Site-selective lysine conjugation methods and applications towards antibody–drug conjugates

Drug Conjugates ◽

Lysine Modification ◽

Site Selective ◽

In this feature article we discuss developments in site-selective lysine modification methodologies and their application towards the synthesis of antibody–drug conjugates; including our recent work on a cysteine-to-lysine transfer (CLT) protocol.

Homogeneous antibody-drug conjugates via site-selective disulfide bridging

Drug Discovery Today Technologies ◽

10.1016/j.ddtec.2018.09.004 ◽

2018 ◽

Vol 30 ◽

pp. 11-20 ◽

Cited By ~ 12

Author(s):

Nafsika Forte ◽

Vijay Chudasama ◽

James R. Baker

Keyword(s):

Drug Conjugates ◽

Disulfide Bridging ◽

Site Selective ◽

ChemInform Abstract: Construction of Homogeneous Antibody-Drug Conjugates Using Site-Selective Protein Chemistry

ChemInform ◽

10.1002/chin.201625267 ◽

2016 ◽

Vol 47 (25) ◽

Cited By ~ 1

Author(s):

Padma Akkapeddi ◽

Saara-Anne Azizi ◽

Allyson M. Freedy ◽

Pedro M. S. D. Cal ◽

Pedro M. P. Gois ◽

...

Keyword(s):

Protein Chemistry ◽

Drug Conjugates ◽

Site Selective ◽

A general approach for the site-selective modification of native proteins, enabling the generation of stable and functional antibody–drug conjugates

Chemical Science ◽

10.1039/c8sc04645j ◽

2019 ◽

Vol 10 (3) ◽

pp. 694-700 ◽

Cited By ~ 23

Author(s):

Stephen J. Walsh ◽

Soleilmane Omarjee ◽

Warren R. J. D. Galloway ◽

Terence T.-L. Kwan ◽

Hannah F. Sore ◽

...

Keyword(s):

Drug Conjugates ◽

Native Proteins ◽

Site Selective ◽

Divinylpyrimidine (DVP) linkers enable access to highly stable and functional antibody–drug conjugates.

Site-selective modification strategies in antibody–drug conjugates

Chemical Society Reviews ◽

10.1039/d0cs00310g ◽

2021 ◽

Author(s):

Stephen J. Walsh ◽

Jonathan D. Bargh ◽

Friederike M. Dannheim ◽

Abigail R. Hanby ◽

Hikaru Seki ◽

...

Keyword(s):

Cell Types ◽

Specific Cell ◽

Specific Targeting ◽

Drug Conjugates ◽

Site Selective ◽

Antibody Drug ◽

Made In

Antibody–drug conjugates (ADCs) harness the highly specific targeting capabilities of an antibody to deliver a cytotoxic payload to specific cell types. This review summarises the advances made in the construction of homogenous ADCs.

Correction: A general approach for the site-selective modification of native proteins, enabling the generation of stable and functional antibody–drug conjugates

Chemical Science ◽

10.1039/c8sc90248h ◽

2019 ◽

Vol 10 (2) ◽

pp. 633-634

Author(s):

Stephen J. Walsh ◽

Soleilmane Omarjee ◽

Warren R. J. D. Galloway ◽

Terence T.-L. Kwan ◽

Hannah F. Sore ◽

...

Keyword(s):

Drug Conjugates ◽

Native Proteins ◽

Site Selective ◽

Correction for ‘A general approach for the site-selective modification of native proteins, enabling the generation of stable and functional antibody–drug conjugates’ by Stephen J. Walsh et al., Chem. Sci., 2019, DOI: 10.1039/c8sc04645j.

Construction of homogeneous antibody–drug conjugates using site-selective protein chemistry

Chemical Science ◽

10.1039/c6sc00170j ◽

2016 ◽

Vol 7 (5) ◽

pp. 2954-2963 ◽

Cited By ~ 82

Author(s):

Padma Akkapeddi ◽

Saara-Anne Azizi ◽

Allyson M. Freedy ◽

Pedro M. S. D. Cal ◽

Pedro M. P. Gois ◽

...

Keyword(s):

Therapeutic Efficacy ◽

Protein Chemistry ◽

Drug Conjugates ◽

Drug Conjugation ◽

Selective Chemical ◽

Site Selective ◽

The use of site-selective chemical drug-conjugation strategies enables the construction of antibody–drug conjugates (ADCs) with superior therapeutic efficacy.”

ASCO-GU 2019: Metastasierte Urothelkarzinome

Onkologische Welt ◽

10.1055/a-0869-6415 ◽

2019 ◽

Vol 10 (03) ◽

pp. 140-141

Author(s):

Alexander Kretzschmar

Keyword(s):

San Francisco ◽

Drug Conjugates ◽

Chapel Hill ◽

Die Therapielandschaft des metastasierten Urothelkarzinoms hat sich seit der Zulassung der ersten Immun-Checkpoint-Inhibitoren verändert. Die neuen Therapien sind deutlich effektiver, allerdings erreichen die Responseraten der neuen Therapien nur bis zu etwa 30 %, beklagte Prof. Matthew Milowsky, Chapel Hill/USA, auf einer Oral Abstract Session auf dem ASCO-GU. In San Francisco gaben erste Vorträge und Poster bereits einen Einblick, wovon diejenigen Patienten profitieren könnten, die auf die etablierten Chemotherapien und die neuen Immuntherapien nicht ansprechen. Manche Onkologen sprechen bereits von der „Post-Checkpoint-Ära”. Als Kandidaten werden vor allem Antikörper-Wirkstoff-Konjugate (antibody-drug conjugates; ADC) gehandelt – und zwar nicht nur zur Therapie des metastasierten Blasenkarzinoms.