Allenamide as an Orthogonal Handle for Selective Modification of Cysteine in Peptides and Proteins

Opportunity  

The global cancer therapeutics market is expected to grow from US$ 164 billion in 2022 to US$ 394 billion by 2032, at a CAGR of 9.20%. The rise in cancer cases and the ageing population are key factors driving the demand for novel cancer therapies. ADCs are promising novel therapeutics, but optimising the linker and payload is critical to their success.  

Technology  

The invention utilises allenamides for the selective binding and labelling of target cysteine residues in peptides and proteins. This technology holds promise for developing inhibitors targeting cysteine proteases, which are enzymes involved in various diseases. Additionally, allenamides can be used to create ADCs and serve as the basis for diagnostic and imaging agents. By harnessing the properties of allenamides, this invention offers a versatile and effective platform for targeting cysteine residues, facilitating advancements in therapeutic and diagnostic fields. 

Figure 1: Allenamide as a Cysteine-Specific Linker for Antibody-Drug Conjugates

Applications & Advantages  

Main application areas include therapeutic development as cysteine protease inhibitors and as linker technology for ADC drugs, as well as in diagnostic development. 

Advantages: 

• Selective binding and labelling of target cysteine residues.
• Versatile platform for diagnostic and therapeutic developments.