Photoconjugation of an Fc-Specific Peptide Enables Efficient DAR 2 Antibody-Drug Conjugate Formation

Tae Jin Lee; Ju Hwan Kim; Se Jeong Kwon; Sun Hee Park; Jinyoung Kim; Hyo Jin Kang; Sang J. Chung

doi:10.1021/acs.orglett.0c03049

Photoconjugation of an Fc-Specific Peptide Enables Efficient DAR 2 Antibody-Drug Conjugate Formation

Tae Jin Lee
, Ju Hwan Kim
, Se Jeong Kwon
, Sun Hee Park
, Jinyoung Kim
, Hyo Jin Kang
, Sang J. Chung

Department of Pharmacy

Sungkyunkwan University
AbTis Company Ltd.
Gyeonggido Business Science Accelerator

Research output: Contribution to journal › Article › peer-review

8 Scopus citations

Abstract

Antibody-drug conjugates (ADCs) in current clinical usage have been constructed via the nonspecific conjugation of drugs to antibodies, rendering the manufacturing processes difficult. In this study, a high-affinity IgG Fc-binding peptide equipped with a photoreactive amino acid was developed and successfully conjugated to Glu-382 of trastuzumab in a site-specific manner. The resulting conjugate was employed to generate a DAR 2 ADC product using click chemistry.

Original language	English
Pages (from-to)	8419-8423
Number of pages	5
Journal	Organic Letters
Volume	22
Issue number	21
DOIs	https://doi.org/10.1021/acs.orglett.0c03049
State	Published - 6 Nov 2020

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10.1021/acs.orglett.0c03049

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title = "Photoconjugation of an Fc-Specific Peptide Enables Efficient DAR 2 Antibody-Drug Conjugate Formation",

abstract = "Antibody-drug conjugates (ADCs) in current clinical usage have been constructed via the nonspecific conjugation of drugs to antibodies, rendering the manufacturing processes difficult. In this study, a high-affinity IgG Fc-binding peptide equipped with a photoreactive amino acid was developed and successfully conjugated to Glu-382 of trastuzumab in a site-specific manner. The resulting conjugate was employed to generate a DAR 2 ADC product using click chemistry.",

author = "Lee, \{Tae Jin\} and Kim, \{Ju Hwan\} and Kwon, \{Se Jeong\} and Park, \{Sun Hee\} and Jinyoung Kim and Kang, \{Hyo Jin\} and Chung, \{Sang J.\}",

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year = "2020",

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doi = "10.1021/acs.orglett.0c03049",

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journal = "Organic Letters",

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T1 - Photoconjugation of an Fc-Specific Peptide Enables Efficient DAR 2 Antibody-Drug Conjugate Formation

AU - Lee, Tae Jin

AU - Kim, Ju Hwan

AU - Kwon, Se Jeong

AU - Park, Sun Hee

AU - Kim, Jinyoung

AU - Kang, Hyo Jin

AU - Chung, Sang J.

PY - 2020/11/6

Y1 - 2020/11/6

N2 - Antibody-drug conjugates (ADCs) in current clinical usage have been constructed via the nonspecific conjugation of drugs to antibodies, rendering the manufacturing processes difficult. In this study, a high-affinity IgG Fc-binding peptide equipped with a photoreactive amino acid was developed and successfully conjugated to Glu-382 of trastuzumab in a site-specific manner. The resulting conjugate was employed to generate a DAR 2 ADC product using click chemistry.

AB - Antibody-drug conjugates (ADCs) in current clinical usage have been constructed via the nonspecific conjugation of drugs to antibodies, rendering the manufacturing processes difficult. In this study, a high-affinity IgG Fc-binding peptide equipped with a photoreactive amino acid was developed and successfully conjugated to Glu-382 of trastuzumab in a site-specific manner. The resulting conjugate was employed to generate a DAR 2 ADC product using click chemistry.

UR - https://www.scopus.com/pages/publications/85095862277

U2 - 10.1021/acs.orglett.0c03049

DO - 10.1021/acs.orglett.0c03049

M3 - Article

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AN - SCOPUS:85095862277

SN - 1523-7060

VL - 22

SP - 8419

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JO - Organic Letters

JF - Organic Letters

IS - 21

ER -

Photoconjugation of an Fc-Specific Peptide Enables Efficient DAR 2 Antibody-Drug Conjugate Formation

Abstract

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