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Sirtuin group in Kuopio. Molecular and Protein modeling

Maija.Lahtela-Kakkonen@uef.fi
www.uef.fi/en/web/farmasia/puhelinluettelo
Address
University of Eastern Finland School of Pharmacy. Yliopistonranta 1C 70211 Kuopio
Finland
Keywords

sirtuin, bromodomain, computer-aided drug design, molecular docking

Models

Techniques

molecular docking, virtual screening, QSAR, homology modeling

Collaborations outside COST

Dr. Panagis Filippakopoulus (University of Oxford, UK) has extensive experience in bromodomains. Dr. Ruin Moaddel (National Institute on Aging, National Institutes of Health, Bethesda, USA) has expertise in developing cellular membrane affinity chromatography columns for drug screening purposes. Docent Hannu Koistinen (Haartman Institute, University of Helsinki, Finland). Docent Koistinen is working on projects related to cancer biology, cell differentiation, and drug discovery. His group is participating in the development of clinical assays for prostate cancer and breast cancer.

Short description of ongoing research projects

We are working on various sirtuins and have developed selective SIRT1 and SIRT2 inhibitors, pan-inhibitors for sirtuins, discovered novel inhibitor scaffolds and reported the first SIRT6 inhibitors. We are also working with other epigenetic regulators like bromodomains.

Publications
  1. BET Inhibition Upregulates SIRT1 and Alleviates Inflammatory Responses.Kokkola T, Suuronen T, Pesonen M, Filippakopoulos P, Salminen A, Jarho EM, Lahtela-Kakkonen M. Chembiochem. 2015 Jul 25. doi: 10.1002/cbic.201500272
  2. Virtual screening approach of sirtuin inhibitors results in two new scaffolds. Kokkonen P, Kokkola T, Suuronen T, Poso A, Jarho E, Lahtela-Kakkonen M. Eur J Pharm Sci. 2015 Aug 30;76:27-32. doi: 10.1016/j.ejps.2015.04.025
  3. Chroman-4-one- and chromone-based sirtuin 2 inhibitors with antiproliferative properties in cancer cells. Seifert T, Malo M, Kokkola T, Engen K, Fridén-Saxin M, Wallén EA, Lahtela-Kakkonen M, Jarho EM, Luthman K. J Med Chem. 2014 Dec 11;57(23):9870-88. doi: 10.1021/jm500930h
  4. Studying SIRT6 regulation using H3K56 based substrate and small molecules.Kokkonen P, Rahnasto-Rilla M, Mellini P, Jarho E, Lahtela-Kakkonen M, Kokkola T.Eur J Pharm Sci. 2014 Oct 15;63:71-6. doi: 10.1016/j.ejps.2014.06.015.
  5. AROS has a context-dependent effect on SIRT1.Kokkola T, Suuronen T, Molnár F, Määttä J, Salminen A, Jarho EM, Lahtela-Kakkonen M.FEBS Lett. 2014 May 2;588(9):1523-8. doi: 10.1016/j.febslet.2014.03.020.
Other activities of potential interest to others


Cost UE