2024年11月17日 · The relatively small size and large surface area of peptides allow for more precise docking to target molecules, which enhances their effectiveness. Researchers' interest in developing peptide ligands and probes for studying the structures and functions of target receptors has increased dramatically in recent years.

2023年5月26日 · The modern peptide mimetics approach incorporates a production of small molecules which mimic peptides in order to overcome their ineffectiveness as drugs when administered orally. The small molecules mimetics retain the desired biological properties of the peptide lead, but are metabolically stable, have unlimited diversity, and can be ...

2023年5月26日 · Peptides can be used for a variety of applications including biomedical research, peptide-based vaccines, peptide nanotubes, design of novel enzymes, diagnostic peptides, etc.

2024年10月1日 · Peptide-to-small-molecule (PTSM) strategy is a way of condensation of large peptide, while the fragment-based-drug-design (FBDD) is the other solution to expand a core fragment hit to large molecules. They are two perspectives to …

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...

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 ...

We first discuss rules that govern the passive permeability of small molecules across the lipid membrane, and mechanisms of membrane transport that have evolved in nature for certain metabolites, peptides, and proteins.

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.

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 ...