Advances in Solid-Phase Peptide and Oligonucleotide Synthesis: Methods, Mechanisms, and Therapeutic Applications

Dear Colleagues,

Solid-phase synthesis remains one of the most powerful and versatile techniques for the preparation of bioactive molecules, enabling the rapid assembly, modification, and optimization of peptides and oligonucleotides (TIDEs) with therapeutic potential. Over the past decade, significant advances have been made in resin chemistry, coupling reagents, automation, and orthogonal protection strategies—paving the way for the more sustainable and scalable synthesis of complex TIDEs.

This Special Issue aims to highlight cutting-edge developments in solid-phase peptide and oligonucleotide synthesis, covering innovations in methodology, automation, linker and protecting group design, and hybrid chemoenzymatic approaches. We also welcome studies focused on structure–activity relationships, conjugation strategies, post-synthetic modifications, and the application of synthetic peptides and oligonucleotides in drug discovery, diagnostics, and biotechnology.

By bringing together contributions from both academia and industry, this Special Issue seeks to bridge the gap between synthetic innovation and therapeutic application, showcasing how advances in chemical synthesis continue to transform modern medicinal chemistry and molecular therapeutics.

Dr. Danah AlShaer
Dr. Rakesh Tiwari
Guest Editors

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