Site-selective modification strategies in antibody–drug conjugates
Antibody–drug conjugates (ADCs) harness the highly specific targeting capabilities of an
antibody to deliver a cytotoxic payload to specific cell types. They have garnered …
antibody to deliver a cytotoxic payload to specific cell types. They have garnered …
The chemistry behind ADCs
V Kostova, P Désos, JB Starck, A Kotschy - Pharmaceuticals, 2021 - mdpi.com
Combining the selective targeting of tumor cells through antigen-directed recognition and
potent cell-killing by cytotoxic payloads, antibody-drug conjugates (ADCs) have emerged in …
potent cell-killing by cytotoxic payloads, antibody-drug conjugates (ADCs) have emerged in …
Diethynyl Phosphinates for Cysteine‐Selective Protein Labeling and Disulfide Rebridging
CE Stieger, L Franz, F Körlin… - Angewandte Chemie …, 2021 - Wiley Online Library
Diethynyl phosphinates were developed as bisfunctional electrophiles for the site‐selective
modification of peptides, proteins and antibodies. One of their electron‐deficient triple bonds …
modification of peptides, proteins and antibodies. One of their electron‐deficient triple bonds …
Modular chemical construction of IgG-like mono-and bispecific synthetic antibodies (SynAbs)
In recent years there has been rising interest in the field of protein–protein conjugation,
especially related to bispecific antibodies (bsAbs) and their therapeutic applications. These …
especially related to bispecific antibodies (bsAbs) and their therapeutic applications. These …
All-in-one disulfide bridging enables the generation of antibody conjugates with modular cargo loading
Antibody–drug conjugates (ADCs) are valuable therapeutic entities which leverage the
specificity of antibodies to selectively deliver cytotoxins to antigen-expressing targets such …
specificity of antibodies to selectively deliver cytotoxins to antigen-expressing targets such …
The renaissance of chemically generated bispecific antibodies
Bispecific antibodies (bsAbs) target two different epitopes. These are an up-and-coming
class of biologics, with two such therapeutics (emicizumab and blinatumomab) FDA …
class of biologics, with two such therapeutics (emicizumab and blinatumomab) FDA …
Ethynylphosphonamidates for the Rapid and Cysteine‐Selective Generation of Efficacious Antibody–Drug Conjugates
MA Kasper, A Stengl, P Ochtrop… - Angewandte Chemie …, 2019 - Wiley Online Library
Requirements for novel bioconjugation reactions for the synthesis of antibody–drug
conjugates (ADCs) are exceptionally high, since conjugation selectivity as well as the …
conjugates (ADCs) are exceptionally high, since conjugation selectivity as well as the …
Leucine-rich alpha-2-glycoprotein 1 (LRG1) as a novel ADC target
Leucine-rich alpha-2-glycoprotein 1 (LRG1) is present abundantly in the microenvironment
of many tumours where it contributes to vascular dysfunction, which impedes the delivery of …
of many tumours where it contributes to vascular dysfunction, which impedes the delivery of …
Orthogonal hydroxyl functionalization of cGAMP confers metabolic stability and enables antibody conjugation
cGAMP is a signaling molecule produced by the cGAS–DNA complex to establish
antimicrobial and antitumor immunity through STING. Whereas STING activation holds …
antimicrobial and antitumor immunity through STING. Whereas STING activation holds …
Dual reactivity disulfide bridging reagents; enabling new approaches to antibody fragment bioconjugation
Disulfide bridging, also known as disulfide stapling, is a powerful strategy for the
construction of site-selective protein bioconjugates. Here we describe the first examples of a …
construction of site-selective protein bioconjugates. Here we describe the first examples of a …