Computationally designed antibody–drug conjugates self-assembled via affinity ligands

Gupta, Nilesh; Ansari, Aasif; Dhoke, Gaurao V.; Chilamari, Maheshwerreddy; Sivaccumar, Jwala; Kumari, Smita; Chatterjee, Snigdha; Goyal, Ravinder; Dutta, Pradip Kumar; Samarla, Mallik; Mukherjee, Madhumita; Sarkar, Arindam; Mandal, Swadhin K.; Rai, Vishal; Biswas, Goutam; Sengupta, Aniruddha; Roy, Sudip; Roy, Moni; Sengupta, Shiladitya

doi:10.1038/s41551-019-0470-8

Cited by 24 publications

(29 citation statements)

References 48 publications

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“…15F). 245 4-Mercaptoethylpyridine (MEP), which is used in antibody purification because of its ability to selectively bind distinct regions within both the Fab and Fc fragments was used to facilitate this non-covalent conjugation. 246,247 This method yielded homogeneous DAR 6 ADCs via reaction of trastuzumab or cetuximab with MEPmodified gemcitabine.…”

Section: C-/n-terminal Modificationsmentioning

confidence: 99%

Site-selective modification strategies in antibody–drug conjugates

et al. 2021

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Section: C-/n-terminal Modificationsmentioning

confidence: 99%

Site-selective modification strategies in antibody–drug conjugates

et al. 2021

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“…In addition, the efficacy of the conjugate was demonstrated using an in vivo xenograft model of human lung adenocarcinoma. 74 …”

Section: Affinity Ligands and Their Role In Site-specific Conjugation Of Unmodified Antibodiesmentioning

confidence: 99%

“…The authors also demonstrate that, despite the interaction being noncovalent, the conjugated antibodies were stable in both mouse and human plasma for 14 days. In addition, the efficacy of the conjugate was demonstrated using an in vivo xenograft model of human lung adenocarcinoma …”

Section: Affinity Ligands and Their Role In Site-specific Conjugation...mentioning

confidence: 99%

“…In addition, the efficacy of the conjugate was demonstrated using an in vivo xenograft model of human lung adenocarcinoma. 74 While very promising and obviously stable, some applications may still require covalent attachment of the label to ensure little to no label loss, in particular, when using detection antibodies in harsher reaction conditions for which these methods may not be optimal.…”

Section: ■ Affinity Ligands and Their Role In Site-specific Conjugati...mentioning

confidence: 99%

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Affinity-Based Methods for Site-Specific Conjugation of Antibodies

2021

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Conjugation of various reagents to antibodies has long been an elegant way to combine the superior binding features of the antibody with other desired but non-natural functions. Applications range from labels for detection in different analytical assays to the creation of new drugs by conjugation to molecules which improves the pharmaceutical effect. In many of these applications, it has been proven advantageous to control both the site and the stoichiometry of the conjugation to achieve a homogeneous product with predictable, and often also improved, characteristics. For this purpose, many research groups have, during the latest decade, reported novel methods and techniques, based on small molecules, peptides, and proteins with inherent affinity for the antibody, for site-specific conjugation of antibodies. This review provides a comprehensive overview of these methods and their applications and also describes a historical perspective of the field.

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“… 178 , 179 Furthermore, studies have also reported computational approaches for self‐assembled synthesizing ADCs by molecular docking and dynamics simulations to overcome the instability and heterogeneity of ADCs. 180 …”

Section: Challenges and Prospectsmentioning

confidence: 99%