The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity

Author:

Košak Urban1,Brus Boris1,Knez Damijan1,Žakelj Simon1,Trontelj Jurij1,Pišlar Anja1,Šink Roman1,Jukič Marko1,Živin Marko2,Podkowa Adrian3,Nachon Florian4ORCID,Brazzolotto Xavier4,Stojan Jure5,Kos Janko1,Coquelle Nicolas6,Sałat Kinga3,Colletier Jacques-Philippe6,Gobec Stanislav1ORCID

Affiliation:

1. Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, 1000 Ljubljana, Slovenia

2. Institute of Pathological Physiology, Faculty of Medicine, University of Ljubljana, Vrazov trg 2, 1000 Ljubljana, Slovenia

3. Faculty of Pharmacy, Jagiellonian University, Medyczna 9 St., 30-688 Krakow, Poland

4. Institut de Recherche Biomédicale des Armées, 91223 Brétigny sur Orge, France

5. Institute of Biochemistry, Faculty of Medicine, University of Ljubljana, Vrazov trg 2, 1000 Ljubljana, Slovenia

6. University Grenoble Alpes, and CNRS and CEA, IBS, F-38044 Grenoble, France

Funder

Agence Nationale de la Recherche

Javna Agencija za Raziskovalno Dejavnost RS

Association France Alzheimer

Commissariat ? l'?nergie Atomique et aux ?nergies Alternatives

Institut Francais

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Reference89 articles.

1. Price, M.; Comas-Herrera, A.; Knapp, M.; Guerchet, M.; Karagiannidou, M.The World Alzheimer Report 2016;Alzheimer’s Disease International (ADI):London, 2016; pp1–131.

2. Forecasting the global burden of Alzheimer's disease

3. Tau post-translational modifications in wild-type and human amyloid precursor protein transgenic mice

4. Subcellular Biochemistry;Glabe C. C.,2005

5. Cellular mechanisms of beta -amyloid production and secretion

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