Small endogenous molecules as moiety to improve targeting of CNS drugs
| Autor: | Viviana De Caro, Libero Italo Giannola, Flavia Maria Sutera |
|---|---|
| Přispěvatelé: | Sutera, F.M., De Caro, V., Giannola, L.I. |
| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Pharmaceutical Science Endogeny Computational biology Pharmacology Blood–brain barrier Diffusion 03 medical and health sciences 0302 clinical medicine medicine small endogenous molecules Moiety CNS prodrug Animals Humans Prodrugs multifunctional drug biology Membrane transport protein Chemistry CNS carrier Membrane Transport Proteins Translation (biology) Transporter Biological Transport Prodrug 030104 developmental biology medicine.anatomical_structure bioisosteric drug Carrier protein Settore CHIM/09 - Farmaceutico Tecnologico Applicativo Blood-Brain Barrier biology.protein Carrier Proteins BBB 030217 neurology & neurosurgery Central Nervous System Agents |
| Zdroj: | Europe PubMed Central |
| ISSN: | 1744-7593 |
| Popis: | A major challenge in the development of novel neuro-therapeutic agents is to effectively overcome the blood-brain barrier (BBB), which acts as a 'working dynamic barrier'. The core problem in the treatment of neurodegenerative diseases is failed delivery of potential medicines due to their inadequate permeation rate. Areas covered: The present review gives a summary of endogenous moieties used in synthesizing prodrugs, derivatives and bioisosteric drugs appositely designed to structurally resemble physiological molecular entities able to be passively absorbed or carried by specific carrier proteins expressed at BBB level. In particular, this overview focuses on aminoacidic, glycosyl, purinergic, ureic and acidic fragments derivatives, most of which can take advantage from BBB carrier-mediated transporters, where passive diffusion is not permitted. Expert opinion: In the authors ’ perspective, further progress in this field could expedite successful translation of new chemical entities into clinical trials. Careful rationalization of the linkage between endogenous molecular structures and putative transporters binding sites could allow to useful work-flows and libraries for synthesizing new BBB-crossing therapeutic substances and/or multifunctional drugs for treatments of central disorders. |
| Databáze: | OpenAIRE |
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