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Pre-clinical pharmacology and mechanism of action of SG3199, the pyrrolobenzodiazepine (PBD) dimer warhead component of antibody-drug conjugate (ADC) payload tesirine
Hartley, John A., Flynn, Michael J., Bingham, John P., Corbett, Simon, Reinert, Halla, Tiberghien, Arnaud, Masterson, Luke A., Antonow, Dyeison, Adams, Lauren, Chowdhury, Sajidah, Williams, David G., Mao, Shenlan, Harper, Jay, Havenith, Carin E. G., Zammarchi, Francesca, Chivers, Simon, van Berkel, Patrick H., Howard, Philip W.
Published in Scientific reports (11.07.2018)
Published in Scientific reports (11.07.2018)
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Design and Synthesis of Tesirine, a Clinical Antibody–Drug Conjugate Pyrrolobenzodiazepine Dimer Payload
Tiberghien, Arnaud C, Levy, Jean-Noel, Masterson, Luke A, Patel, Neki V, Adams, Lauren R, Corbett, Simon, Williams, David G, Hartley, John A, Howard, Philip W
Published in ACS medicinal chemistry letters (10.11.2016)
Published in ACS medicinal chemistry letters (10.11.2016)
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ADCT-301, a Pyrrolobenzodiazepine (PBD) Dimer–Containing Antibody–Drug Conjugate (ADC) Targeting CD25-Expressing Hematological Malignancies
Flynn, Michael J., Zammarchi, Francesca, Tyrer, Peter C., Akarca, Ayse U., Janghra, Narinder, Britten, Charles E., Havenith, Carin E.G., Levy, Jean-Noel, Tiberghien, Arnaud, Masterson, Luke A., Barry, Conor, D'Hooge, Francois, Marafioti, Teresa, Parren, Paul W.H.I., Williams, David G., Howard, Philip W., van Berkel, Patrick H., Hartley, John A.
Published in Molecular cancer therapeutics (01.11.2016)
Published in Molecular cancer therapeutics (01.11.2016)
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Design, Synthesis, and Biophysical and Biological Evaluation of a Series of Pyrrolobenzodiazepine−Poly(N-methylpyrrole) Conjugates
Wells, Geoff, Martin, Christopher R. H, Howard, Philip W, Sands, Zara A, Laughton, Charles A, Tiberghien, Arnaud, Woo, Chi Kit, Masterson, Luke A, Stephenson, Marissa J, Hartley, John A, Jenkins, Terence C, Shnyder, Steven D, Loadman, Paul M, Waring, Michael J, Thurston, David E
Published in Journal of medicinal chemistry (07.09.2006)
Published in Journal of medicinal chemistry (07.09.2006)
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Resistance to Pyrrolobenzodiazepine Dimers Is Associated with SLFN11 Downregulation and Can Be Reversed through Inhibition of ATR
Mao, Shenlan, Chaerkady, Raghothama, Yu, Wen, D’Angelo, Gina, Garcia, Andrew, Chen, Hong, Barrett, Allison M., Phipps, Sandrina, Fleming, Ryan, Hess, Sonja, Koopmann, Jens-Oliver, Dimasi, Nazzareno, Wilson, Susan, Pugh, Kathryn, Cook, Kimberly, Masterson, Luke A., Gao, Changshou, Wu, Herren, Herbst, Ronald, Howard, Philip W., Tice, David A., Cobbold, Mark, Harper, Jay
Published in Molecular cancer therapeutics (01.03.2021)
Published in Molecular cancer therapeutics (01.03.2021)
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Efficacy, Tolerability, and Pharmacokinetic Studies of Antibody–Drug Conjugates Containing a Low-Potency Pyrrolobenzodiazepine Dimer
Gregson, Stephen J., Pugh, Kathryn, Patel, Neki, Afif-Rider, Shameen, Vijayakrishnan, Balakumar, Santos, Kathleen, Riedl, Jitka, Hutchinson, Ian, Kang, Gyoung-Dong, Chooi, K. Phin, Beard, Rhiannon, Adams, Lauren, Barry, Conor S., Ball, Kathryn, Masterson, Luke A., McFarlane, Mary, Hartley, John A., Howard, Philip W.
Published in Molecular cancer therapeutics (06.09.2022)
Published in Molecular cancer therapeutics (06.09.2022)
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Discovery of Peptidomimetic Antibody–Drug Conjugate Linkers with Enhanced Protease Specificity
Wei, BinQing, Gunzner-Toste, Janet, Yao, Hui, Wang, Tao, Wang, Jing, Xu, Zijin, Chen, Jinhua, Wai, John, Nonomiya, Jim, Tsai, Siao Ping, Chuh, Josefa, Kozak, Katherine R, Liu, Yichin, Yu, Shang-Fan, Lau, Jeff, Li, Guangmin, Phillips, Gail D, Leipold, Doug, Kamath, Amrita, Su, Dian, Xu, Keyang, Eigenbrot, Charles, Steinbacher, Stefan, Ohri, Rachana, Raab, Helga, Staben, Leanna R, Zhao, Guiling, Flygare, John A, Pillow, Thomas H, Verma, Vishal, Masterson, Luke A, Howard, Philip W, Safina, Brian
Published in Journal of medicinal chemistry (08.02.2018)
Published in Journal of medicinal chemistry (08.02.2018)
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Synthesis and evaluation of pyrrolobenzodiazepine dimer antibody-drug conjugates with dual β-glucuronide and dipeptide triggers
Gregson, Stephen J., Barrett, Allison M., Patel, Neki V., Kang, Gyoung-Dong, Schiavone, Davide, Sult, Erin, Barry, Conor S., Vijayakrishnan, Balakumar, Adams, Lauren R., Masterson, Luke A., D'Hooge, Francois, Snaith, Mike, Harper, Jay, Hartley, John A., Howard, Philip W.
Published in European journal of medicinal chemistry (01.10.2019)
Published in European journal of medicinal chemistry (01.10.2019)
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Pyrrolobenzodiazepine Dimer Antibody–Drug Conjugates: Synthesis and Evaluation of Noncleavable Drug-Linkers
Gregson, Stephen J., Masterson, Luke A., Wei, Binqing, Pillow, Thomas H., Spencer, Susan D., Kang, Gyoung-Dong, Yu, Shang-Fan, Raab, Helga, Lau, Jeffrey, Li, Guangmin, Lewis Phillips, Gail D., Gunzner-Toste, Janet, Safina, Brian S., Ohri, Rachana, Darwish, Martine, Kozak, Katherine R., dela Cruz-Chuh, Josefa, Polson, Andrew, Flygare, John A., Howard, Philip W.
Published in Journal of medicinal chemistry (14.12.2017)
Published in Journal of medicinal chemistry (14.12.2017)
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An optimised synthesis of SG3376, a non-cleavable antibody-drug conjugate pyrrolobenzodiazepine drug-linker
Tiberghien, Arnaud C., Gregson, Stephen J., Masterson, Luke A., Levy, Jean-Noel, Kemp, Gary C., Adams, Lauren R., Patel, Neki V., Howard, Philip W.
Published in Tetrahedron letters (15.11.2017)
Published in Tetrahedron letters (15.11.2017)
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SG2285, a Novel C2-Aryl-Substituted Pyrrolobenzodiazepine Dimer Prodrug That Cross-links DNA and Exerts Highly Potent Antitumor Activity
Hartley, John A., Hamaguchi, Anzu, Coffils, Marissa, Martin, Christopher R.H., Suggitt, Marie, Chen, Zhizhi, Gregson, Stephen J., Masterson, Luke A., Tiberghien, Arnaud C., Hartley, Janet M., Pepper, Christopher, Lin, Thet Thet, Fegan, Christopher, Thurston, David E., Howard, Philip W.
Published in Cancer research (Chicago, Ill.) (01.09.2010)
Published in Cancer research (Chicago, Ill.) (01.09.2010)
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Synthesis of a novel C2/C2′-aryl-substituted pyrrolo[2,1- c][1,4]benzodiazepine dimer prodrug with improved water solubility and reduced DNA reaction rate
Howard, Philip W., Chen, Zhizhi, Gregson, Stephen J., Masterson, Luke A., Tiberghien, Arnaud C., Cooper, Nectaroula, Fang, Min, Coffils, Marissa J., Klee, Sarah, Hartley, John A., Thurston, David E.
Published in Bioorganic & medicinal chemistry letters (15.11.2009)
Published in Bioorganic & medicinal chemistry letters (15.11.2009)
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Synthesis and biological evaluation of novel pyrrolo[2,1- c][1,4]benzodiazepine prodrugs for use in antibody-directed enzyme prodrug therapy
Masterson, Luke A., Spanswick, Victoria J., Hartley, John A., Begent, Richard H., Howard, Philip W., Thurston, David E.
Published in Bioorganic & medicinal chemistry letters (15.01.2006)
Published in Bioorganic & medicinal chemistry letters (15.01.2006)
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Synthesis and biological evaluation of pyrrolo[2,1- c ][1,4]benzodiazepine (PBD) C8 cyclic amine conjugates
Masterson, Luke A., Croker, Stephen J., Jenkins, Terence C., Howard, Philip W., Thurston, David E.
Published in Bioorganic & medicinal chemistry letters (23.02.2004)
Published in Bioorganic & medicinal chemistry letters (23.02.2004)
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Pre-Clinical Activity of Adct-301, a Novel Pyrrolobenzodiazepine (PBD) Dimer-Containing Antibody Drug Conjugate (ADC) Targeting CD25-Expressing Hematological Malignancies
Flynn, Michael J, van Berkel, Patrick, Zammarchi, Francesca, Levy, Jean-Noel, Tiberghien, Arnaud, Masterson, Luke A, D’Hooge, François, Adams, Lauren, Williams, David G, Howard, Philip W, Hartley, John A
Published in Blood (06.12.2014)
Published in Blood (06.12.2014)
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Approaches to Short-Acting Neuromuscular Blocking Agents: Nonsymmetrical Bis-tetrahydroisoquinolinium Mono- and Diesters
Dhar, Nirmal C, Maehr, Robert B, Masterson, Luke A, Midgley, John M, Stenlake, John B, Wastila, William B
Published in Journal of medicinal chemistry (19.01.1996)
Published in Journal of medicinal chemistry (19.01.1996)
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SG2285, a novel C2-aryl-substituted pyrrolobenzodiazepine dimer pro-drug that cross-links DNA and exerts highly potent antitumor activity
Hartley, John A., Hamaguchi, Anzu, Coffils, Marissa, Martin, Christopher R.H., Suggitt, Marie, Chen, Zhizhi, Gregson, Stephen J., Masterson, Luke A., Tiberghien, Arnaud C., Hartley, Janet M., Pepper, Christopher, Lin, Thet Thet, Fegan, Christopher, Thurston, David E., Howard, Philip W.
Published in Cancer research (Chicago, Ill.) (26.07.2010)
Published in Cancer research (Chicago, Ill.) (26.07.2010)
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Synthesis of a novel C2/C2'-aryl-substituted pyrrolo2,1-c1,4benzodiazepine dimer prodrug with improved water solubility and reduced DNA reaction rate
Howard, Philip W, Chen, Zhizhi, Gregson, Stephen J, Masterson, Luke A, Tiberghien, Arnaud C, Cooper, Nectaroula, Fang, Min, Coffils, Marissa J, Klee, Sarah, Hartley, John A, Thurston, David E
Published in Bioorganic & medicinal chemistry letters (15.11.2009)
Published in Bioorganic & medicinal chemistry letters (15.11.2009)
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Synthesis and biological evaluation of novel pyrrolo2,1-c1,4benzodiazepine prodrugs for use in antibody-directed enzyme prodrug therapy
Masterson, Luke A, Spanswick, Victoria J, Hartley, John A, Begent, Richard H, Howard, Philip W, Thurston, David E
Published in Bioorganic & medicinal chemistry letters (15.01.2006)
Published in Bioorganic & medicinal chemistry letters (15.01.2006)
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