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Potentiation of PBD Dimers by Lipophilicity Manipulation

Author(s):

Thaїs Cailleau*, Lauren R. Adams , Neha Arora , Gyoung-Dong Kang, Luke Masterson, Neki Patel, John A. Hartley, Shenlan Mao, Jay Harper and Philip W. Howard   Pages 1 - 11 ( 11 )

Abstract:


Pyrrolobenzodiazepine (PBD) dimers are highly potent DNA cross linking agents used as warheads in Antibody Drug Conjugates (ADCs) for cancer therapy. We propose to investigate the correlation existing between the lipophilicity of those molecules and their activity (both in vitro and in vivo) as well as any effect observed during conjugation.

Keywords:

ADC, Pyrrolobenzodiazepine, P-gp pump, Tesirine, N-Methylpiperazine, Amide coupling, Cathepsin B.

Affiliation:

Spirogen-Medimmune, Queen Mary BioEnterprises Innovation Centre, 42 New road, Whitechapel, London E1 2AX, Spirogen-Medimmune, Queen Mary BioEnterprises Innovation Centre, 42 New road, Whitechapel, London E1 2AX, Spirogen-Medimmune, Queen Mary BioEnterprises Innovation Centre, 42 New road, Whitechapel, London E1 2AX, Spirogen-Medimmune, Queen Mary BioEnterprises Innovation Centre, 42 New road, Whitechapel, London E1 2AX, Spirogen-Medimmune, Queen Mary BioEnterprises Innovation Centre, 42 New road, Whitechapel, London E1 2AX, Spirogen-Medimmune, Queen Mary BioEnterprises Innovation Centre, 42 New road, Whitechapel, London E1 2AX, Spirogen-Medimmune, Queen Mary BioEnterprises Innovation Centre, 42 New road, Whitechapel, London E1 2AX, Oncology Research, MedImmune, LLC, Gaithersburg, Maryland, Oncology Research, MedImmune, LLC, Gaithersburg, Maryland, Spirogen-Medimmune, Queen Mary BioEnterprises Innovation Centre, 42 New road, Whitechapel, London E1 2AX



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