Department für Pharmazie Zi.Nr.: C1.050A |
TLX (human homologue of Drosophila tailless) is an orphan nuclear receptor that is mainly expressed in neural stem cells. Its link to neurodegenerative diseases and neurological disorders evokes our group’s interest for TLX as a pharmaceutical target. In order to explore the pharmacological potential and the medicinal chemistry of this nuclear receptor, a set of potent and selective tool compounds is needed. My current aim is to perform SAR studies on a recently discovered TLX lead agonist.
Michel, M.; Benítez-Buelga, C.; Calvo, P. A.; Hanna, B. M. F.; Mortusewicz, O.; Masuyer, G.; Davies, J.; Wallner, O.; Sanjiv, K.; Albers, J. J.; Castañeda-Zegarra, S.; Jemth, A.-S.; Visnes, T.; Sastre-Perona, A.; Danda, A. N.; Homan, E. J.; Marimuthu, K.; Zhenjun, Z.; Chi, C. N.; Sarno, A.; Wiita, E.; Nicolai, C. von; Komor, A. J.; Rajagopal, V.; Müller, S.; Hank, E. C.; Varga, M.; Scaletti, E. R.; Pandey, M.; Karsten, S.; Haslene-Hox, H.; Loevenich, S.; Marttila, P.; Rasti, A.; Mamonov, K.; Ortis, F.; Schömberg, F.; Loseva, O.; Stewart, J.; D'Arcy-Evans, N.; Koolmeister, T.; Henriksson, M.; Michel, D.; Ory, A. de; Acero, L.; Calvete, O.; Scobie, M.; Hertweck, C.; Vilotijevic, I.; Kalderén, C.; Osorio, A.; Perona, R.; Stolz, A.; Stenmark, P.; Berglund, U. W.; Vega, M. de; Helleday, T. Small-molecule activation of OGG1 increases oxidative DNA damage repair by gaining a new function. Science, 2022, 376, 1471–1476. DOI: 10.1126/science.abf8980.
Müller, C.; Hank, E.; Giera, M.; Bracher, F. Dehydrocholesterol Reductase 24 (DHCR24): Medicinal Chemistry, Pharmacology and Novel Therapeutic Options. Curr. Med. Chem., 2022, 29, 4005–4025. DOI: 10.2174/0929867328666211115121832.