Journal
CURRENT PHARMACEUTICAL DESIGN
Volume 15, Issue 6, Pages 637-658Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/138161209787315648
Keywords
beta-Amyloid; A beta; multivalent; multifunction; ligand; Alzheimer's disease; AD drug; imaging probe; early diagnosis
Categories
Funding
- Ministry of Education, Science and Technology [2E20560, 2N30420]
- Ministry of Knowledge Economy [2M20830]
Ask authors/readers for more resources
Ligands selectively targeting beta-amyloid in the living brain are promising candidates of therapeutics and early diagnosis tools for Alzheimer's disease. Among the major stages of beta-amyloid aggregation, monomers and oligomers are excellent targets to reduce neurotoxic brain damages for prevention of the disease progression, while oligomers and fibrils, abundant in the late stage of the disease, are pathological objectives to develop reliable imaging probes. So far, there have been many efforts to develop a wide variety of monovalent beta-amyloid ligands such as thioflavin T, PIB, FDDNP, curcumin, and tramiprosate. However, pathology of Alzheimer's disease is not fully understood yet so that there is currently no cure and further investigations on Alzheimer's disease are needed. For past several years, multivalent beta-amyloid ligands have offered an alternative route by enhancing binding affinity of drug candidates. In addition, it has been revealed that not only neurotoxicity due to the protein misfolding but also other factors are involved in the beta-amyloid cascade such as oxidative stress, inflammation, metal chelation, and several types of neurotransmitters. Thus, there have been numerous studies to improve binding affinities of single beta-amyloid ligands via adopting multivalent effects or to develop drug candidates targeting multiple stages of the pathological cascade. In this review, multivalent and multifunctional amyloid ligands and their promising aspects as an alternative approach to Alzheimer's disease are discussed.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available