2024年11月17日 · Smaller peptides, known as oligopeptides, may contain as few as two to ten amino acid residues. Peptides play significant roles in the human body. For example, insulin regulates metabolism [6], while dynorphin mediates pain signals [7]. They also play crucial roles in endocrine signaling and can act as growth factors.

2022年2月14日 · Small molecule drugs are known to have an extended therapeutic history with inherent advantages, including low production costs and sale prices, oral administration, and good membrane...

2024年10月1日 · Endowing properties of peptides onto small molecules can evolutionarily combine the advantages of both moieties and improve the biological druggability of molecules. Herein, we present eight representative recent cases in this conversion and elaborate on the transformation process of each case.

2022年7月29日 · Here, we propose a novel small molecule lead discovery strategy, ″Peptide-to-Small Molecule″, which is a combination of rapid identification of high-affinity macrocyclic peptides via peptide display screening followed by pharmacophore-guided de novo design of small molecules, and demonstrate the applicability using nicotinamide N ...

2024年2月16日 · By applying the properties of the peptide–protein interaction the development of small molecules for drug discovery has the potential to be more efficient. In this review, we discuss the methods that allow for the unique binding properties of peptides to proteins, and the methods deployed to transfer these qualities to potent small molecules.

2023年12月6日 · Almost a decade ago, we summarized the advantages of peptide-based drugs over small molecule counterparts and the necessary target selection, lead optimization and formulation steps required to make synthetic peptide therapeutics both useful and appreciated alternatives from human therapy and pharmaceutical investment perspectives (Otvos and ...

Here we propose a panoramic review of the common principles for the conversion of peptides into small organic molecules and the most interesting findings in peptide-based leads of the last decades.

Peptide-drug conjugates are a unique class of molecules that integrate peptides and small molecule drugs to achieve increased therapeutic outcomes. They represent an important field in drug discovery that is related in principle to antibody-directed drug targeting.

2020年1月1日 · In fact, the generation of small molecule peptidomimetics consists of reducing the conformational flexibility and the peptide character to improve the potency and selectivity, and to achieve hit compounds with improved bioactivity and pharmacokinetics profile.

Small peptides are a group of bioactive compounds with low molecular weights and complex structures. This review covers recent advances in the microbial production of small peptide, focusing on the development of chassis cells functioning as green factories using synthetic biology approaches.