matsuno H, Stassen JM, Vermylen J, Deckmyn H (1994) Circulation 90:2203
246. Choi ET, Engel L, Callow AD, Sun S, Trachtenberg J, Santoro S, Ryan US (1994) J Vasc Surg 19:125
247. Noiri E, Gailit J, Sheth D, Magazine H, Gurrath M, Muller G, Kessler H, Goligorsky MS (1994) Kidney Int 46:1050
248. Romanov V, Noiri E, Czerwinski G, Finsinger D, Kessler H, Goligorsky MS (1997) Kidney Int 52:93
249. Goligorsky MS, Noiri E, Kessler H, Romanov V (1997) Kidney Int 51:1487
250. Brooks PC, Montgomery AMP, Rosenfeld M, Reisfeld RA, Hu TH, Klier G, Cheresh DA (1994) Cell 79:1157
251. Eskens F, Dumez H, Verweij J, Brindley C, Perschl A, Kovar A, Wynendaele W, van Oosterom A (2000) Clin Cancer Res 6:4524s
252. Auernheimer J, Zukowski D, Dahmen C, Kantlehner M, Enderle A, Goodman SL, Kessler H (2005) Chem Bio Chem 6:2034
253. Elmengaard B, Bechtold JE, Søballe K (2005) Biomaterials 26:3521
254. Schliephake H, Scharnweber D, Dard M, Rossler S, Sewing A, Meyer J, Hoogestraat D (2002) Clin Oral Implants Res 13:312
255. Hersel U, Dahmen C, Kessler H (2003) Biomaterials 24:4385
256. Kantlehner M, Schaffner P, Finsinger D, Meyer J, Jonczyk A, Diefenbach B, Nies B, Hölzemann G, Goodman SL, Kessler H (2000) Chem Bio Chem 1:107
257. Kantlehner M, Finsinger D, Meyer J, Schaffner P, Jonczyk A, Diefenbach B, Nies B, Kessler H (1999) Angew Chem Int Ed 38:560
258. Dahmen C, Auernheimer J, Meyer A, Enderle A, Goodman SL, Kessler H (2004) Angew Chem Int Ed 43:6649
259. Haubner R, Wester HJ, Reuning U, Senekowitsch-Schmidtke R, Diefenbach B, Kessler H, Stöcklin G, Schwaiger M (1999) J Nucl Med 40:1061
260. Haubner R, Wester HR (2004) Curr Pharm Des 10:1439
261. Gottschalk K-E, Kessler H (2004) Structure 12:1109
262. Li R, Gorelik R, Nanda V, Law PB, Lear JD, DeGrado WF, Bennett JS (2004) J Biol Chem 279:26 666
263. Haubner R, Wester HJ, Burkhart F, Senekowitsch-Schmidtke R, Weber W, Goodman SL, Kessler H, Schwaiger M (2001) J Nucl Med 42:326
264. Haubner R, Wester HJ, Weber WA, Mang C, Ziegler SI, Goodman SL, Senekowitsch-Schmidtke R, Kessler H, Schwaiger M (2001) Cancer Res 61:1781
265. Thumshirn G, Hersel U, Goodman SL, Kessler H (2003) Chem Eur J 9:2717
266. Poethko T, Schottelius M, Thumshim G, Hersel U, Herz M, Henriksen G, Kessler H, Schwaiger M, Wester HJ (2004) J Nucl Med 45:892
267. Chen X, Tohme M, Park R, Hou Y, Bading JR, Conti PS (2004) Mol Imaging 3:96
268. Chen X, Sievers E, Hou Y, Park R, Tohme M, Bart R, Bremner R, Bading JR, Conti PS (2005) Neoplasia 7:271
269. Line BR, Mitra A, Nan A, Ghandehari H (2005) J Nucl Med 46:1552
270. Nasongkla N, Shuai X, Ai H, Weinberg BD, Pink J, Boothman DA, Gao JM (2004) Angew Chem Int Ed 43:6323
271. Burkhart DJ, Kalet BT, Coleman MP, Post GC, Koch TH (2004) Mol Cancer Ther 3:1593
272. Chen X, Plasencia C, Hou Y, Neamati N (2005) J Med Chem 48:5874
273. Schiffelers RM, Ansari A, Xu J, Zhou Q, Tang Q, Storm G, Molema G, Lu PY, Scaria PV, Woodle MC (2004) Nucleic Acids Res 32:e149
274. Raddatz P (1995) Expert Opin Ther Pat 5:1163
275. Ojima I, Chakravarty S, Dong Q (1995) Bioorg Med Chem 3:337
276. Wityak J, Sielecki TM (1996) Expert Opin Ther Pat 6:1175
277. Coller BS (1997) J Clin Invest 99:1467