The dawn of a new era: targeting the “undruggables” with antibody-based therapeutics

L Qian, X Lin, X Gao, RU Khan, JY Liao, S Du… - Chemical …, 2023 - ACS Publications
The high selectivity and affinity of antibodies toward their antigens have made them a highly
valuable tool in disease therapy, diagnosis, and basic research. A plethora of chemical and …

Chemical synthesis of bioactive proteins

O Harel, M Jbara - Angewandte Chemie, 2023 - Wiley Online Library
Nature has developed a plethora of protein machinery to operate and maintain nearly every
task of cellular life. These processes are tightly regulated via post‐expression modifications …

Chemical generation of checkpoint inhibitory T cell engagers for the treatment of cancer

PA Szijj, MA Gray, MK Ribi, C Bahou, JCF Nogueira… - Nature …, 2023 - nature.com
Bispecific T cell engagers (BiTEs), a subset of bispecific antibodies (bsAbs), can promote a
targeted cancer cell's death by bringing it close to a cytotoxic T cell. Checkpoint inhibitory T …

Deciphering the Role of the Ser‐Phosphorylation Pattern on the DNA‐Binding Activity of Max Transcription Factor Using Chemical Protein Synthesis

RV Nithun, YM Yao, X Lin, S Habiballah… - Angewandte Chemie …, 2023 - Wiley Online Library
The chemical synthesis of site‐specifically modified transcription factors (TFs) is a powerful
method to investigate how post‐translational modifications (PTMs) influence TF‐DNA …

Ultrafast Au (III)-Mediated Arylation of Cysteine

EA Doud, JAR Tilden, JW Treacy… - Journal of the …, 2024 - ACS Publications
Through mechanistic work and rational design, we have developed the fastest
organometallic abiotic Cys bioconjugation. As a result, the developed organometallic Au (III) …

Novel formats of antibody conjugates: recent advances in payload diversity, conjugation, and linker chemistry

T Fujii, Y Matsuda - Expert Opinion on Biological Therapy, 2023 - Taylor & Francis
Introduction In the field of bioconjugates, the focus on antibody–drug conjugates (ADCs)
with novel payloads beyond the traditional categories of potent cytotoxic agents is …

On-Demand Thio-Succinimide Hydrolysis for the Assembly of Stable Protein–Protein Conjugates

AV Vasco, RJ Taylor, Y Méndez… - Journal of the American …, 2024 - ACS Publications
Chemical post-translational protein–protein conjugation is an important technique with
growing applications in biotechnology and pharmaceutical research. Maleimides represent …

Trimming crystallizable fragment (Fc) glycans enables the direct enzymatic transfer of biomacromolecules to antibodies as therapeutics

Y Yang, Z Song, T Tian, Z Zhao, J Chen… - Angewandte Chemie …, 2023 - Wiley Online Library
Glycoengineering has provided powerful tools to construct site‐specific antibody conjugates.
However, only small‐molecule payloads can be directly transferred to native or engineered …

Microbial synthesis of high-molecular-weight, highly repetitive protein polymers

J Jeon, SV Subramani, KZ Lee, B Jiang… - International journal of …, 2023 - mdpi.com
High molecular weight (MW), highly repetitive protein polymers are attractive candidates to
replace petroleum-derived materials as these protein-based materials (PBMs) are …

Rapid Access to Potent Bispecific T Cell Engagers Using Biogenic Tyrosine Click Chemistry

I Shajan, LNC Rochet, SR Tracey… - Bioconjugate …, 2023 - ACS Publications
Bispecific antibodies as T cell engagers designed to display binding capabilities to both
tumor-associated antigens and antigens on T cells are considered promising agents in the …