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Intern
    Sonderforschungsbereich 630

    B8 Engstler

    Project Part B8

    VSG as unexpected drug target for sleeping sickness

    Prof. Dr. Markus Engstler

    Cell and Developmental Biology

    At any given time African trypanosomes express just one out of several hundred variant surface glycoprotein (VSG) genes. The sporadic switch in VSG expression forms the molecular basis of antigenic variation. We have found that certain triphenylmethanes (TPMs) bind to all VSG variants tested. In the presence of light, some TPMs become highly toxic for the parasites. We plan to decipher the molecular mechanism of TPM-toxicity and want to exploit those findings for rational design of TPM-based trypanocidal compounds.

    Selected, SFB-relevant Publications

    G. Hiltensperger, N. G. Jones, S. Niedermeier, A. Stich, M. Kaiser, J. Jung, S. Puhl, A. Damme, H. Braunschweig, L. Meinel, M. Engstler, U. Holzgrabe; Synthesis and structure-activity relationships of new quinolone-type molecules against Trypanosoma brucei. J Med Chem 2012, 55, 2538-2548.