A Tribute to Ronald T. Borchardt - Teacher, Mentor, Scientist, Colleague, Leader, Friend, and Family Man

Journal of Pharmaceutical Sciences

Volumn 105, Issue 2, 2016, Pages 370-385

  Schowen, Katharine Barbara ^a   Schowen, Richard L ^a   Borchardt, Susan E ^b   Borchardt, Paul M ^b   Artursson, Per ^c   Audus, Kenneth L ^d   Augustijns, Patrick ^e   Nicolazzo, Joseph A ^f   Raub, Thomas J ^g   Schöneich, Christian ^a   Siahaan, Teruna J ^a   Takakura, Yoshi ^h   Thakker, Dhiren R ⁱ   Wolfe, Michael S ^j  

^a UNIVERSITY OF KANSAS   (United States)

^b Uppsala University ^*  (United States)

^c UPPSALA UNIVERSITY   (Sweden)

^d UNIVERSITY OF KANSAS   (United States)

^e DEPARTMENT OF PHARMACEUTICAL AND PHARMACOLOGICAL SCIENCES   (Belgium)

^f MONASH UNIVERSITY   (Australia)

^g ELI LILLY AND COMPANY   (United States)

^h KYOTO UNIVERSITY   (Japan)

ⁱ UNC Hamner Institute for Drug Safety Sciences   (United States)

^j BRIGHAM AND WOMEN S HOSPITAL   (United States)

more..

Author keywords

[No Author keywords available]

Indexed keywords

ACADEMIC ACHIEVEMENT; ARTICLE; CAREER; PHARMACIST; PHARMACY; POSTGRADUATE EDUCATION; FAMILY; FRIEND; HISTORY; HUMAN; LABORATORY PERSONNEL; LEADERSHIP; MENTOR; PHARMACY SCHOOL;

ANNIVERSARIES AND SPECIAL EVENTS; FACULTY, PHARMACY; FAMILY; FRIENDS; HISTORY, 20TH CENTURY; HISTORY, 21ST CENTURY; HUMANS; LABORATORY PERSONNEL; LEADERSHIP; MENTORS;

EID: 84964422513     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.24687     Document Type: Article

References (216)

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4. E.E. Smissman, R.T. Borchardt, and K.B. Schowen Conformational aspects of systems related to acetylcholine. 4. The syntheses of the dl-2-dimethylamino-trans-decalin methiodides J Med Chem 15 5 1972 545 548
5. S. Milstien, and L.A. Cohen Stereopopulation control. I. Rate enhancement in the lactonizations of 0-hydroxyhydrocinnamic acids J Am Chem Soc 94 26 1972 9158 9165
6. R.T. Borchardt, and L.A. Cohen Stereopopulation control. II. Rate enhancement of intramolecular nucleophilic displacement J Am Chem Soc 94 26 1972 9166 9174
7. R.T. Borchardt, and L.A. Cohen Stereopopulation control. III. Facilitation of intramolecular conjugate addition of the carboxyl group J Am Chem Soc 94 26 1972 9175 9182
8. R.T. Borchardt, and L.A. Cohen Stereopopulation control. IV. Facilitation of intramolecular conjugate addition of solvated hydroxyl groups J Am Chem Soc 95 25 1973 8303 8313
9. R.T. Borchardt, and L.A. Cohen Stereopopulation control. V. Facilitation of intramolecular conjugate addition of an aldehyde hydrate and hemiacetal J Am Chem Soc 95 25 1973 8313 8319
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17. R.T. Borchardt, and D. Thakker Affinity labeling of catechol-O-methyltransferase with N-iodoacetyl-3,5-dimethoxy-4-hydroxyphenylethylamine Biochem Biophys Res Commun 54 3 1973 1233 1239
18. R.T. Borchardt Affinity labeling of catechol-O-methyltransferase by the oxidation products of 6-hydroxydopamine Mol Pharmacol 11 1975 436 449
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21. R.T. Borchardt, and D.R. Thakker Affinity labeling of catechol O-methyltransferase by N-haloacetyl derivatives of 3,5-dimethoxy-4-hydroxyphenylethylamine and 3,4-dimethoxy-5-hydroxyphenylethylamine. Kinetics of inactivation Biochemistry 14 20 1975 4543 4551
22. R.T. Borchardt, E.E. Smissman, D. Nerland, and J.R. Reid Catechol O-methyltransferase. 7. Affinity labeling with the oxidation products of 6-aminodopamine J Med Chem 19 1 1976 30 37
23. R.T. Borchardt Chemical probes of the active site of catechol-O-methyltransferase E. Usdin, N. Weiner, Biochemistry and function of monoamine enzymes 1977 Marcel Dekker New York 707 726
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25. R.T. Borchardt, and D.R. Thakker Evidence for sulfhydryl groups at the active site of catechol-O-methyltransferase Biochim Biophys Acta 445 3 1976 598 609
26. M.R. Hegazi, R.T. Borchardt, and R.L. Schowen An SN2-like transition state for methyl transfer catalyzed by catechol-O-methyltransferase J Am Chem Soc 98 1976 3048 3049
27. M.F. Hegazi, R.T. Borchardt, and R.L. Schowen Alpha-deuterium and carbon-13 isotope effects for methyl transfer catalyzed by catechol-O-methyltransferase: SN2-like transition state J Am Chem Soc 101 1979 4359 4365
28. J. Olsen, Y.S. Wu, R.T. Borchardt, and R.L. Schowen Transition-state structure and catalytic power in methyl transfer. In Transmethylation E. Usdin, R.T. Borchardt, C.R. Creveling, 1979 Elsevier-North Holland New York 127 133
29. P.E. Hanna, and R.T. Borchardt Histamine N-methyltransferase. Inhibition and potentiation by trans- and cis-1,5-diphenyl-3-dimethylaminopyrrolidine J Med Chem 17 4 1974 741 743
30. R.T. Borchardt, Y.S. Wu, and B.S. Wu S-adenosyl-l-homocysteine dialdehyde: An affinity labeling reagent for histamine-N-methyltransferase Biochem Biophys Res Commun 78 3 1977 1025 1033
31. R.T. Borchardt, Y.S. Wu, and B.S. Wu Affinity labeling of histamine N-methyltransferase by 2′,3′-dialdehyde derivatives of S-adenosylhomocysteine and S-adenosylmethionine. Kinetics of inactivation Biochemistry 17 20 1978 4145 4152
32. R.T. Borchardt Inhibition of indolethylamine-N-methyltransferase by analogs of S-adenosylhomocysteine Biochem Pharmacol 24 16 1975 1542 1544
33. P.S. Leboy, J.M. Glick, F.G. Steiner, S. Haney, and R.T. Borchardt S-adenosylhomocysteine analogues as inhibitors of specific tRNA methylation Biochim Biophys Acta 520 1 1978 153 163
34. G.L. Grunewald, J.M. Grindel, W.C. Vincek, and R.T. Borchardt Importance of the aromatic ring in adrenergic amines. Nonaromatic analoques of phenylethanolamine as substrates for phenylethanolamine N-methyltransferase Mol Pharmacol 11 5 1975 694 699
35. G.L. Grunewald, W.C. Vincek, D.P. Davis, and R.T. Borchardt Some new inhibitors of epinephrine biosynthesis E. Usdin, I.J. Kopin, J. Barchas, Catecholamines: Basic and clinical frontiers 1979 Pergamon Press New York 189 191
36. W.C. Vincek, C.S. Aldrich, R.T. Borchardt, and G.L. Grunewald Importance of the aromatic ring in adrenergic amines. 5. Nonaromatic analogues of phenylethanolamine as inhibitors of phenylethanolamine N-methyltransferase: Role of hydrophobic and steric interactions J Med Chem 24 1 1981 7 12
37. D.P. Davis, R.T. Borchardt, and G.L. Grunewald Importance of the aromatic ring in adrenergic amines. 6. Nonaromatic analogues of phenylethanolamine as inhibitors of phenylethanolamine N-methyltransferase: Role of pi-electronic and steric interactions J Med Chem 24 1 1981 12 16
38. G.L. Grunewald, R.T. Borchardt, M.F. Rafferty, and P. Krass Conformational preferences of amphetamine analogues for inhibition of phenylethanolamine N-methyltransferase. Conformationally defined adrenergic agents. 5 Mol Pharmacol 20 2 1981 377 381
39. N.Y. Liang, R.E. Tessel, G.L. Grunewald, and R.T. Borchardt Inhibitors of phenylethanolamine N-methyltransferase. 1. Effects of 2-cycloocytyl-2-hydroxyethylamine on rat brain and adrenal catecholamine content and blood pressure J Pharmacol Exp Ther 223 2 1982 375 381
40. N.Y. Liang, R.E. Tessel, G.L. Grunewald, and R.T. Borchardt Inhibitors of phenylethanolamine-N-methyltransferase. 2. Comparison of nonaromatic analogs of phenylethanolamines, 7,8-dichloro-1,2,3,4-tetrahydroisoquinoline (SKF-64139) and 2,3-dichloro-alpha-methylbenzylamine: Effects on rat brain and adrenal catecholamine content and blood pressure J Pharmacol Exp Ther 223 2 1982 382 387
41. M.F. Rafferty, D.S. Wilson, J.A. Monn, P. Krass, R.T. Borchardt, and G.L. Grunewald Importance of the aromatic ring in adrenergic amines. 7. Comparison of the stereoselectivity of norepinephrine N-methyltransferase for aromatic vs. nonaromatic substrates and inhibitors J Med Chem 25 10 1982 1198 1204
42. M.F. Rafferty, P. Krass, R.T. Borchardt, and G.L. Grunewald Importance of the aromatic ring in adrenergic amines. 8. 2-(Aminomethyl)-trans-2-decalols as inhibitors of norepinephrine N-methyltransferase J Med Chem 25 10 1982 1250 1252
43. G.L. Grunewald, J.A. Monn, M.F. Rafferty, R.T. Borchardt, and P. Krass Probes of the active site of norepinephrine N-methyltransferase: Effect of hydrophobic and hydrophilic interactions on side-chain binding of amphetamine and alpha-methylbenzylamine J Med Chem 25 10 1982 1248 1250
44. M.F. Rafferty, R.T. Borchardt, and G.L. Grunewald Directional probes of the hydrophobic component of the aromatic ring binding site of norepinephrine N-methyltransferase J Med Chem 25 10 1982 1204 1208
45. N.Y. Liang, R.T. Borchardt, J.C. Choi, R.E. Tessel, and G.L. Grunewald Effects of phenylethanolamine N-methyltransferase inhibitors on rat brain catecholamine levels and body temperature Res Commun Chem Pathol Pharmacol 37 3 1982 445 452
46. N.Y. Liang, J.A. Hower, and R.T. Borchardt Effects of phenylethanolamine N-methyltransferase inhibitors on uptake and release of norepinephrine and dopamine from rat brain Res Commun Chem Pathol Pharmacol 49 3 1985 467 470
47. G.L. Grunewald, T.M. Caldwell, Q. Li, M. Slavica, K.R. Criscione, R.T. Borchardt, and W. Wang Synthesis and biochemical evaluation of 3-fluoromethyl-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor J Med Chem 42 18 1999 3588 3601
48. L. Eiden, R.T. Borchardt, and C.O. Rutledge Protein carboxymethylation in neurosecretary process E. Usdin, R.T. Borchardt, C.R. Creveling, Transmethylation 1979 Elsevier North-Holland New York 539 546
49. R.T. Borchardt, L.E. Eiden, B. Wu, and C.O. Rutledge Sinefungin, a potent inhibitor or S-adenosylmethionine: Protein O-methyltransferase Biochem Biophys Res Commun 89 3 1979 919 924
50. L.E. Eiden, R.T. Borchardt, and C.O. Rutledge Characteristics of protein carboxyl methylation in the rat hypothalamus J Neurochem 38 3 1982 631 637
51. R.T. Borchardt, D. Kuonen, J.A. Huber, and A. Moorman Inhibition of calf thymus and rat hypothalamic synaptosomal protein carboxymethyltransferase by analogues of S-adenosylhomocysteine Mol Pharmacol 21 1 1982 181 186
52. R.T. Borchardt, and Y.S. Wu Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 5. Role of the asymmetric sulfonium pole in the enzymatic binding of S-adenosyl-l-methionine J Med Chem 19 9 1976 1099 1103
53. C.S. Pugh, R.T. Borchardt, and H.O. Stone Inhibition of Newcastle disease virion messenger RNA (guanine-7-)-methyltransferase by analogues of S-adenosylhomocysteine Biochemistry 16 17 1977 3928 3932
54. C.S. Pugh, R.T. Borchardt, and H.O. Stone Sinefungin, a potent inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication J Biol Chem 253 12 1978 4075 4077
55. A.M. Wertheimer, S.Y. Chen, R.T. Borchardt, and Y. Furuichi S-adenosylmethionine and its analogs. Structural features correlated with synthesis and methylation of mRNAs of cytoplasmic polyhedrosis virus J Biol Chem 255 12 1980 5924 5930
56. C.S. Pugh, and R.T. Borchardt Effects of S-adenosylhomocysteine analogues on vaccinia viral messenger ribonucleic acid synthesis and methylation Biochemistry 21 7 1982 1535 1541
57. R.T. Borchardt, and Y.S. Wu Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 1. Modification of the amino acid portion of S-adenosylhomocysteine J Med Chem 17 8 1974 862 868
58. R.T. Borchardt, J.A. Huber, and Y.S. Wu Potential inhibitor of S-adenosylmethionine-dependent methyltransferases. 2. Modification of the base portion of S-adenosylhomocysteine J Med Chem 17 8 1974 868 873
59. R.T. Borchardt Synthesis and biological activity of analogs of S-adenosylhomocysteine and inhibitors of methyltransferases F. Solvatore, E. Borck, V. Zappia, H.G. Williams-Ashman, F. Schlenk, The biochemistry of S-adenosylmethionine 1977 Columbia University Press New York 151 170
60. R.T. Borchardt, and Y.S. Wu Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 3. Modifications of the sugar portion of S-adenosylhomocysteine J Med Chem 18 3 1975 300 304
61. R.T. Borchardt, and Y. Wu S-aristeromycinyl-L-homocysteine, apotent inhibitor of S-adenosylmethionine-dependent transmethylations J Med Chem 19 1 1976 197 198
62. R.T. Borchardt, J.A. Huber, and Y.S. Wu Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 4. Further modifications of the amino and base portions of S-adenosyl-L-homocysteine J Med Chem 19 9 1976 1094 1099
63. R.T. Borchardt, Y.S. Wu, J.A. Huber, and A.F. Wycpalek Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 6. Structural modifications of S-adenosylmethionine J Med Chem 19 9 1976 1104 1110
64. R.T. Borchardt, Y.S. Wu, and B.S. Wu Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 7. Role of the ribosyl moiety in enzymatic binding of S-adenosyl-L-homocysteine and S-adenosyl-l-methionine J Med Chem 21 12 1978 1307 1310
65. R.T. Borchardt S-adenosyl-l-methionine-dependent macro-molecule methyltransferases: Potential targets for the design of chemotherapeutic agents J Med Chem 23 4 1980 347 357
66. R.T. Borchardt, B.T. Keller, and U. Patel-Thombre Neplanocin A. A potent inhibitor of S-adenosylhomocysteine hydrolase and of vaccinia virus multiplication in mouse L929 cells J Biol Chem 259 7 1984 4353 4358
67. M. Hasobe, J.G. McKee, D.R. Borcherding, and R.T. Borchardt 9-(Trans-2′,trans-3′-dihydroxycyclopent-4′-enyl)-adenine and -3-deazaadenine: Analogs of neplanocin A which retain potent antiviral activity but exhibit reduced cytotoxicity Antimicrob Agents Chemother 31 11 1987 1849 1851
68. D.M. Houston, E.K. Dolence, B.T. Keller, U. Patel-Thombre, and R.T. Borchardt Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 8. Molecular dissections of carbocyclic 3-deazaadenosine as inhibitors of S-adenosylhomocysteine hydrolase J Med Chem 28 4 1985 467 471
69. D.M. Houston, E.K. Dolence, B.T. Keller, U. Patel-Thombre, and R.T. Borchardt Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 9. 2′,3′-Dialdehyde derivatives of carbocyclic purine nucleosides as inhibitors of S-adenosylhomocysteine hydrolase J Med Chem 28 4 1985 471 477
70. D.M. Houston, B. Matuszewska, and R.T. Borchardt Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 10. Base- and amino acid modified analogues of S-aristeromycinyl-L-homocysteine J Med Chem 28 4 1985 478 482
71. B.T. Keller, and R.T. Borchardt Adenosine dialdehyde: A potent inhibitor of vaccinia virus multiplication in mouse L929 cells Mol Pharmacol 31 5 1987 485 492
72. D.R. Borcherding, S.A. Scholtz, and R.T. Borchardt Synthesis of analogs of neplanocin-A - Utilization of optically-active dihydroxycyclopentenones derived from carbohydrates J Org Chem 52 24 1987 5457 5461
73. M. Hasobe, J.G. McKee, D.R. Borcherding, B.T. Keller, and R.T. Borchardt Effects of 9-(trans-2′,trans-3′-dihydroxycyclopent-4′-enyl)-adenine and -3-deazaadenine on the metabolism of S-adenosylhomocysteine in mouse L929 cells Mol Pharmacol 33 6 1988 713 720
74. D.R. Borcherding, S. Narayanan, M. Hasobe, J.G. McKee, B.T. Keller, and R.T. Borchardt Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 11. Molecular dissections of neplanocin A as potential inhibitors of S-adenosylhomocysteine hydrolase J Med Chem 31 9 1988 1729 1738
75. S.R. Narayanan, B.T. Keller, D.R. Borcherding, S.A. Scholtz, and R.T. Borchardt 9-(Trans-2′,trans-3′-dihydroxycyclopent-4′-enyl) derivatives of adenine and 3-deazaadenine: Potent inhibitors of bovine liver S-adenosylhomocysteine hydrolase J Med Chem 31 3 1988 500 503
76. M. Hasobe, J.G. McKee, and R.T. Borchardt Relationship between intracellular concentration of S-adenosylhomocysteine and inhibition of vaccinia virus replication and inhibition of murine L-929 cell growth Antimicrob Agents Chemother 33 6 1989 828 834
77. M. Hasobe, J.G. McKee, H. Ishii, M. Cools, R.T. Borchardt, and E. De Clercq Elucidation of the mechanism by which homocysteine potentiates the anti-vaccinia virus effects of the S-adenosylhomocysteine hydrolase inhibitor 9-(trans-2′,trans-3′-dihydroxycyclopent-4′-enyl)-adenine Mol Pharmacol 36 3 1989 490 496
78. E. De Clercq, M. Cools, J. Balzarini, V.E. Marquez, D.R. Borcherding, R.T. Borchardt, J.C. Drach, S. Kitaoka, and T. Konno Broad-spectrum antiviral activities of neplanocin A, 3-deazaneplanocin A, and their 5′-nor derivatives Antimicrob Agents Chemother 33 8 1989 1291 1297
79. I. Votruba, M. Hasobe, A. Holy, and R.T. Borchardt 2-Methylpropyl ester of 3-(adenin-9-yl)-2-hydroxypropanoic acid. Mechanism of antiviral action in vaccinia virus-infected L929 cells Biochem Pharmacol 39 10 1990 1573 1580
80. M.S. Wolfe, and R.T. Borchardt S-adenosyl-L-homocysteine hydrolase as a target for antiviral chemotherapy J Med Chem 34 5 1991 1521 1530
81. M.S. Wolfe, Y. Lee, W.J. Bartlett, D.R. Borcherding, and R.T. Borchardt 4′-Modified analogues of aristeromycin and neplanocin A: Synthesis and inhibitory activity toward S-adenosyl-L-homocysteine hydrolase J Med Chem 35 10 1992 1782 1791
82. S. Liu, M.S. Wolfe, and R.T. Borchardt Rational approaches to the design of antiviral agents based on S-adenosyl-L-homocysteine hydrolase as a molecular target Antiviral Res 19 3 1992 247 265
83. M.J. Robins, V. Samano, W. Zhang, J. Balzarini, E. De Clercq, R.T. Borchardt, Y. Lee, and C.S. Yuan Nucleic acid related compounds. 74. Synthesis and biological activity of 2′(and 3′)-deoxy-2′(and 3′)-methylenenucleoside analogues that function as mechanism-based inhibitors of S-adenosyl-L-homocysteine hydrolase and/or ribonucleotide reductase J Med Chem 35 12 1992 2283 2293
84. D.B. Ault-Riche, Y. Lee, C.S. Yuan, M. Hasobe, M.S. Wolfe, D.R. Borcherding, and R.T. Borchardt Effects of 4′-modified analogs of aristeromycin on the metabolism of S-adenosyl-L-homocysteine in murine L929 cells Mol Pharmacol 43 6 1993 989 997
85. M.J. Robins, S.F. Wnuk, K.B. Mullah, N.K. Dalley, C.S. Yuan, Y.H. Lee, and R.T. Borchardt Nucleic-acid related-compounds. 80. Synthesis of 5′-S-(alkyl and aryl)-5′-fluoro-5′-thioadenosines with xenon difluoride or (diethylamido)sulfur trifluoride, hydrolysis in aqueous buffer, and inhibition of S-adenosyl-L-homocysteine hydrolase by derived adenosine 5′-aldehyde species J Org Chem 59 3 1994 544 555
86. S.F. Wnuk, C.S. Yuan, R.T. Borchardt, J. Balzarini, E. De Clercq, and M.J. Robins Nucleic acid related compounds. 84. Synthesis of 6′-(E and Z)-halohomovinyl derivatives of adenosine, inactivation of S-adenosyl-L-homocysteine hydrolase, and correlation of anticancer and antiviral potencies with enzyme inhibition J Med Chem 37 21 1994 3579 3587
87. U.G. Patel, and R.T. Borchardt Adenine nucleoside 2′,3′-dialdehydes: Potent inhibitors of bovine liver S-adenosylhomocysteine hydrolase Biochemistry 24 1985 1130 1136
88. B.T. Keller, R.S. Clark, A.E. Pegg, and R.T. Borchardt Purification and characterization of some metabolic effects of S-neplanocylmethionine Mol Pharmacol 28 4 1985 364 370
89. B. Matuszewska, and R.T. Borchardt The role of nicotinamide adenine dinucleotide in the inhibition of bovine liver S-adenosylhomocysteine hydrolase by neplanocin A J Biol Chem 262 1 1987 265 268
90. S.D. Paisley, M.S. Wolfe, and R.T. Borchardt Oxidation of neplanocin A to the corresponding 3′-keto derivative by S-adenosylhomocysteine hydrolase J Med Chem 32 7 1989 1415 1418
91. J.L. Wolfe, D. Vandervelde, and R.T. Borchardt Facilitated intramolecular conjugate addition of N-(P-methoxyphenyl)-3-(3′,6′-dioxo-2′,4′-dimethylcyclohexa-1′,4′-dienyl)-3,3-dimethylpropionamide. 1. Product characterization J Org Chem 57 23 1992 6138 6142
92. S.M. Liu, M.S. Wolfe, C.S. Yuan, S.M. Ali, and R.T. Borchardt Synthesis and evaluation of 4′,5′-dehydro-5′-fluoroaristeromycins as S-adenosyl-L-homocysteine (AdoHcy) hydrolase inhibitors Bioorg Med Chem Lett 2 12 1992 1741 1744
93. S. Liu, S.F. Wnuk, C. Yuan, M.J. Robins, and R.T. Borchardt Adenosine-5′-carboxaldehyde: A potent inhibitor of S-adenosyl-L-homocysteine hydrolase J Med Chem 36 7 1993 883 887
94. C.S. Yuan, S.M. Liu, S.F. Wnuk, M.J. Robins, and R.T. Borchardt Rational approaches to the design of mechanism-based inhibitors of S-adenosylhomocysteine hydrolase Nucleos Nucleot 14 3-5 1995 439 447
95. C.S. Yuan, S. Liu, S. Wnuk, M.J. Robins, and R.T. Borchardt Design and synthesis of S-adenosylhomocysteine hydrolase as broad-spectrum antiviral agents E.D. Clercq, Advances in antiviral drug design 1996 JAI Press, Inc. Greenwick, Connecticut 41 88
96. S. Liu, C.S. Yuan, and R.T. Borchardt Aristeromycin-5′-carboxaldehyde: A potent inhibitor of S-adenosyl-L-homocysteine hydrolase J Med Chem 39 12 1996 2347 2353
97. S.F. Wnuk, S. Liu, C.S. Yuan, R.T. Borchardt, and M.J. Robins Inactivation of S-adenosyl-L-homocysteine hydrolase by amide and ester derivatives of adenosine-5′-carboxylic acid J Med Chem 39 21 1996 4162 4166
98. S.F. Wnuk, C.S. Yuan, R.T. Borchardt, J. Balzarini, E. De Clercq, and M.J. Robins Anticancer and antiviral effects and inactivation of S-adenosyl-L-homocysteine hydrolase with 5′-carboxaldehydes and oximes synthesized from adenosine and sugar-modified analogues J Med Chem 40 11 1997 1608 1618
99. S.F. Wnuk, C.S. Yuan, R.T. Borchardt, and M.J. Robins Synthesis of homologated halovinyl derivatives from aristeromycin and their inhibition of human placental S-adenosyl-L-homocysteine hydrolase Nucleos Nucleot 17 1-3 1998 99 113
100. M.J. Robins, S.F. Wnuk, X. Yang, C.S. Yuan, R.T. Borchardt, J. Balzarini, and E. De Clercq Inactivation of S-adenosyl-L-homocysteine hydrolase and antiviral activity with 5′,5′,6′,6′-tetradehydro-6′-deoxy-6′-halohomoadenosine analogues (4'-haloacetylene analogues derived from adenosine) J Med Chem 41 20 1998 3857 3864
101. C.S. Yuan, Y. Saso, E. Lazarides, R.T. Borchardt, and M.J. Robins Recent advances in S-adenosyl-L-homocysteine hydrolase inhibitors and their potential clinical applications Expert Opin Ther Pat 9 9 1999 1197 1206
102. S.F. Wnuk, C.S. Yuan, R.T. Borchardt, and M.J. Robins Design and biological evaluation of new mechanism-based inhibitors of S-adenosyl-L-homocysteine hydrolase Nucleos Nucleot 18 4-5 1999 595 596
103. D. Yin, X. Yang, C.S. Yuan, and R.T. Borchardt Mechanism-based S-adenosyl-L-homocysteine hydrolase inhibitors in the search for broad-spectrum antiviral agents P.F. Torrence, Biomedical chemistry: Applying chemical principles to the understanding and treatment of disease 2000 John Wiley & Sons, Inc New York 41 71
104. S.F. Wnuk, C.A. Valdez, J. Khan, P. Moutinho, M.J. Robins, X.D. Yang, R.T. Borchardt, J. Balzarini, and E. De Clercq Doubly homologated dihalovinyl and acetylene analogues of adenosine: Synthesis, interaction with S-adenosyl-L-homocysteine hydrolase, and antiviral and cytostatic effects J Med Chem 43 6 2000 1180 1186
105. X. Yang, D. Yin, S.F. Wnuk, M.J. Robins, and R.T. Borchardt Mechanisms of inactivation of human S-adenosylhomocysteine hydrolase by 5′,5′,6′,6′-tetradehydro-6′-deoxy-6′-halohomoadenosines Biochemistry 39 49 2000 15234 15241
106. S.F. Wnuk, B.O. Ro, C.A. Valdez, E. Lewandowska, N.X. Valdez, P.R. Sacasa, D. Yin, J. Zhang, R.T. Borchardt, and E. De Clercq Sugar-modified conjugated diene analogues of adenosine and uridine: Synthesis, interaction with S-adenosyl-L-homocysteine hydrolase, and antiviral and cytostatic effects J Med Chem 45 12 2002 2651 2658
107. R.W. Miles, L.P. Nielsen, G.J. Ewing, D. Yin, R.T. Borchardt, and M.J. Robins S-homoadenosyl-L-cysteine and S-homoadenosyl-L-homocysteine. Synthesis and binding studies of hon-hydrolyzed substrate analogues with S-adenosyl-L-homocysteine hydrolase J Org Chem 67 23 2002 8258 8260
108. S.F. Wnuk, P.R. Sacasa, L.N. Crain, E. Lewandowska, J. Zhang, and R.T. Borchardt Stereocontrolled synthesis of diene and enyne sugar-modified nucleosides and their interaction with S-adenosyl-L-homocysteine hydrolase Nucleosides Nucleotides Nucleic Acids 22 5-8 2003 783 785
109. S.F. Wnuk, E. Lewandowska, P.R. Sacasa, L.N. Crain, J. Zhang, R.T. Borchardt, and E. De Clercq Stereoselective synthesis of sugar-modified enyne analogues of adenosine and uridine. Interaction with S-adenosyl-L-homocysteine hydrolase and antiviral and cytotoxic effects J Med Chem 47 21 2004 5251 5257
110. M. Wang, J. Zhang, D. Andrei, K. Kuczera, R.T. Borchardt, and S.F. Wnuk Are L-adenosine and its derivatives substrates for S-adenosyl-L-homocysteine hydrolase? J Med Chem 48 10 2005 3649 3653
111. S.F. Wnuk, P.R. Sacasa, E. Lewandowska, D. Andrei, S. Cai, and R.T. Borchardt Synthesis of 5′-functionalized nucleosides: S-adenosylhomocysteine analogues with the carbon-5′ and sulfur atoms replaced by a vinyl or halovinyl unit Bioorg Med Chem 16 10 2008 5424 5433
112. B.T. Keller, and R.T. Borchardt Metabolic conversion of neplanocin-A to S-neplanocylmethionine by mouse L929-cells Biochem Biophys Res Commun 120 1 1984 131 137
113. C.S. Yuan, D.B. Ault-Riche, and R.T. Borchardt Chemical modification and site-directed mutagenesis of cysteine residues in human placental S-adenosylhomocysteine hydrolase J Biol Chem 271 45 1996 28009 28016
114. M.A. Turner, C.S. Yuan, R.T. Borchardt, M.S. Hershfield, G.D. Smith, and P.L. Howell Structure determination of selenomethionyl S-adenosylhomocysteine hydrolase using data at a single wavelength Nat Struct Biol 5 5 1998 369 376
115. X. Yang, Y. Hu, D.H. Yin, M.A. Turner, M. Wang, R.T. Borchardt, P.L. Howell, K. Kuczera, and R.L. Schowen Catalytic strategy of S-adenosyl-L-homocysteine hydrolase: Transition-state stabilization and the avoidance of abortive reactions Biochemistry 42 7 2003 1900 1909
116. Y. Hu, X. Yang, D.H. Yin, J. Mahadevan, K. Kuczera, R.L. Schowen, and R.T. Borchardt Computational characterization of substrate binding and catalysis in S-adenosylhomocysteine hydrolase Biochemistry 40 50 2001 15143 15152
117. P. Elrod, J. Zhang, X. Yang, D. Yin, Y. Hu, R.T. Borchardt, and R.L. Schowen Contributions of active site residues to the partial and overall catalytic activities of human S-adenosylhomocysteine hydrolase Biochemistry 41 25 2002 8134 8142
118. M. Wang, J.R. Unruh, C.K. Johnson, K. Kuczera, R.L. Schowen, and R.T. Borchardt Effects of ligand binding and oxidation on hingebending motions in S-adenosyl-L-homocysteine hydrolase Biochemistry 45 25 2006 7778 7786
119. Q.S. Li, S. Cai, R.T. Borchardt, J. Fang, K. Kuczera, C.R. Middaugh, and R.L. Schowen Comparative kinetics of cofactor association and dissociation for the human and trypanosomal S-adenosylhomocysteine hydrolases. 1. Basic features of the association and dissociation processes Biochemistry 46 19 2007 5798 5809
120. C. Hu, J. Fang, R.T. Borchardt, R.L. Schowen, and K. Kuczera Molecular dynamics simulations of domain motions of substrate-free S-adenosyl-L-homocysteine hydrolase in solution Proteins 71 1 2008 131 143
121. D.B. Ault-Riche, C.S. Yuan, and R.T. Borchardt A single mutation at lysine 426 of human placental S-adenosylhomocysteine hydrolase inactivates the enzyme J Biol Chem 269 50 1994 31472 31478
122. D. Yin, X. Yang, Y. Hu, K. Kuczera, R.L. Schowen, R.T. Borchardt, and T.C. Squier Substrate binding stabilizes S-adenosylhomocysteine hydrolase in a closed conformation Biochemistry 39 32 2000 9811 9818
123. M.A. Turner, X.D. Yang, D. Yin, K. Kuczera, R.T. Borchardt, and P.L. Howell Structure and function of S-adenosylhomocysteine hydrolase Cell Biochem Biophys 33 2 2000 101 125
124. C.S. Yuan, J. Yeh, S. Liu, and R.T. Borchardt Mechanism of inactivation of S-adenosylhomocysteine hydrolase by (Z)-4′,5′-didehydro-5′-deoxy-5′-fluoroadenosine J Biol Chem 268 23 1993 17030 17037
125. C.S. Yuan, J. Yeh, T.C. Squier, A. Rawitch, and R.T. Borchardt Ligand-dependent changes in intrinsic fluorescence of S-adenosylhomocysteine hydrolase: Implications for the mechanism of inhibitor-induced inhibition Biochemistry 32 39 1993 10414 10422
126. M. Hasobe, H. Liang, D.B. Aultriche, D.R. Borcherding, M.S. Wolfe, and R.T. Borchardt (1′r,2′s,3′r)-9-(2′,3′-Dihydroxycyclopentan-1′-Yl)-adenine and 3-deaza-adenine - Analogs of aristeromycin which exhibit potent antiviral activity with reduced cytotoxicity Antiviral Chem Chemother 4 4 1993 245 248
127. C.S. Yuan, S.F. Wnuk, S. Liu, M.J. Robins, and R.T. Borchardt (E)-5′,6′-didehydro-6′-deoxy-6′-fluorohomoadenosine: A substrate that measures the hydrolytic activity of S-adenosylhomocysteine hydrolase Biochemistry 33 40 1994 12305 12311
128. C.S. Yuan, and R.T. Borchardt Photoaffinity labeling of human placental S-adenosylhomocysteine hydrolase with [2-3H]8-azido-adenosine J Biol Chem 270 27 1995 16140 16146
129. H. Huang, C.S. Yuan, S.F. Wnuk, M.J. Robins, and R.T. Borchardt The mechanism of inactivation of human placental S-adenosylhomocysteine hydrolase by (E)-4′,5′-didehydro-5′-methoxyadenosine and adenosine 5'-carboxaldehyde oxime Arch Biochem Biophys 343 1 1997 109 117
130. S.F. Wnuk, Y. Mao, C.S. Yuan, R.T. Borchardt, G. Andrei, J. Balzarini, E. De Clercq, and M.J. Robins Discovery of type II (covalent) inactivation of S-adenosyl-L-homocysteine hydrolase involving its "hydrolytic activity": Synthesis and evaluation of dihalohomovinyl nucleoside analogues derived from adenosine J Med Chem 41 16 1998 3078 3083
131. C.S. Yuan, S.F. Wnuk, M.J. Robins, and R.T. Borchardt A novel mechanism-based inhibitor (6′-bromo-5′,6′-didehydro-6′-deoxy-6′-fluorohomoadenosine) that covalently modifies human placental S-adenosylhomocysteine hydrolase J Biol Chem 273 29 1998 18191 18197
132. M.J. Robins, V. Neschadimenko, B.O. Ro, C.S. Yuan, R.T. Borchardt, and S.F. Wnuk Nucleic acid related compounds. 101. S-adenosyl-L-homocysteine hydrolase does not hydrate (5′-fluoro)vinyl or (6′-halo)homovinyl analogues derived from 3′-deoxyadenosine or 3′-(chloro or fluoro)-3′-deoxyadenosine J Org Chem 63 4 1998 1205 1211
133. Q.S. Li, S. Cai, J. Fang, R.T. Borchardt, K. Kuczera, C.R. Middaugh, and R.L. Schowen Comparative kinetics of cofactor association and dissociation for the human and trypanosomal S-adenosylhomocysteine hydrolases. 2. The role of helix 18 stability Biochemistry 47 17 2008 4983 4991
134. S. Cai, Q.S. Li, R.T. Borchardt, K. Kuczera, and R.L. Schowen The antiviral drug ribavirin is a selective inhibitor of S-adenosyl-L-homocysteine hydrolase from trypanosoma cruzi Bioorg Med Chem 15 23 2007 7281 7287
135. S. Cai, Q.S. Li, J. Fang, R.T. Borchardt, K. Kuczera, C.R. Middaugh, and R.L. Schowen The rationale for targeting the NAD/NADH cofactor binding site of parasitic S-adenosyl-L-homocysteine hydrolase for the design of anti-parasitic drugs Nucleosides Nucleotides Nucleic Acids 28 5 2009 485 503
136. Q.S. Li, S. Cai, J. Fang, R.T. Borchardt, K. Kuczera, C.R. Middaugh, and R.L. Schowen Evaluation of NAD(H) analogues as selective inhibitors for Trypanosoma cruzi S-adenosylhomocysteine hydrolase Nucleosides Nucleotides Nucleic Acids 28 5 2009 473 484
137. S. Cai, J. Fang, Q.S. Li, R.T. Borchardt, K. Kuczera, C.R. Middaugh, and R.L. Schowen Comparative kinetics of cofactor association and dissociation for the human and trypanosomal S-adenosylhomocysteine hydrolases. 3. Role of lysyl and tyrosyl residues of the C-terminal extension Biochemistry 49 38 2010 8434 8441
138. R.T. Borchardt Hidalgo, I.J., Raub, T.J. and Borchardt, R.T.: Colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability. Gastroenterology, 96, 736-749, 1989 - The backstory APPS J 13 3 2011 323 327
139. R.T. Borchardt Interview with a distinguished pharmaceutical scientist: Ronald T. Borchardt, Ph.D., recipient of the 1997 AAPS distinguished pharmaceutical scientist award Pharm Res 14 11 1997 1500 1503
140. R.T. Borchardt Drug design with ADME in mind; recent paradigm shift in drug discovery. Solvay Pharmaceuticals Conference on Medicinal Chemistry - Towards drugs of the future: Key issues in lead finding and lead optimization, 2007 2008 IOS Press Garmisch-Partenkirchen, Germany, Amsterdam 57 74
141. I. Osiecka, P.A. Porter, R.T. Borchardt, J.A. Fix, and C.R. Gardner In vitro drug absorption models. I. Brush border membrane vesicles, isolated mucosal cells and everted intestinal rings: Characterization and salicylate accumulation Pharm Res 2 6 1985 284 293
142. I. Osiecka, M. Cortese, P.A. Porter, R.T. Borchardt, J.A. Fix, and C.R. Gardner Intestinal absorption of alpha-methyldopa: In vitro mechanistic studies in rat small intestinal segments J Pharmacol Exp Ther 242 2 1987 443 449
143. K.L. Audus, and R.T. Borchardt Characterization of an in vitro blood-brain barrier model system for studying drug transport and metabolism Pharm Res 3 2 1986 81 87
144. K.L. Audus, and R.T. Borchardt Characteristics of the large neutral amino acid transport system of bovine brain microvessel endothelial cell monolayers J Neurochem 47 2 1986 484 488
145. S. Rim, K.L. Audus, and R.T. Borchardt Relationship of octanol/buffer and octanol/water partition coefficients to transcellular diffusion across brain microvessel endothelial cell monolayers Int J Pharm 32 1986 79 84
146. J.B. van Bree, K.L. Audus, and R.T. Borchardt Carrier-mediated transport of baclofen across monolayers of bovine brain endothelial cells in primary culture Pharm Res 5 6 1988 369 371
147. J.E. Chastain Jr., and R.T. Borchardt L-a-methyldopa transport across bovine brain microvessel endothelial cell monolayers, a model of the blood brain barrier Neurosci Res Commun 4 1989 147 152
148. J.E. Chastain Jr., and R.T. Borchardt Acivicin transport across bovine brain microvessel endothelial cell monolayers, a model of the blood brain barrier Neurosci Res Commun 6 1990 51 55
149. Y. Takakura, S.L. Kuentzel, T.J. Raub, A. Davies, S.A. Baldwin, and R.T. Borchardt Hexose uptake in primary cultures of bovine brain microvessel endothelial cells. I. Basic characteristics and effects of D-glucose and insulin Biochim Biophys Acta 1070 1 1991 1 10
150. A. Baranczyk-Kuzma, K.L. Audus, and R.T. Borchardt Catecholamine-metabolizing enzymes of bovine brain microvessel endothelial cell monolayers J Neurochem 46 6 1986 1956 1960
151. G.K. Scriba, and R.T. Borchardt Metabolism of catecholamine esters by cultured bovine brain microvessel endothelial cells J Neurochem 53 2 1989 610 615
152. G.K. Scriba, and R.T. Borchardt Metabolism of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) by bovine brain microvessel endothelial cells Brain Res 501 1 1989 175 178
153. A. Baranczyk-Kuzma, J.A. Garren, I.J. Hidalgo, and R.T. Borchardt Substrate specificity and some properties of phenol sulfotransferase from human intestinal Caco-2 cells Life Sci 49 16 1991 1197 1206
154. A. Baranczyk-Kuzma, K.L. Audus, F.L. Guillot, and R.T. Borchardt Effects of selected vasoactive substances on adenylate cyclase activity in brain, isolated brain microvessels, and primary cultures of brain microvessel endothelial cells Neurochem Res 17 2 1992 209 214
155. K.R. Smith, A. Kato, and R.T. Borchardt Characterization of specific receptors for atrial natriuretic factor on cultured bovine brain capillary endothelial cells Biochem Biophys Res Commun 157 1 1988 308 314
156. R.G. Rosenfeld, H. Pham, B.T. Keller, R.T. Borchardt, and W.M. Pardridge Demonstration and structural comparison of receptors for insulin-like growth factor-I and -II (IGF-I and -II) in brain and blood-brain barrier Biochem Biophys Res Commun 149 1 1987 159 166
157. D.W. Miller, B.T. Keller, and R.T. Borchardt Identification and distribution of insulin receptors on cultured bovine brain microvessel endothelial cells: Possible function in insulin processing in the blood-brain barrier J Cell Physiol 161 2 1994 333 341
158. K.L. Audus, J. Rose, W. Wang, and R.T. Borchardt Brain microvessel endothelial cell culture systems W.M. Pardridge, An introduction to the blood-brain barrier: Methodology, biology and pathology 1998 Cambridge University Press New York 86 93
159. M. Rousset, G. Chevalier, J.P. Rousset, E. Dussaulx, and A. Zweibaum Presence and cell growth-related variations of glycogen in human colorectal adenocarcinoma cell lines in culture Cancer Res 39 2 Pt 1 1979 531 534
160. I.J. Hidalgo, T.J. Raub, and R.T. Borchardt Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability Gastroenterology 96 3 1989 736 749
161. I.J. Hidalgo, and R.T. Borchardt Transport of bile acids in a human intestinal epithelial cell line, Caco-2 Biochim Biophys Acta 1035 1 1990 97 103
162. D.C. Kim, A.W. Harrison, M.J. Ruwart, K.F. Wilkinson, J.F. Fisher, I.J. Hidalgo, and R.T. Borchardt Evaluation of the bile acid transporter in enhancing intestinal permeability to renin-inhibitory peptides J Drug Target 1 4 1993 347 359
163. K.Y. Ng, and R.T. Borchardt Biotin transport in a human intestinal epithelial cell line (Caco-2) Life Sci 53 14 1993 1121 1127
164. I. Islam, K.Y. Ng, K.T. Chong, T.J. McQuade, J.O. Hui, K.F. Wilkinson, B.D. Rush, M.J. Ruwart, R.T. Borchardt, and J.F. Fisher Evaluation of a vitamin-cloaking strategy for oligopeptide therapeutics: Biotinylated HIV-1 protease inhibitors J Med Chem 37 2 1994 293 304
165. R.T. Borchardt, P. Smith, and G. Wilson Models for assessing drug absorption and metabolism 1996 Plenum Press New York
166. C. Ehrhardt, and K.-J. Kim Drug absorption studies: In situ, in vitro and in silico models 2008 Springer New York
167. M.C. Manning, K. Patel, and R.T. Borchardt Stability of protein pharmaceuticals Pharm Res 6 11 1989 903 918
168. N.P. Bhatt, K. Patel, and R.T. Borchardt Chemical pathways of peptide degradation. I. Deamidation of adrenocorticotropic hormone Pharm Res 7 6 1990 593 599
169. K. Patel, and R.T. Borchardt Chemical pathways of peptide degradation. II. Kinetics of deamidation of an asparaginyl residue in a model hexapeptide Pharm Res 7 7 1990 703 711
170. K. Patel, and R.T. Borchardt Chemical pathways of peptide degradation. III. Effect of primary sequence on the pathways of deamidation of asparaginyl residues in hexapeptides Pharm Res 7 8 1990 787 793
171. M.C. Lai, M.J. Hageman, R.L. Schowen, R.T. Borchardt, and E.M. Topp Chemical stability of peptides in polymers. 1. Effect of water on peptide deamidation in poly(vinyl alcohol) and poly(vinyl pyrrolidone) matrixes J Pharm Sci 88 10 1999 1073 1080
172. C. Oliyai, J.P. Patel, L. Carr, and R.T. Borchardt Chemical pathways of peptide degradation. VII. Solid state chemical instability of an aspartyl residue in a model hexapeptide Pharm Res 11 6 1994 901 908
173. C.L. Stevenson, A.R. Friedman, T.M. Kubiak, M.E. Donlan, and R.T. Borchardt Effect of secondary structure on the rate of deamidation of several growth hormone releasing factor analogs Int J Pept Protein Res 42 6 1993 497 503
174. B. Li, M.H. O'Meara, J.W. Lubach, R.L. Schowen, E.M. Topp, E.J. Munson, and R.T. Borchardt Effects of sucrose and mannitol on asparagine deamidation rates of model peptides in solution and in the solid state J Pharm Sci 94 8 2005 1723 1735
175. S. Li, C. Schöneich, G.S. Wilson, and R.T. Borchardt Chemical pathways of peptide degradation. V. Ascorbic acid promotes rather than inhibits the oxidation of methionine to methionine sulfoxide in small model peptides Pharm Res 10 11 1993 1572 1579
176. S. Li, T.H. Nguyen, C. Schöneich, and R.T. Borchardt Aggregation and precipitation of human relaxin induced by metal-catalyzed oxidation Biochemistry 34 17 1995 5762 5772
177. B. Li, R.T. Borchardt, E.M. Topp, D. VanderVelde, and R.L. Schowen Racemization of an asparagine residue during peptide deamidation J Am Chem Soc 125 38 2003 11486 11487
178. F.W. Okumu, G.M. Pauletti, D.G. Vander Velde, T.J. Siahaan, and R.T. Borchardt Effect of restricted conformational flexibility on the permeation of model hexapeptides across Caco-2 cell monolayers Pharm Res 14 2 1997 169 175
179. K. Tamura, K.A. Agrios, D. Vander Velde, J. Aube, and R.T. Borchardt Effect of stereochemistry on the transport of Aca-linked betaturn peptidomimetics across a human intestinal cell line Bioorg Med Chem 5 9 1997 1859 1866
180. G.T. Knipp, D.G. Vander Velde, T.J. Siahaan, and R.T. Borchardt The effect of beta-turn structure on the passive diffusion of peptides across Caco-2 cell monolayers Pharm Res 14 10 1997 1332 1340
181. D.C. Kim, P.S. Burton, and R.T. Borchardt A correlation between the permeability characteristics of a series of peptides using an in vitro cell culture model (Caco-2) and those using an in situ perfused rat ileum model of the intestinal mucosa Pharm Res 10 12 1993 1710 1714
182. E.G. Chikhale, P.S. Burton, and R.T. Borchardt The effect of verapamil on the transport of peptides across the blood-brain barrier in rats: Kinetic evidence for an apically polarized efflux mechanism J Pharmacol Exp Ther 273 1 1995 298 303
183. M. Sudoh, G.M. Pauletti, W. Yao, W. Moser, A. Yokoyama, A. Pasternak, P.A. Sprengeler, A.B. Smith 3rd, R. Hirschmann, and R.T. Borchardt Transport characteristics of peptidomimetics. Effect of the pyrrolinone bioisostere on transport across Caco-2 cell monolayers Pharm Res 15 5 1998 719 725
184. J. Gao, O. Murase, R.L. Schowen, J. Aube, and R.T. Borchardt A functional assay for quantitation of the apparent affinities of ligands of P-glycoprotein in Caco-2 cells Pharm Res 18 2 2001 171 176
185. J. Gao, M. Sudoh, J. Aube, and R.T. Borchardt Transport characteristics of peptides and peptidomimetics: I. N-methylated peptides as substrates for the oligopeptide transporter and P-glycoprotein in the intestinal mucosa J Pept Res 57 4 2001 316 329
186. J. Gao, S.L. Winslow, D. Vander Velde, J. Aube, and R.T. Borchardt Transport characteristics of peptides and peptidomimetics: II. Hydroxyethylamine bioisostere-containing peptidomimetics as substrates for the oligopeptide transporter and P-glycoprotein in the intestinal mucosa J Pept Res 57 5 2001 361 373
187. K. Tamura, C.P. Lee, P.L. Smith, and R.T. Borchardt Effect of charge on oligopeptide transporter-mediated permeation of cyclic dipeptides across Caco-2 cell monolayers Pharm Res 13 11 1996 1752 1754
188. K. Tamura, P.K. Bhatnagar, J.S. Takata, C.P. Lee, P.L. Smith, and R.T. Borchardt Metabolism, uptake, and transepithelial transport of the diastereomers of Val-Val in the human intestinal cell line, Caco-2 Pharm Res 13 8 1996 1213 1218
189. K. Tamura, C.P. Lee, P.L. Smith, and R.T. Borchardt Metabolism, uptake, and transepithelial transport of the stereoisomers of Val-Val-Val in the human intestinal cell line, Caco-2 Pharm Res 13 11 1996 1663 1667
190. G.T. Knipp, N.F. Ho, C.L. Barsuhn, and R.T. Borchardt Paracellular diffusion in Caco-2 cell monolayers: Effect of perturbation on the transport of hydrophilic compounds that vary in charge and size J Pharm Sci 86 10 1997 1105 1110
191. J. Li, K. Tamura, C.P. Lee, P.L. Smith, R.T. Borchardt, and I.J. Hidalgo Structure-affinity relationships of Val-Val and Val-Val-Val stereoisomers with the apical oligopeptide transporter in human intestinal Caco-2 cells J Drug Target 5 5 1998 317 327
192. G.M. Pauletti, F.W. Okumu, and R.T. Borchardt Effect of size and charge on the passive diffusion of peptides across Caco-2 cell monolayers via the paracellular pathway Pharm Res 14 2 1997 164 168
193. R.T. Borchardt Physicochemical and biochemical factors that influence the oral delivery of peptide mimetics P.T.P. Kaumaya, R.S. Hodges, Peptides: Chemistry, structure and biology 1996 Escom Science Publishers Leiden, The Netherlands 902 904
194. R.A. Conradi, P.S. Burton, and R.T. Borchardt Physicochemical and biological factors that influence a drug's cellular permeability by passive diffusion V. Pliska, B. Testa, H.V. Waterbeend, Lipophilicity in drug action and toxicity 1996 VCH Weinheim Weinheim, Germany 233 252
195. G.M. Pauletti, S. Gangwar, G.T. Knipp, M.M. Nerurkar, F.W. Okumu, K. Tamura, T.J. Siahaan, and R.T. Borchardt Structural requirements for intestinal absorption of peptide drugs J Control Release 41 1-2 1996 3 17
196. P.S. Burton, R.A. Conradi, N.F. Ho, A.R. Hilgers, and R.T. Borchardt How structural features influence the biomembrane permeability of peptides J Pharm Sci 85 12 1996 1336 1340
197. R.T. Borchardt, E.H. Kerns, C.A. Lipinski, D.R. Thakker, and B. Wang Pharmaceutical profiling in drug discovery for lead selection 2004 AAPS Press Arlington, Virginia
198. R.T. Borchardt, E.H. Kerns, D.R. Thakker, M.J. Hageman, and J.L. Stevens Optimization of the drug-like properties of leads 2006 AAPS Press Arlington, Virginia
199. R.T. Borchardt, R.M. Freidinger, T.K. Sawyer, and P. Smith Integration of pharmaceutical discovery and development: Case histories 1998 Plenum Press New York
200. V. Stella, R.T. Borchardt, M. Hageman, H. Maag, R. Oliyai, and J. Tilley Prodrugs: Challenges and rewards (part I) 2007 AAPS Press Arlington, Virginia
201. V. Stella, R.T. Borchardt, M.J. Hageman, H. Maag, R. Oliyai, and J. Tilley Prodrugs: Challenges and rewards (part II) 2007 AAPS Press Arlington, Virginia
202. G.M. Pauletti, S. Gangwar, T.J. Siahaan, J. Aube, and R.T. Borchardt Improvement of oral peptide bioavailability: Peptide mimetics and prodrug strategies Adv Drug Deliv Rev 27 1997 235 256
203. K.L. Amsberry, and R.T. Borchardt The lactonization of 2'-hydroxyhydrocinnamic acid amides: A potential prodrugs for amides J Org Chem 55 1990 5867 5877
204. B. Wang, S. Liu, and R.T. Borchardt Development of a novel redox-sensitive protecting group for amines which utilizes a facilitated lactonization reaction J Org Chem 60 1995 539 543
205. R.A. Gray, D.G. Vander Velde, C.J. Burke, M.C. Manning, C.R. Middaugh, and R.T. Borchardt Delta-sleep-inducing peptide: Solution conformational studies of a membrane-permeable peptide Biochemistry 33 6 1994 1323 1331
206. B.M. Liederer, T. Fuchs, D. Vander Velde, T.J. Siahaan, and R.T. Borchardt Effects of amino acid chirality and the chemical linker on the cell permeation characteristics of cyclic prodrugs of opioid peptides J Med Chem 49 4 2006 1261 1270
207. R.T. Borchardt Optimizing oral absorption of peptides using prodrug strategies J Control Release 62 1999 231 238
208. W. Wang, R.T. Borchardt, and B. Wang Orally active peptidomimetic RGD analogs that are glycoprotein IIb/IIIa antagonists Curr Med Chem 7 4 2000 437 453
209. W. Wang, G. Camenisch, D.C. Sane, H. Zhang, E. Hugger, G.L. Wheeler, R.T. Borchardt, and B. Wang A coumarin-based prodrug strategy to improve the oral absorption of RGD peptidomimetics J Control Release 65 1-2 2000 245 251
210. H.T. He, C.R. Xu, X. Song, and T.J. Siahaan Syntheses of cyclic prodrugs of RGD peptidomimetics with various macrocyclic ring sizes: Evaluation of physicochemical, transport and antithrombic properties J Pept Res 61 6 2003 331 342
211. X. Song, C.R. Xu, H.T. He, and T.J. Siahaan Synthesis of a novel cyclic prodrug of RGD peptidomimetic to improve its cell membrane permeation Bioorg Chem 30 4 2002 285 301
212. X. Song, H.T. He, and T.J. Siahaan Synthesis of cyclic prodrugs of Aggrastat and its analogue with a modified phenylpropionic acid linker Org Lett 4 4 2002 549 552
213. E. Usdin, R.T. Borchardt, and C.R. Creveling Transmethylations 1979 Elsevier North Holland New York
214. E. Usdin, R.T. Borchardt, and C.R. Creveling The biochemistry of S-adenosylmethionine and related compounds 1982 Macmillan Press London, UK
215. R.T. Borchardt, C.R. Creveling, and P.M. Ueland Biological methylation and drug design - Experimental and clinical roles of S-adenosylmethionine 1986 Humana Press Clifton, New Jersey
216. R.T. Borchardt, A. Repta, and V. Stella Directed drug delivery: A multidisciplinary problem 1985 Humana Press Clifton, New Jersey