Tumor Targeting and Prodrug Lab

Antibody-targeted Enzyme Activation of Prodrugs

 
 

You can read the abstracts of most of these publications by clicking on the name of the first author.   

Index

Reviews
Carboxypeptidase G2
Beta-lactamase
Penicillin V-amidase
Cytosine Deaminase
Nitroreductase
Alkaline Phosphatase
beta-glucuronidase
Carboxypeptidase A
beta-galactosidase
catalytic antibodies
Others

Reviews

Rihova-B. Targeting of drugs to cell surface receptors. Crit-Rev-Biotechnol. 1997; 17(2): 149-69

Melton-RG; Sherwood-RF. Antibody-enzyme conjugates for cancer therapy. J-Natl-Cancer-Inst. 1996 Feb 21; 88(3-4): 153-65

Baxter-LT; Jain-RK. Pharmacokinetic analysis of the microscopic distribution of enzyme-conjugated antibodies and prodrugs: comparison with experimental data. Br-J-Cancer. 1996 Feb; 73(4): 447-56

Melton-RG; Sherwood-RF. Antibody-enzyme conjugates for cancer therapy. Centre for Applied Microbiology and Research, Porton Down, Salisbury, UK. J-Natl-Cancer-Inst. 1996 Feb 21; 88(3-4): 153-65

Bagshawe-KD. Antibody-directed enzyme prodrug therapy for cancer: its theoretical basis and application. Mol-Med-Today. 1995 Dec; 1(9): 424-31

Connors-TA; Knox-RJ. Prodrugs in cancer chemotherapy. Stem-Cells-Dayt. 1995 Sep; 13(5): 501-11

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Springer-CJ; Niculescu-Duvaz-I. Antibody-directed enzyme prodrug therapy (ADEPT) with mustard prodrugs. Anticancer-Drug-Des. 1995 Jul; 10(5): 361-72

Bagshawe-KD. ADEPT and related concepts. Cell-Biophys. 1994; 24-25: 83-91

Bagshawe-KD; Sharma-SK; Springer-CJ; Rogers-GT. Antibody directed enzyme prodrug therapy (ADEPT). A review of some theoretical, experimental and clinical aspects. Ann-Oncol. 1994 Dec; 5(10): 879-91

Carboxypeptidase G2

Stribbling-SM; Martin-J; Pedley-RB; Boden-JA; Sharma-SK; Springer-CJ. Biodistribution of an antibody-enzyme conjugate for antibody-directed enzyme prodrug therapy in nude mice bearing a human colon adenocarcinoma xenograft. Cancer-Chemother-Pharmacol. 1997; 40(4): 277-84

Martin-J; Stribbling-SM; Poon-GK; Begent-RH; Napier-M; Sharma-SK; Springer-CJ. Antibody-directed enzyme prodrug therapy: pharmacokinetics and plasma levels of prodrug and drug in a phase I clinical trial. Cancer-Chemother-Pharmacol. 1997; 40(3): 189-201

Rowsell-S; Pauptit-RA; Tucker-AD; Melton-RG; Blow-DM; Brick-P. Crystal structure of carboxypeptidase G2, a bacterial enzyme with applications in cancer therapy. Structure. 1997 Mar 15; 5(3): 337-47

Springer-CJ; Bavetsias-V; Jackman-AL; Boyle-FT; Marshall-D; Pedley-RB; Bisset-GM. Prodrugs of thymidylate synthase inhibitors: potential for antibody directed enzyme prodrug therapy (ADEPT). Anticancer-Drug-Des. 1996 Dec; 11(8): 625-36

Blakey-DC; Burke-PJ; Davies-DH; Dowell-RI; East-SJ; Eckersley-KP; Fitton-JE; McDaid-J; Melton-RG; Niculescu-Duvaz-IA; Pinder-PE; Sharma-SK; Wright-AF; Springer-CJ ZD2767, an improved system for antibody-directed enzyme prodrug therapy that results in tumor regressions in colorectal tumor xenografts. Cancer-Res. 1996 Jul 15; 56(14): 3287-92

Bagshawe-KD; Sharma-SK. Cyclosporine delays host immune response to antibody enzyme conjugate in ADEPT. Transplant-Proc. 1996 Dec; 28(6): 3156-8

Sharma-SK; Bagshawe-KD; Melton-RG; Begent-RH. Effect of cyclosporine on immunogenicity of a bacterial enzyme carboxypeptidase G2 in ADEPT. Transplant-Proc. 1996 Dec; 28(6): 3154-5

Dowell-RI; Springer-CJ; Davies-DH; Hadley-EM; Burke-PJ; Boyle-FT; Melton-RG; Connors-TA; Blakey-DC; Mauger-AB. New mustard prodrugs for antibody-directed enzyme prodrug therapy: alternatives to the amide link. J-Med-Chem. 1996 Mar 1; 39(5): 1100-5

Blakey-DC; Davies-DH; Dowell-RI; East-SJ; Burke-PJ; Sharma-SK; Springer-CJ; Mauger-AB; Melton-RG. Anti-tumour effects of an antibody-carboxypeptidase G2 conjugate in combination with phenol mustard prodrugs. Br-J-Cancer. 1995 Nov; 72(5): 1083-8

Rogers-GT; Burke-PJ; Sharma-SK; Koodie-R; Boden-JA. Plasma clearance of an antibody--enzyme conjugate in ADEPT by monoclonal anti-enzyme: its effect on prodrug activation in vivo. Br-J-Cancer. 1995 Dec; 72(6): 1357-63.

Springer-CJ; Dowell-R; Burke-PJ; Hadley-E; Davis-DH; Blakey-DC; Melton-RG; Niculescu-Duvaz-I. Optimization of alkylating agent prodrugs derived from phenol and aniline mustards: a new clinical candidate prodrug (ZD2767) for antibody-directed enzyme prodrug therapy (ADEPT). J-Med-Chem. 1995 Dec 22; 38(26): 5051-65

Springer-CJ; Poon-GK; Sharma-SK; Bagshawe-KD. Analysis of antibody-enzyme conjugate clearance by investigation of prodrug and active drug in an ADEPT clinical study. Cell-Biophys. 1994; 24-25: 193-207

Werlen-RC; Lankinen-M; Rose-K; Blakey-D; Shuttleworth-H; Melton-R; Offord-RE. Site-specific conjugation of an enzyme and an antibody fragment. Bioconjug-Chem. 1994 Sep-Oct; 5(5): 411-7

Sharma-SK; Boden-JA; Springer-CJ; Burke-PJ; Bagshawe-KD. Antibody-directed enzyme prodrug therapy (ADEPT). A three-phase study in ovarian tumor xenografts. Cell-Biophys. 1994; 24-25: 219-28

Sharma, S. K.; Bagshawe, K. D.; Melton, R. G.; Sherwood, R. F. Human Immune Response to Monoclonal Antibody-Enzyme Conjugates in ADEPT Pilot Clinical Trial. Cell Biophys. 1992, 21, 109-120.

Bagshawe, K. D.; Sharma, S. K.; Springer, C. J.; Antoniw, P.; Rogers, G. T.; Burke, P. J.; Melton, R.; Sherwood, R. Antibody-Enzyme Conjugates Can Generate Cytotoxic Drugs from Inactive Precursors at Tumor Sites. Antibody Immunoconj. Radiopharm. 1991, 4, 915-922.

Springer, C. J.; Bagshawe, K. D.; Sharma, S. K.; Searle, F.; Boden, J. A.; Antoniw, P.; Burke, P. J.; Rogers, G. T.; Sherwood, R. F.; Melton, R. G. Ablation of Human Choriocarcinoma Xenografts by Antibody-directed Enzyme Prodrug Therapy (ADEPT) with Three Novel Compounds. Eur. J. Cancer 1991, 27, 1361-1366.

Sharma, S. K.; Bagshawe, K.D.; Springer, C.J.; Burke, P.J.; Rogers, G.T.; Boden, J.A.; Antoniw, P.; Melton, R.G.; Sherwood, R.F. Antibody-Directed Enzyme Prodrug Therapy (ADEPT): A Three Phase System. Dis. Markers 1991, 9, 225-231.

Springer, C.J.; Antoniw, P.; Bagshawe, K.D. The Activation by Endogenous Enzymes of a Prodrug Designed for Use in Antibody-Directed Prodrug Therapy. in Monoclonal Antibodies-Applications in Clinical Oncology; Epenetos, A.A. Ed.; Chapman and Hall:London, 1991; pp 185-191.

Springer, C. J.; Antoniw, P.; Bagshawe, K. D.; Wilman, D. E. V. Comparison of Half-lives and Cytotoxicity of N-Chloroethyl-4-amino and N-Mesyloxyethyl-benzoyl Coumpounds, Products of Prodrugs in Antibody-directed Enzyme Prodrug Therapy (ADEPT). Anti-Cancer Drug Design 1991, 6, 467-479.

Melton, R. G.; Searle, F.; Sherwood, R. F.; Bagshawe, K. D.; Boden, J. A. The Potential of Carboxypeptidase G2:Antibody Conjugates as Anti-Tumour Agents. II. In Vivo Localising and Clearance properties in a Choriocarcinoma Model. Br. J. Cancer 1990, 61, 420-424.

Springer, C. J.; Antoniw, P.; Bagshawe, K. D.; Searle, F.; Bisset, G. M. F.; Jarman, M. Novel Prodrugs Which are Activated to Cytotoxic Alkylating Agents by Carboxypeptidase G2. J. Med. Chem. 1990, 33, 677-681.

Antoniw, P.; Springer, C. J.; Bagshawe, K. D.; Searle, F.; Melton, R. G.; Rogers, G. T.; Burke, P. J.; Sherwood, R. F. Disposition of the Prodrug 4-(bis(2-Chloroethyl) Amino) Benzoyl-L-Glutamic Acid and its Active Parent Drug in Mice. Br. J. Cancer 1990, 62, 909-914.

Sharma, S. K.; Bagshawe, K. D.; Burke, P. J.; Boden, R. W.; Rogers, G. T. Inactivation and Clearance of an Anti-CEA Carboxypeptidase G2 Conjugate in Blood after Localization in a Xenograft Model. Br. J. Cancer 1990, 61, 659-662.

Bagshawe, K. D.; Springer, C. J.; Searle, F.; Antoniw, P.; Sharma, S.; Melton, R. G.; Sherwood, R. F. A Cytotoxic Agent Can be Generated Selectively at Cancer Sites. Br. J. Cancer 1988, 58, 700-703.

Sherwood, R. F.; Melton, R. G.; Alwan, S. M.; Hughes, P. Purification and Properties of Carboxypeptidase G2 from Pseudomonas sp. strain RS-16. Use of a Novel Triazine Dye Affinity Method. Eur. J. Biochem. 1985, 148, 447-453.

Minton, N. P.; Atkinson, T.; Sherwood, R. F. Molecular cloning of the Pseudomonas Carboxypeptidase G2 Gene and Its Expression in Escherichia coli and Pseudomonas putida. J. Bacteriol. 1983, 156, 1222-12227.

Kalghatgi, K. K.; Bertino, J. R. Folate-Degrading Enzymes: A Review with Special Emphasis on Carboxypeptidase G. in Enzymes as Drugs; Molcenberg, J. S.; Roberts, J. Eds.; John Wiley and Sons, Inc.: New York, 1981; pp 77-102.

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Beta-lactamase

Siemers-NO; Kerr-DE; Yarnold-S; Stebbins-MR; Vrudhula-VM; Hellstrom-I; Hellstrom-KE; Senter-PD. Construction, expression, and activities of L49-sFv-beta-lactamase, a single-chain antibody fusion protein for anticancer prodrug activation. Bioconjug-Chem. 1997 Jul-Aug; 8(4): 510-9

Vrudhula-VM; Svensson-HP; Senter-PD. Immunologically specific activation of a cephalosporin derivative of mitomycin C by monoclonal antibody beta-lactamase conjugates. J-Med-Chem. 1997 Aug 15; 40(17): 2788-92

Rodrigues-ML; Carter-P; Wirth-C; Mullins-S; Lee-A; Blackburn-BK. Synthesis and beta-lactamase-mediated activation of a cephalosporin-taxol prodrug. Chem-Biol. 1995 Apr; 2(4): 223-7

Brison, O. Gene Amplification and Tumor Progression. Biochim. Biophys. Acta 1993, 1115, 25-41.

Eccles, S. A.; Court, W. J.; Box, G. A.; Dean, C. J.; Melton, R. G.; Springer, C. J. Regression of Established Breast Carcinoma Xenografts with Antibody-directed Enzyme Prodrug Therapy against c-erbB2 p185. Cancer Res. 1994, 54, 5171-5177.

Eccles, S. A.; Cort, W. J.; Box, G. A.; Dean, C. J.; Melton, R. G.; Springer, C. J. Regression of Established Breast Carcinoma Xenografts with Antibody-Directed Enzyme Prodrug Therapy against c-erbB2 p185. Cancer Res. 1994, 54, 5171-5177.

Goshorn, S. C.; Svensson, H. P.; Kerr, D. E.; Somerville, J. E., Senter, P. D.; Fell, H. P. Genetic Construction, Expression, and Characterization of a Single Chain Anti-Carcinoma Antibody Fused to beta-Lactamase. Cancer Res. 1993, 53, 2123-2127.

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Jungheim, L. N.; Sheperd, T. A.; Meyer, D. L. Synthesis of Acylhydrazido-Substituted Cephems. Design of Cephalosporin-Vinca Alkaloid Prodrugs: Substrates for an Antibody-Targeted Enzyme. J. Org. Chem. 1992, 57, 2334-2340.

Meyer, D. L.; Jungheim, L. N.; Mikolajczyk, S. D.; Shepherd, T. A; Starling, J. J.; Ahlem, C. N. Preparation and Characterization of a beta-Lactamase-Fab' Conjugate for the Site-Specific Activation of Oncolytic Agents. Bioconjugate Chem. 1992, 3, 42-48.

Meyer, D. L.; Jungheim, L. N.; Law, K. L.; Mikolajczyk, S. D.; Shepherd, T. A.; Mackensen, D. G.; Briggs, S. L.; Starling, J. J. Site-specific Prodrug Activation by Antibody-beta-Lactamase Conjugates: Regression and Long-Term Growth Inhibition of Human Colon Carcinoma Xenograft Models. Cancer Res. 1993, 53, 3956-3964.

Rodrigues, M. L.; Presta, L. G.; Kotts, C. E.; Wirth, C.; Mordenti, J., Osaka, G.; Wong, W. L. T.; Blackburn, B; Carter, P. Development of a Humanized Disulfide-stabilized Anti-p185HER2 Fv-beta-Lactamase Fusion Protein for Activation of a Cephalosporin Doxorubicin Prodrug. Cancer Res. 1995, 55, 63-70.

Shepherd, T. A.; Jungheim, L. N.; Meyer, D. L.; Starling, J. J. A Novel Targeted Delivery System Utilizing a Cephalosporin-Oncolytic Prodrug Activated by an Antibody beta-Lactamase Conjugate for the Treatment of Cancer. Bioorg. Med. Chem. Lett. 1991, 1, 21-26.

Svensson, H. P.; Kadow, J. F.; Vrudhula, V. M.; Wallace, P. M.; Senter, P. D. Monoclonal Antibody-b-Lactamase Conjugates for the Activation of a Cephalosporin Mustard Prodrug. Bioconjugate Chem. 1992, 3, 176-181.

Penicillin-V-Amidase

Bignami, G. S.; Senter, P. D.; Grothaus, P. G.; Fischer, K. J.; Humphreys, T.; Wallace, P. M. N-(4'-Hydroxyphenylacetyl)palytoxin: A Palytoxin Prodrug That Can Be Activated by a Monoclonal Antibody-Pennicillin G amidase Conjugate. Cancer Res. 1992, 52, 5759-5764.

Kerr, D. E.; Senter, P. D.; Burnett, W. V.; Hirschberg, D. L.; Hellstrūm, I.; Hellstrūm, K. E. Antibody-Penicillin-V-Amidase Conjugates Kill Antigen-Positive Tumor Cells When Combined with Doxorubicin Phenoxyacetamide. Cancer Immunol. Immunother. 1990, 31, 202-206.

Vrudhula, V. M.; Senter, P. D.; Fischer, K. J.; Wallace, P. M. Prodrugs od Doxorubicin and Melphalan and Their Activation by a Monoclonal Antibody-Penicillin-G Amidase Conjugate. J. Med. Chem. 1993, 36, 919-923.

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Cytosine Deaminase

Kerr, D. E.; Garrigues, U. S.; Wallace, P. M.; Hellstrūm, K. E.; Hellstrūm, I.; Senter, P. D. Application of Monoclonal Antibodies against Cytosine Deaminase for in Vivo Clearance of a Cytosine Deaminase Immunoconjugate. Bioconj. Chem. 1993, 4, 353-357.

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Senter, P. D.; Su, P. C. D.; Katsuragi, T.; Sakai, T.; Cosand, W. L.; Hellstrūm, I.; Hellstrūm, K. E. Generation of 5-Fluorouracil from 5-Fluorocytosine by Monoclonal Antibody-Cytosine Deaminase Conjugates. Bioconjugate Chem. 1991, 2, 447-451.

Wallace, P. M.; MacMaster, J. F.; Smith, V. F., Kerr, D. E.; Senter, P. D.; Cosand, W. L. Intratumoral Generation of 5-Fluorouracil Mediated by an Antibody-Cytosine Deaminase Conjugate in Combination with 5-Fluorocytosine. Cancer Res. 1994, 54, 2719-2723.

Nitroreductase

Siim-BG; Denny-WA; Wilson-WR. Nitro reduction as an electronic switch for bioreductive drug activation. Oncol-Res. 1997; 9(6-7): 357-69

Atwell-GJ; Boyd-M; Palmer-BD; Anderson-RF; Pullen-SM; Wilson-WR; Denny-WA. Synthesis and evaluation of 4-substituted analogues of 5-[N,N-bis (2-chloroethyl)amino]-2-nitrobenzamide as bioreductively activated prodrugs using an Escherichia coli nitroreductase. Anticancer-Drug-Des. 1996 Oct; 11(7): 553-67

Anlezark-GM; Melton-RG; Sherwood-RF; Wilson-WR; Denny-WA; Palmer-BD; Knox-RJ; Friedlos-F; Williams-A. Bioactivation of dinitrobenzamide mustards by an E. coli B nitroreductase. Biochem-Pharmacol. 1995 Aug 25; 50(5): 609-18.

Friedlos, F.; Knox, R. J. Metabolism of NAD(P)H by Blood Components. Relevance to Bioreductively Activated Prodrugs in a Targeted Enzyme Therapy System. Biochem. Pharmacol. 1992, 44, 631-635.

Knox-RJ; Friedlos-F; Jarman-M; Davies-LC; Goddard-P; Anlezark-GM; Melton-RG; Sherwood-RF. Virtual cofactors for an Escherichia coli nitroreductase enzyme: relevance to reductively activated prodrugs in antibody directed enzyme prodrug therapy (ADEPT). Biochem-Pharmacol. 1995 May 26; 49(11): 1641-7

Mauger, A. B.; Burke, P. J.; Somani, H. H.; Friedlos, F.; Knox, R. J. Self-Immolative Prodrugs: Candidates for Antibody-Directed Enzyme Prodrug Therapy in Conjunction with a Nitroreductase Enzyme. J. Med. Chem. 1994, 37, 3452-3458.

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Alkaline Phosphatase

Haisma, H. J.; Boven, E.; van Muijen, M.; De Vries, R.; Pinedo, H. M. Analysis of a Conjugate Between Anti-Carcinoembryonic Antigen Monoclonal Antibody and Alkaline Phosphatase for Specific Activation of the Prodrug Etoposide Phosphate. Cancer Immunol. Immunother. 1992, 34, 343-348.

Sahin, U.; hartmann, F.; Senter, P.; Pohl, C.; Engert, A.; Diehl, V.; Pfreundschuh, M. Specific Activation of the Prodrug Mitomycin Phosphate by a Bispecific Anti-CD30/ Anti-Alkaline Phosphatase Monoclonal Antibody. Cancer Res. 1990, 50, 6944-6948.

Senter, P. D.; Saulnier, M. G.; Schreiber, G. J.; Hirschberg, D. L.; Brown, J. P.; Hellstrūm, I.; Hellstrūm, K. E. Anti-tumor Effects of Antibody-Alkaline Phosphatase Conjugates in Combination with Etoposide Phosphate. Proc. Natl. Acad. Sci., USA 1988, 85, 4842-4846.

Senter, P. D.; Schreiber, G. J.; Hirschberg, D. L.; Ashe, S. A.; Hellstrūm, K. E.; Hellstrūm, I. Enhancement of the in Vitro and in Vivo Antitumor Activities of Phosphorylated Mitomycin C and Etoposide Derivatives by Monoclonal Antibody-Alkaline Phosphatase Conjugates. Cancer Res. 1989, 49, 5789-5792.

Wallace, P. M.; Senter, P. D. In Vitro and in Vivo Activities of Monoclonal Antibody-Alkaline Phospatase Conjugates in Combination with Phenol Mustard Phosphate. Bioconjugate Chem. 1991, 2, 349-352.

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Beta-glucuronidase

Haisma-HJ; Brakenhoff-RH; v.d.-Meulen-Muileman-I; Pinedo-HM; Boven-E. Construction and characterization of a fusion protein of single-chain anti-carcinoma antibody 323/A3 and human beta-glucuronidase. Cancer-Immunol-Immunother. 1998 Jan; 45(5): 266-72

Cheng-TL; Chen-BM; Chan-LY; Wu-PY; Chern-JW; Roffler-SR. Poly(ethylene glycol) modification of beta-glucuronidase-antibody conjugates for solid-tumor therapy by targeted activation of glucuronide prodrugs. Cancer-Immunol-Immunother. 1997 Aug; 44(6): 305-15

Bakina-E; Wu-Z; Rosenblum-M; Farquhar-D. Intensely cytotoxic anthracycline prodrugs: glucuronides. J-Med-Chem. 1997 Dec 5; 40(25): 4013-8

Chen-BM; Chan-LY; Wang-SM; Wu-MF; Chern-JW; Roffler-SR. Cure of malignant ascites and generation of protective immunity by monoclonal antibody-targeted activation of a glucuronide prodrug in rats. Int-J-Cancer. 1997 Nov 4; 73(3): 392-402

de-Bont-DB; Leenders-RG; Haisma-HJ; van-der-Meulen-Muileman-I; Scheeren-HW. Synthesis and biological activity of beta-glucuronyl carbamate-based prodrugs of paclitaxel as potential candidates for ADEPT. Bioorg-Med-Chem. 1997 Feb; 5(2): 405-14

Houba-PH; Boven-E; Haisma-HJ. Improved characteristics of a human beta-glucuronidase-antibody conjugate after deglycosylation for use in antibody-directed enzyme prodrug therapy. Bioconjug-Chem. 1996 Sep-Oct; 7(5): 606-11

Schumacher-U; Adam-E; Zangemeister-Wittke-U; Gossrau-R. Histochemistry of therapeutically relevant enzymes in human tumours transplanted into severe combined immunodeficient (SCID) mice: nitric oxide synthase-associated diaphorase, beta-D-glucuronidase and non-specific alkaline phosphatase. Acta-Histochem. 1996 Nov; 98(4): 381-7

Houba-PH; Leenders-RG; Boven-E; Scheeren-JW; Pinedo-HM; Haisma-HJ. Characterization of novel anthracycline prodrugs activated by human beta-glucuronidase for use in antibody-directed enzyme prodrug therapy. Biochem-Pharmacol. 1996 Aug 9; 52(3): 455-63

Bosslet, K.; Czech, J.; Lorenz, P.; Sedlacek, H. H.; Schuermann, M.; Seemann, G. Molecular and Functional Characterisation of a Fusion Protein Suited for Tumour Specific Prodrug Activation. Br. J. Cancer 1992, 65, 234-238.

Bosslet, K.; Czech, J.; Hoffmann, D. Tumor-selective Prodrug Activation by Fusion Protein-mediated Catalysis. Cancer Res. 1994, 54, 2151-2159.

Gesson, J.-P.; Jacquesy, J.-C.; Mondon, M; Petit, P.; Renoux, B.; Andrianomenjanahary, S.; Dufat-Trinh Van, H.; Koch, M.; Michel, S.; Tillequin, F.; Florent, J.-C.; Monneret, C.; Bosslet, K.; Czech, J.; Hoffmann, D. Prodrugs of Anthracyclines for Chemotherapy via Enzyme-Monoclonal Antibody Conjugates. Anti-Cancer Drug Design 1994, 9, 409-423.

Haisma, H. J.; Boven, E.; van Muijen, M.; de Jong, J.; van der Vijgh, W. J. F.; Pinedo, H. M. A Monoclonal Antibody-beta-Glucuronidase Conjugate as Activator of the Prodrug Epirubicin-Glucuronide for Specific Treatment of Cancer. Br. J. Cancer 1992, 66, 474-478.

Haisma-HJ; van-Muijen-M; Pinedo-HM; Boven-E. Comparison of two anthracycline-based prodrugs for activation by a monoclonal antibody-beta-glucuronidase conjugate in the specific treatment of cancer. Cell-Biophys. 1994; 24-25: 185-92

Roffler, S. R.; Wang, S-M.; Chern, J-W.; Yeh, M-Y.; and Tung, E. Anti-Neoplastic Glucuronide Prodrug Treatment of Human Tumor Cells Targeted with a Monoclonal Antibody-Enzyme Conjugate. Biochem. Pharmacol. 1991, 42, 2062-2065.

Wang, S-M.; Chern, J-W.; Yeh, M-Y.; Ng, J. C.; Tung, E.; Roffler, S. R. Specific Activation of Glucuronide Prodrugs by Antibody-Targeted Enzyme Conjugates for Cancer Therapy. Cancer Res. 1992, 52, 4484-4491.

Vingerhoeds, M. H.; Haisma, H. J.; van Muijen, M.; van de Rijt, R. B. J.; Crommelin, D. J. A.; Storm, G. A New Application for Liposomes in Cancer Therapy. Immunoliposomes Bearing Enzymes (Immuno-Enzymosomes) for Site-Specific Activation of Prodrugs. FEBS Lett. 1993, 3, 485-490.

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Carboxypeptidase A

Smith-GK; Banks-S; Blumenkopf-TA; Cory-M; Humphreys-J; Laethem-RM; Miller-J; Moxham-CP; Mullin-R; Ray-PH; Walton-LM; Wolfe-LA-3rd. Toward antibody-directed enzyme prodrug therapy with the T268G mutant of human carboxypeptidase A1 and novel in vivo stable prodrugs of methotrexate. J-Biol-Chem. 1997 Jun 20; 272(25): 15804-16

Perron-MJ; Page-M. Activation of methotrexate-phenylalanine by monoclonal antibody--carboxypeptidase A conjugate for the specific treatment of ovarian cancer in vitro. Br-J-Cancer. 1996 Feb; 73(3): 281-7

Laethem-RM; Blumenkopf-TA; Cory-M; Elwell-L; Moxham-CP; Ray-PH; Walton-LM; Smith-GK. Expression and characterization of human pancreatic preprocarboxypeptidase A1 and preprocarboxypeptidase A2. Arch-Biochem-Biophys. 1996 Aug 1; 332(1): 8-18

Haenseler, E.; Esswein, A.; Vitols, K. S.; Montejano, Y.; Mueller, B. M.; Reisfeld, R. A.; Huennekens, F. M. Activation of Methotrexate-a-Alanine by Carboxypeptidase A-Monoclonal Antibody Conjugate. Biochem. 1992, 31, 891-897.

Kuefner, U.; Lohrmann, U.; Montejano, Y. D.; Vitols, K. S.; Huennekens, F. M. Carboxypeptidase-Mediated Release of Methotrexate from Methotrexate a-Peptides. Biochem. 1989, 28, 2288-2297.

Perron-MJ; Page-M. Activation of methotrexate-phenylalanine by monoclonal antibody--carboxypeptidase A conjugate for the specific treatment of ovarian cancer in vitro.Br-J-Cancer. 1996 Feb; 73(3): 281-7

Vitols, K. S.; Haenseler, E.; Montejano, Y.; Baer, T.; Huennekens, F. M. Activation of Methotrexate Prodrugs by Enzyme/Monoclonal Antibody Conjugates. Pteridines 1992, 3, 125-126.

Vitols, K. S.; Haag-Zeino, B.; Baer, T.; Montejano, Y. D.; Huennekens, F. M. Methotrexate-a-Phenylalanine: Optimization of Methotrexate Prodrug for Activation by Carboxypeptidase A-Monoclonal Antobody Conjugate. Cancer Res. 1995, 55, 478-481.

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Beta-galactosidase

Abraham-R; Aman-N; von-Borstel-R; Darsley-M; Kamireddy-B; Kenten-J; Morris-G; Titmas-R. Conjugates of COL-1 monoclonal antibody and beta-D-galactosidase can specifically kill tumor cells by generation of 5-fluorouridine from the prodrug beta-D-galactosyl-5-fluorouridine. Cell-Biophys. 1994; 24-25: 127-33

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Catalytic antibodies

Wentworth-P; Datta-A; Blakey-D; Boyle-T; Partridge-LJ; Blackburn-GM Toward antibody-directed "abzyme" prodrug therapy, ADAPT: carbamate prodrug activation by a catalytic antibody and its in vitro application to human tumor cell killing. Proc-Natl-Acad-Sci-U-S-A. 1996; 93(2): 799-803

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Others

Crosasso-P; Brusa-P; Dosio-F; Arpicco-S; Pacchioni-D; Schuber-F; Cattel-L. Antitumoral activity of liposomes and immunoliposomes containing 5-fluorouridine prodrugs. J-Pharm-Sci. 1997 Jul; 86(7): 832-9

Vingerhoeds-MH; Haisma-HJ; Belliot-SO; Smit-RH; Crommelin-DJ; Storm-G. Immunoliposomes as enzyme-carriers (immuno-enzymosomes) for antibody-directed enzyme prodrug therapy (ADEPT): optimization of prodrug activating capacity. Pharm-Res. 1996 Apr; 13(4): 604-10

Blakey-DC; Pinder-PE; Wright-AF. Comparison of the cellular internalization of antibodies used either as immunotoxins or in ADEPT. Cell-Biophys. 1994; 24-25: 175-83

Miyashita, H.; Karaki, Y.; Kikuchi, M.; Fujii, I. Prodrug Activation Via Catalytic Antibodies. Proc. Natl. Acad. Sci. USA 1993, 90, 5337-5340.

Muzykantov, V. R.; Trubetskaya, O. V.; Puchnina, E. A.; Sakharov, D. V.; Domogatsky, S. P. Cytotoxicity of Glucose Oxidase Conjugated With Antibodies to Target Cells: Killing Efficiency Depends on the Conjugate Internalization. Biochim. Biophys. Acta 1990, 1053, 27-31.

Rowlinson-Busza, G.; Bamias, A.; Krausz, T.; Evans, D. J.; Epenetos, A. A. Cytotoxicity Following Specific Activation of Amygdalin. in Monoclonal Antibodies. Applications in Clinical Oncology; Epenetos, A. A., Ed.; Chapman and Hall Medical: London, 1992; pp 179-183

Yuan, F.; Baxter, L. T.; Jain, R. K. Pharmacokinetic Analysis of Two-Step Approaches Using Bifunctional and Enzyme-conjugated Antibodies. Cancer Res. 1991, 51,3119-3130.

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