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Items: 19


Peptide-Cleavable Self-immolative Maytansinoid Antibody-Drug Conjugates Designed To Provide Improved Bystander Killing.

Costoplus JA, Veale KH, Qiu Q, Ponte JF, Lanieri L, Setiady Y, Dong L, Skaletskaya A, Bartle LM, Salomon P, Wu R, Maloney EK, Kovtun YV, Ab O, Lai K, Chari RVJ, Widdison WC.

ACS Med Chem Lett. 2019 Sep 27;10(10):1393-1399. doi: 10.1021/acsmedchemlett.9b00310. eCollection 2019 Oct 10.


Synthesis and Evaluation of Camptothecin Antibody-Drug Conjugates.

Li W, Veale KH, Qiu Q, Sinkevicius KW, Maloney EK, Costoplus JA, Lau J, Evans HL, Setiady Y, Ab O, Abbott SM, Lee J, Wisitpitthaya S, Skaletskaya A, Wang L, Keating TA, Chari RVJ, Widdison WC.

ACS Med Chem Lett. 2019 Sep 6;10(10):1386-1392. doi: 10.1021/acsmedchemlett.9b00301. eCollection 2019 Oct 10.


A Case Study Comparing Heterogeneous Lysine- and Site-Specific Cysteine-Conjugated Maytansinoid Antibody-Drug Conjugates (ADCs) Illustrates the Benefits of Lysine Conjugation.

Yoder NC, Bai C, Tavares D, Widdison WC, Whiteman KR, Wilhelm A, Wilhelm SD, McShea MA, Maloney EK, Ab O, Wang L, Jin S, Erickson HK, Keating TA, Lambert JM.

Mol Pharm. 2019 Sep 3;16(9):3926-3937. doi: 10.1021/acs.molpharmaceut.9b00529. Epub 2019 Jul 31.


Bioanalytical workflow for novel scaffold protein-drug conjugates: quantitation of total Centyrin protein, conjugated Centyrin and free payload for Centyrin-drug conjugate in plasma and tissue samples using liquid chromatography-tandem mass spectrometry.

Shi C, Goldberg S, Lin T, Dudkin V, Widdison W, Harris L, Wilhelm S, Jmeian Y, Davis D, O'Neil K, Weng N, Jian W.

Bioanalysis. 2018 Oct 1;10(20):1651-1665. doi: 10.4155/bio-2018-0201. Epub 2018 Oct 29.


LC/MS/MS Bioanalysis of Protein-Drug Conjugates-The Importance of Incorporating Succinimide Hydrolysis Products.

Shi C, Goldberg S, Lin T, Dudkin V, Widdison W, Harris L, Wilhelm S, Jmeian Y, Davis D, O'Neil K, Weng N, Jian W.

Anal Chem. 2018 Apr 17;90(8):5314-5321. doi: 10.1021/acs.analchem.8b00411. Epub 2018 Apr 3.


A New Triglycyl Peptide Linker for Antibody-Drug Conjugates (ADCs) with Improved Targeted Killing of Cancer Cells.

Singh R, Setiady YY, Ponte J, Kovtun YV, Lai KC, Hong EE, Fishkin N, Dong L, Jones GE, Coccia JA, Lanieri L, Veale K, Costoplus JA, Skaletskaya A, Gabriel R, Salomon P, Wu R, Qiu Q, Erickson HK, Lambert JM, Chari RV, Widdison WC.

Mol Cancer Ther. 2016 Jun;15(6):1311-20. doi: 10.1158/1535-7163.MCT-16-0021. Epub 2016 Mar 29.


Understanding How the Stability of the Thiol-Maleimide Linkage Impacts the Pharmacokinetics of Lysine-Linked Antibody-Maytansinoid Conjugates.

Ponte JF, Sun X, Yoder NC, Fishkin N, Laleau R, Coccia J, Lanieri L, Bogalhas M, Wang L, Wilhelm S, Widdison W, Pinkas J, Keating TA, Chari R, Erickson HK, Lambert JM.

Bioconjug Chem. 2016 Jul 20;27(7):1588-98. doi: 10.1021/acs.bioconjchem.6b00117. Epub 2016 Jun 20.


Development of Anilino-Maytansinoid ADCs that Efficiently Release Cytotoxic Metabolites in Cancer Cells and Induce High Levels of Bystander Killing.

Widdison WC, Ponte JF, Coccia JA, Lanieri L, Setiady Y, Dong L, Skaletskaya A, Hong EE, Wu R, Qiu Q, Singh R, Salomon P, Fishkin N, Harris L, Maloney EK, Kovtun Y, Veale K, Wilhelm SD, Audette CA, Costoplus JA, Chari RV.

Bioconjug Chem. 2015 Nov 18;26(11):2261-78. doi: 10.1021/acs.bioconjchem.5b00430. Epub 2015 Sep 30.


Metabolites of antibody-maytansinoid conjugates: characteristics and in vitro potencies.

Widdison W, Wilhelm S, Veale K, Costoplus J, Jones G, Audette C, Leece B, Bartle L, Kovtun Y, Chari R.

Mol Pharm. 2015 Jun 1;12(6):1762-73. doi: 10.1021/mp5007757. Epub 2015 Apr 8.


Antibody-drug conjugates: an emerging concept in cancer therapy.

Chari RV, Miller ML, Widdison WC.

Angew Chem Int Ed Engl. 2014 Apr 7;53(15):3796-827. doi: 10.1002/anie.201307628. Epub 2014 Feb 20. Review.


Synthesis and evaluation of hydrophilic linkers for antibody-maytansinoid conjugates.

Zhao RY, Wilhelm SD, Audette C, Jones G, Leece BA, Lazar AC, Goldmacher VS, Singh R, Kovtun Y, Widdison WC, Lambert JM, Chari RV.

J Med Chem. 2011 May 26;54(10):3606-23. doi: 10.1021/jm2002958. Epub 2011 May 4.


Disulfide-linked antibody-maytansinoid conjugates: optimization of in vivo activity by varying the steric hindrance at carbon atoms adjacent to the disulfide linkage.

Kellogg BA, Garrett L, Kovtun Y, Lai KC, Leece B, Miller M, Payne G, Steeves R, Whiteman KR, Widdison W, Xie H, Singh R, Chari RV, Lambert JM, Lutz RJ.

Bioconjug Chem. 2011 Apr 20;22(4):717-27. doi: 10.1021/bc100480a. Epub 2011 Mar 22.


Design of antibody-maytansinoid conjugates allows for efficient detoxification via liver metabolism.

Sun X, Widdison W, Mayo M, Wilhelm S, Leece B, Chari R, Singh R, Erickson H.

Bioconjug Chem. 2011 Apr 20;22(4):728-35. doi: 10.1021/bc100498q. Epub 2011 Mar 10.


Maytansine and cellular metabolites of antibody-maytansinoid conjugates strongly suppress microtubule dynamics by binding to microtubules.

Lopus M, Oroudjev E, Wilson L, Wilhelm S, Widdison W, Chari R, Jordan MA.

Mol Cancer Ther. 2010 Oct;9(10):2689-99. doi: 10.1158/1535-7163.MCT-10-0644.


Antibody-maytansinoid conjugates designed to bypass multidrug resistance.

Kovtun YV, Audette CA, Mayo MF, Jones GE, Doherty H, Maloney EK, Erickson HK, Sun X, Wilhelm S, Ab O, Lai KC, Widdison WC, Kellogg B, Johnson H, Pinkas J, Lutz RJ, Singh R, Goldmacher VS, Chari RV.

Cancer Res. 2010 Mar 15;70(6):2528-37. doi: 10.1158/0008-5472.CAN-09-3546. Epub 2010 Mar 2.


Tumor delivery and in vivo processing of disulfide-linked and thioether-linked antibody-maytansinoid conjugates.

Erickson HK, Widdison WC, Mayo MF, Whiteman K, Audette C, Wilhelm SD, Singh R.

Bioconjug Chem. 2010 Jan;21(1):84-92. doi: 10.1021/bc900315y.


Semisynthetic maytansine analogues for the targeted treatment of cancer.

Widdison WC, Wilhelm SD, Cavanagh EE, Whiteman KR, Leece BA, Kovtun Y, Goldmacher VS, Xie H, Steeves RM, Lutz RJ, Zhao R, Wang L, Blättler WA, Chari RV.

J Med Chem. 2006 Jul 13;49(14):4392-408.


Antibody-maytansinoid conjugates are activated in targeted cancer cells by lysosomal degradation and linker-dependent intracellular processing.

Erickson HK, Park PU, Widdison WC, Kovtun YV, Garrett LM, Hoffman K, Lutz RJ, Goldmacher VS, Blättler WA.

Cancer Res. 2006 Apr 15;66(8):4426-33.


Eradication of large colon tumor xenografts by targeted delivery of maytansinoids.

Liu C, Tadayoni BM, Bourret LA, Mattocks KM, Derr SM, Widdison WC, Kedersha NL, Ariniello PD, Goldmacher VS, Lambert JM, Blättler WA, Chari RV.

Proc Natl Acad Sci U S A. 1996 Aug 6;93(16):8618-23.

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