Cytotoxic payloads for antibody-drug conjugates / edited by David E. Thurston (King's College London, UK) and Paul J.M. Jackson (Femtogenix Ltd, UK)

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Resource type: Ressourcentyp: Buch (Online)Buch (Online)Sprache: Englisch Reihen: RSC drug discovery series ; 71Verlag: Cambridge : Royal Society of Chemistry, [2019]Copyright-Datum: © 2019Beschreibung: 1 Online-RessourceISBN:

9781788018456
9781788012898

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Andere physische Formen: 9781788010771 | Erscheint auch als: Cytotoxic payloads for antibody--drug conjugates. Druck-Ausgabe Cambridge : Royal Society of Chemistry, [2019] | Erscheint auch als: Cytotoxic payloads for antibody-drug conjugates. Druck-Ausgabe. Cambridge : Royal Society of Chemistry, 2019. xxi, 480 SeitenLOC-Klassifikation:

RS201.A56

DOI: DOI: 10.1039/9781788012898Online-Ressourcen:

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Zusammenfassung: Cover; Cytotoxic Payloads for Antibody-Drug Conjugates; Preface; Contents; Chapter 1 -- Introduction to Antibody-Drug Conjugates (ADCs); 1.1 Introduction to Cancer; 1.2 Cancer Treatments; 1.3 Antibody-Drug Conjugates (ADCs); 1.3.1 Mechanism of Action of ADCs; 1.3.2 Antibody Selection; 1.3.3 Linker Design; 1.3.3.1 Cleavable Linkers; 1.3.3.2 Non-cleavable Linkers; 1.3.4 Payload Selection; 1.3.5 Conjugation of Payload; 1.3.5.1 Conjugation via Lysine Residues; 1.3.5.2 Conjugation via Thiol Groups; 1.3.5.3 Site-specific Conjugation; 1.3.5.4 Click Chemistry for ConjugationZusammenfassung: 1.3.5.5 Other Types of Conjugation1.3.6 Analytical Characterisation of ADCs; 1.3.6.1 Drug to Antibody Ratio (DAR); 1.3.6.2 Determination of Unconjugated Payload Content in an ADC; 1.3.6.3 Hydrophobicity Prediction; 1.4 Conclusions; References; Chapter 2 -- Design Factors Important for Antibody-Drug Conjugate (ADC) Payloads; 2.1 Introduction; 2.2 The Challenges in Making Effective ADCs; 2.3 Distribution of ADCs into Tumour Tissue; 2.3.1 Diffusion and Extravasation of ADCs; 2.3.2 Effect of Linker-Payload on ADC Distribution into Tumour TissueZusammenfassung: 2.3.3 The Effect of Target Antigen Density on ADC Distribution2.4 Retention of ADCs by Tumour Tissue; 2.5 Uptake and Metabolism of ADCs by Cancer Cells; 2.5.1 Release of Cytotoxic Payload in Tumour Tissue; 2.5.2 Trafficking and Release of Cytotoxic Payload in Tumour Tissue; 2.5.3 Payload Metabolites and Bystander Killing; 2.6 Design Factors Important for the Safety of ADCs; 2.7 ADCs and the Tumour Microenvironment; 2.8 Summary; Acknowledgements; References; Chapter 3 -- Use of Molecular Modelling Techniques in Antibody-Drug Conjugate (ADC) Payload Discovery and Development; 3.1 IntroductionZusammenfassung: 3.2 Molecular Modelling of MMAE/MMAF Payloads3.3 Molecular Modelling of C8-linked Pyrrolobenzodiazepines (PBDs); 3.3.1 Molecular Modelling Studies of C7-linked PBD Dimers; 3.3.2 Molecular Modelling of C8/C2′-linked and C2/C2′-linked PBD Dimers; 3.4 Conclusion and Future Perspective; References; Chapter 4 -- Auristatin Payloads for Antibody-Drug Conjugates (ADCs); 4.1 Discovery of the Auristatins; 4.2 Mechanism of Action; 4.3 Activity; 4.4 Synthetic Availability and Analogues; 4.5 Validation of Auristatins Payloads for ADC Technology; 4.5.1 Auristatin E and Related ConjugatesZusammenfassung: 4.5.2 Development of Brentuximab Vedotin (ADCETRIS™)4.5.3 More MMAE Conjugates; 4.5.4 Novel Linker Technologies; 4.5.5 Extending the Range of Auristatin E- type Molecules; 4.6 Development of Monomethyl Auristatin F; 4.6.1 MMAF Properties; 4.6.2 Development of Alternative Ways of Linking MMAF to an Antibody; 4.6.3 C-Terminus- linked Auristatin F Conjugates; 4.7 Conclusions; References; Chapter 5 -- Maytansinoid Payloads for Antibody-Drug Conjugates (ADCs); 5.1 Introduction; 5.2 Maytansinoids: Structure-Activity Relationships (SARs); 5.3 Synthesis of Maytansinoid-ADCsZusammenfassung: Antibody-drug conjugates are a promising areas of anticancer drug discovery, conveying several advantages, including the ability to select likely responders, efficient delivery of cytotoxic agents and reduced toxicity. This book describes payloads used to date and novel payloads that may be used clinically in the futurePPN: PPN: 1671895363Package identifier: Produktsigel: ZDB-1-RSEK

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