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Items: 34


Exposure-Efficacy Analysis of Antibody-Drug Conjugates Delivering an Excessive Level of Payload to Tissues.

Zhang D, Dragovich PS, Yu SF, Ma Y, Pillow TH, Sadowsky JD, Su D, Wang W, Polson A, Khojasteh SC, Hop CE.

Drug Metab Dispos. 2019 Jul 29. pii: dmd.119.087023. doi: 10.1124/dmd.119.087023. [Epub ahead of print]


Catalytic cleavage of disulfide bonds in small molecules and linkers of antibody- drug conjugates.

Zhang D, Fourie-O'Donohue A, Dragovich PS, Pillow TH, Sadowsky JD, Kozak KR, Cass RT, Liu L, Deng Y, Liu Y, Hop CE, Khojasteh SC.

Drug Metab Dispos. 2019 May 13. pii: dmd.118.086132. doi: 10.1124/dmd.118.086132. [Epub ahead of print]


Carfilzomib Is Not an Appropriate Payload of Antibody-Drug Conjugates Due to Rapid Inactivation by Lysosomal Enzymes.

Ma Y, Dela Cruz-Chuh J, Khojasteh SC, Dragovich PS, Pillow TH, Zhang D.

Drug Metab Dispos. 2019 Aug;47(8):884-889. doi: 10.1124/dmd.119.086595. Epub 2019 May 9.


Antibody-Drug Conjugates Derived from Cytotoxic seco-CBI-Dimer Payloads Are Highly Efficacious in Xenograft Models and Form Protein Adducts In Vivo.

Su D, Chen J, Cosino E, Dela Cruz-Chuh J, Davis H, Del Rosario G, Figueroa I, Goon L, He J, Kamath AV, Kaur S, Kozak KR, Lau J, Lee D, Lee MV, Leipold D, Liu L, Liu P, Lu GL, Nelson C, Ng C, Pillow TH, Polakis P, Polson AG, Rowntree RK, Saad O, Safina B, Stagg NJ, Tercel M, Vandlen R, Vollmar BS, Wai J, Wang T, Wei B, Xu K, Xue J, Xu Z, Yan G, Yao H, Yu SF, Zhang D, Zhong F, Dragovich PS.

Bioconjug Chem. 2019 May 15;30(5):1356-1370. doi: 10.1021/acs.bioconjchem.9b00133. Epub 2019 Apr 22.


Exploration of Pyrrolobenzodiazepine (PBD)-Dimers Containing Disulfide-Based Prodrugs as Payloads for Antibody-Drug Conjugates.

Pei Z, Chen C, Chen J, Cruz-Chuh JD, Delarosa R, Deng Y, Fourie-O'Donohue A, Figueroa I, Guo J, Jin W, Khojasteh SC, Kozak KR, Latifi B, Lee J, Li G, Lin E, Liu L, Lu J, Martin S, Ng C, Nguyen T, Ohri R, Lewis Phillips G, Pillow TH, Rowntree RK, Stagg NJ, Stokoe D, Ulufatu S, Verma VA, Wai J, Wang J, Xu K, Xu Z, Yao H, Yu SF, Zhang D, Dragovich PS.

Mol Pharm. 2018 Sep 4;15(9):3979-3996. doi: 10.1021/acs.molpharmaceut.8b00431. Epub 2018 Aug 6.


Conjugation of Indoles to Antibodies through a Novel Self-Immolating Linker.

Dragovich PS, Blake RA, Chen C, Chen J, Chuh J, den Besten W, Fan F, Fourie A, Hartman SJ, He C, He J, Ingalla ER, Kozak KR, Leong SR, Lu J, Ma Y, Meng L, Nannini M, Oeh J, Ohri R, Lewis Phillips G, Pillow TH, Rowntree RK, Sampath D, Vandlen R, Vollmar B, Wai J, Wertz IE, Xu K, Xu Z, Zhang D.

Chemistry. 2018 Apr 3;24(19):4830-4834. doi: 10.1002/chem.201800859. Epub 2018 Mar 25.


Modulating Antibody-Drug Conjugate Payload Metabolism by Conjugation Site and Linker Modification.

Su D, Kozak KR, Sadowsky J, Yu SF, Fourie-O'Donohue A, Nelson C, Vandlen R, Ohri R, Liu L, Ng C, He J, Davis H, Lau J, Del Rosario G, Cosino E, Cruz-Chuh JD, Ma Y, Zhang D, Darwish M, Cai W, Chen C, Zhou H, Lu J, Liu Y, Kaur S, Xu K, Pillow TH.

Bioconjug Chem. 2018 Apr 18;29(4):1155-1167. doi: 10.1021/acs.bioconjchem.7b00785. Epub 2018 Mar 13.


High-Throughput Cysteine Scanning To Identify Stable Antibody Conjugation Sites for Maleimide- and Disulfide-Based Linkers.

Ohri R, Bhakta S, Fourie-O'Donohue A, Dela Cruz-Chuh J, Tsai SP, Cook R, Wei B, Ng C, Wong AW, Bos AB, Farahi F, Bhakta J, Pillow TH, Raab H, Vandlen R, Polakis P, Liu Y, Erickson H, Junutula JR, Kozak KR.

Bioconjug Chem. 2018 Feb 21;29(2):473-485. doi: 10.1021/acs.bioconjchem.7b00791. Epub 2018 Feb 9.


Immolation of p-Aminobenzyl Ether Linker and Payload Potency and Stability Determine the Cell-Killing Activity of Antibody-Drug Conjugates with Phenol-Containing Payloads.

Zhang D, Le H, Cruz-Chuh JD, Bobba S, Guo J, Staben L, Zhang C, Ma Y, Kozak KR, Lewis Phillips GD, Vollmar BS, Sadowsky JD, Vandlen R, Wei B, Su D, Fan P, Dragovich PS, Khojasteh SC, Hop CECA, Pillow TH.

Bioconjug Chem. 2018 Feb 21;29(2):267-274. doi: 10.1021/acs.bioconjchem.7b00576. Epub 2018 Feb 7.


Intratumoral Payload Concentration Correlates with the Activity of Antibody-Drug Conjugates.

Zhang D, Yu SF, Khojasteh SC, Ma Y, Pillow TH, Sadowsky JD, Su D, Kozak KR, Xu K, Polson AG, Dragovich PS, Hop CECA.

Mol Cancer Ther. 2018 Mar;17(3):677-685. doi: 10.1158/1535-7163.MCT-17-0697. Epub 2018 Jan 18.


Discovery of Peptidomimetic Antibody-Drug Conjugate Linkers with Enhanced Protease Specificity.

Wei B, Gunzner-Toste J, Yao H, Wang T, Wang J, Xu Z, Chen J, Wai J, Nonomiya J, Tsai SP, Chuh J, Kozak KR, Liu Y, Yu SF, Lau J, Li G, Phillips GD, Leipold D, Kamath A, Su D, Xu K, Eigenbrot C, Steinbacher S, Ohri R, Raab H, Staben LR, Zhao G, Flygare JA, Pillow TH, Verma V, Masterson LA, Howard PW, Safina B.

J Med Chem. 2018 Feb 8;61(3):989-1000. doi: 10.1021/acs.jmedchem.7b01430. Epub 2017 Dec 21.


Pyrrolobenzodiazepine Dimer Antibody-Drug Conjugates: Synthesis and Evaluation of Noncleavable Drug-Linkers.

Gregson SJ, Masterson LA, Wei B, Pillow TH, Spencer SD, Kang GD, Yu SF, Raab H, Lau J, Li G, Lewis Phillips GD, Gunzner-Toste J, Safina BS, Ohri R, Darwish M, Kozak KR, Dela Cruz-Chuh J, Polson A, Flygare JA, Howard PW.

J Med Chem. 2017 Dec 14;60(23):9490-9507. doi: 10.1021/acs.jmedchem.7b00736. Epub 2017 Nov 16.


Design, synthesis, and biological evaluation of pyrrolobenzodiazepine-containing hypoxia-activated prodrugs.

Dragovich PS, Broccatelli F, Chen J, Fan P, Le H, Mao W, Pillow TH, Polson AG, Wai J, Xu Z, Yao H, Zhang D.

Bioorg Med Chem Lett. 2017 Dec 1;27(23):5300-5304. doi: 10.1016/j.bmcl.2017.10.023. Epub 2017 Oct 13.


Stabilizing a Tubulysin Antibody-Drug Conjugate To Enable Activity Against Multidrug-Resistant Tumors.

Staben LR, Yu SF, Chen J, Yan G, Xu Z, Del Rosario G, Lau JT, Liu L, Guo J, Zheng B, Cruz-Chuh JD, Lee BC, Ohri R, Cai W, Zhou H, Kozak KR, Xu K, Lewis Phillips GD, Lu J, Wai J, Polson AG, Pillow TH.

ACS Med Chem Lett. 2017 Sep 5;8(10):1037-1041. doi: 10.1021/acsmedchemlett.7b00243. eCollection 2017 Oct 12.


Cathepsin B Is Dispensable for Cellular Processing of Cathepsin B-Cleavable Antibody-Drug Conjugates.

Caculitan NG, Dela Cruz Chuh J, Ma Y, Zhang D, Kozak KR, Liu Y, Pillow TH, Sadowsky J, Cheung TK, Phung Q, Haley B, Lee BC, Akita RW, Sliwkowski MX, Polson AG.

Cancer Res. 2017 Dec 15;77(24):7027-7037. doi: 10.1158/0008-5472.CAN-17-2391. Epub 2017 Oct 18.


Development of Efficient Chemistry to Generate Site-Specific Disulfide-Linked Protein- and Peptide-Payload Conjugates: Application to THIOMAB Antibody-Drug Conjugates.

Sadowsky JD, Pillow TH, Chen J, Fan F, He C, Wang Y, Yan G, Yao H, Xu Z, Martin S, Zhang D, Chu P, Dela Cruz-Chuh J, O'Donohue A, Li G, Del Rosario G, He J, Liu L, Ng C, Su D, Lewis Phillips GD, Kozak KR, Yu SF, Xu K, Leipold D, Wai J.

Bioconjug Chem. 2017 Aug 16;28(8):2086-2098. doi: 10.1021/acs.bioconjchem.7b00258. Epub 2017 Jul 13.


Decoupling stability and release in disulfide bonds with antibody-small molecule conjugates.

Pillow TH, Sadowsky JD, Zhang D, Yu SF, Del Rosario G, Xu K, He J, Bhakta S, Ohri R, Kozak KR, Ha E, Junutula JR, Flygare JA.

Chem Sci. 2017 Jan 1;8(1):366-370. doi: 10.1039/c6sc01831a. Epub 2016 Aug 22.


High-Resolution Accurate-Mass Mass Spectrometry Enabling In-Depth Characterization of in Vivo Biotransformations for Intact Antibody-Drug Conjugates.

He J, Su D, Ng C, Liu L, Yu SF, Pillow TH, Del Rosario G, Darwish M, Lee BC, Ohri R, Zhou H, Wang X, Lu J, Kaur S, Xu K.

Anal Chem. 2017 May 16;89(10):5476-5483. doi: 10.1021/acs.analchem.7b00408. Epub 2017 May 3.


Modulating Therapeutic Activity and Toxicity of Pyrrolobenzodiazepine Antibody-Drug Conjugates with Self-Immolative Disulfide Linkers.

Pillow TH, Schutten M, Yu SF, Ohri R, Sadowsky J, Poon KA, Solis W, Zhong F, Del Rosario G, Go MAT, Lau J, Yee S, He J, Liu L, Ng C, Xu K, Leipold DD, Kamath AV, Zhang D, Masterson L, Gregson SJ, Howard PW, Fang F, Chen J, Gunzner-Toste J, Kozak KK, Spencer S, Polakis P, Polson AG, Flygare JA, Junutula JR.

Mol Cancer Ther. 2017 May;16(5):871-878. doi: 10.1158/1535-7163.MCT-16-0641. Epub 2017 Feb 21.


Novel linkers and connections for antibody-drug conjugates to treat cancer and infectious disease.

Pillow TH.

Pharm Pat Anal. 2017 Jan;6(1):25-33. doi: 10.4155/ppa-2016-0032. Epub 2017 Feb 3.


Linker Immolation Determines Cell Killing Activity of Disulfide-Linked Pyrrolobenzodiazepine Antibody-Drug Conjugates.

Zhang D, Pillow TH, Ma Y, Cruz-Chuh JD, Kozak KR, Sadowsky JD, Lewis Phillips GD, Guo J, Darwish M, Fan P, Chen J, He C, Wang T, Yao H, Xu Z, Chen J, Wai J, Pei Z, Hop CE, Khojasteh SC, Dragovich PS.

ACS Med Chem Lett. 2016 Aug 26;7(11):988-993. eCollection 2016 Nov 10.


Targeted drug delivery through the traceless release of tertiary and heteroaryl amines from antibody-drug conjugates.

Staben LR, Koenig SG, Lehar SM, Vandlen R, Zhang D, Chuh J, Yu SF, Ng C, Guo J, Liu Y, Fourie-O'Donohue A, Go M, Linghu X, Segraves NL, Wang T, Chen J, Wei B, Phillips GD, Xu K, Kozak KR, Mariathasan S, Flygare JA, Pillow TH.

Nat Chem. 2016 Dec;8(12):1112-1119. doi: 10.1038/nchem.2635. Epub 2016 Oct 17.


Analogues of DNA minor groove cross-linking agents incorporating aminoCBI, an amino derivative of the duocarmycins: Synthesis, cytotoxicity, and potential as payloads for antibody-drug conjugates.

Giddens AC, Lee HH, Lu GL, Miller CK, Guo J, Lewis Phillips GD, Pillow TH, Tercel M.

Bioorg Med Chem. 2016 Nov 15;24(22):6075-6081. doi: 10.1016/j.bmc.2016.09.068. Epub 2016 Sep 30.


Antibody Drug Conjugates Differentiate Uptake and DNA Alkylation of Pyrrolobenzodiazepines in Tumors from Organs of Xenograft Mice.

Ma Y, Khojasteh SC, Hop CE, Erickson HK, Polson A, Pillow TH, Yu SF, Wang H, Dragovich PS, Zhang D.

Drug Metab Dispos. 2016 Dec;44(12):1958-1962. Epub 2016 Sep 28.


Chemical Structure and Concentration of Intratumor Catabolites Determine Efficacy of Antibody Drug Conjugates.

Zhang D, Yu SF, Ma Y, Xu K, Dragovich PS, Pillow TH, Liu L, Del Rosario G, He J, Pei Z, Sadowsky JD, Erickson HK, Hop CE, Khojasteh SC.

Drug Metab Dispos. 2016 Sep;44(9):1517-23. doi: 10.1124/dmd.116.070631. Epub 2016 Jul 14.


The cryptophycins as potent payloads for antibody drug conjugates.

Verma VA, Pillow TH, DePalatis L, Li G, Phillips GL, Polson AG, Raab HE, Spencer S, Zheng B.

Bioorg Med Chem Lett. 2015 Feb 15;25(4):864-8. doi: 10.1016/j.bmcl.2014.12.070. Epub 2015 Jan 2.


Site-specific trastuzumab maytansinoid antibody-drug conjugates with improved therapeutic activity through linker and antibody engineering.

Pillow TH, Tien J, Parsons-Reponte KL, Bhakta S, Li H, Staben LR, Li G, Chuh J, Fourie-O'Donohue A, Darwish M, Yip V, Liu L, Leipold DD, Su D, Wu E, Spencer SD, Shen BQ, Xu K, Kozak KR, Raab H, Vandlen R, Lewis Phillips GD, Scheller RH, Polakis P, Sliwkowski MX, Flygare JA, Junutula JR.

J Med Chem. 2014 Oct 9;57(19):7890-9. doi: 10.1021/jm500552c. Epub 2014 Sep 18.


Antibody-drug conjugates for the treatment of cancer.

Flygare JA, Pillow TH, Aristoff P.

Chem Biol Drug Des. 2013 Jan;81(1):113-21. doi: 10.1111/cbdd.12085. Review.


Taxol-oligoarginine conjugates overcome drug resistance in-vitro in human ovarian carcinoma.

Wender PA, Galliher WC, Bhat NM, Pillow TH, Bieber MM, Teng NN.

Gynecol Oncol. 2012 Jul;126(1):118-23. doi: 10.1016/j.ygyno.2012.03.049. Epub 2012 Apr 6.


Overcoming multidrug resistance of small-molecule therapeutics through conjugation with releasable octaarginine transporters.

Dubikovskaya EA, Thorne SH, Pillow TH, Contag CH, Wender PA.

Proc Natl Acad Sci U S A. 2008 Aug 26;105(34):12128-33. doi: 10.1073/pnas.0805374105. Epub 2008 Aug 19.


The design of guanidinium-rich transporters and their internalization mechanisms.

Wender PA, Galliher WC, Goun EA, Jones LR, Pillow TH.

Adv Drug Deliv Rev. 2008 Mar 1;60(4-5):452-72. doi: 10.1016/j.addr.2007.10.016. Epub 2007 Nov 9. Review.


Function-oriented synthesis, step economy, and drug design.

Wender PA, Verma VA, Paxton TJ, Pillow TH.

Acc Chem Res. 2008 Jan;41(1):40-9. Epub 2007 Dec 27. Review.


Real-time analysis of uptake and bioactivatable cleavage of luciferin-transporter conjugates in transgenic reporter mice.

Wender PA, Goun EA, Jones LR, Pillow TH, Rothbard JB, Shinde R, Contag CH.

Proc Natl Acad Sci U S A. 2007 Jun 19;104(25):10340-5. Epub 2007 Jun 11.


Molecular transporters: synthesis of oligoguanidinium transporters and their application to drug delivery and real-time imaging.

Goun EA, Pillow TH, Jones LR, Rothbard JB, Wender PA.

Chembiochem. 2006 Oct;7(10):1497-515. Review. No abstract available.


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