Neurotrophin mimetics are small molecules or peptide like molecules that can modulate the action of the neurotrophin receptor.
One of the main causes of neurodegeneration involves changes in the expression of neurotrophins (NTs) and/or their receptors (TrkA, TrkB, TrkC and p75NTR). Indeed, these imbalances or changes in their activity, lead to neuronal damage resulting in neurological and neurodegenerative conditions. The therapeutic properties of neurotrophins attracted the focus of many researchers during the years, but the poor pharmacokinetic properties, such as reduced bioavailability and low metabolic stability, the hyperalgesia, the inability to penetrate the blood–brain barrier and the short half-lives render the large neurotrophin proteins not suitable to be implemented as drugs.[1]
For this reason, several efforts have been made to develop neurotrophin mimetics (small molecules and peptidomimetics) that can modulate the action of the neurotrophin receptors (Trks and p75NTR) and possess drug-like pharmacokinetic and pharmacodynamic profiles. Specifically, these mimetics can be classified as TrkA and TrkB receptor agonists and p75NTR modulators/antagonists.[2]
^Josephy-Hernandez, Sylvia; Jmaeff, Sean; Pirvulescu, Iulia; Aboulkassim, Tahar; Saragovi, H. Uri (January 2017). "Neurotrophin receptor agonists and antagonists as therapeutic agents: An evolving paradigm". Neurobiology of Disease. 97 (Pt B): 139–155. doi:10.1016/j.nbd.2016.08.004. ISSN 0969-9961. PMID 27546056. S2CID 8469340.
^Gudasheva, Tatiana A.; Povarnina, Polina Y.; Tarasiuk, Aleksey V.; Seredenin, Sergey B. (September 2021). "Low-molecular mimetics of nerve growth factor and brain-derived neurotrophic factor: Design and pharmacological properties". Medicinal Research Reviews. 41 (5): 2746–2774. doi:10.1002/med.21721. ISSN 0198-6325. PMID 32808322. S2CID 221163909.
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