Prof. Dr. Erwin von Angerer

Akademischer Direktor

• Endocrine Therapy of Breast Cancer

We have a long term interest in the synthesis and biological characterisation of new non-steroidal estrogen antagonists. Based on various heterocyclic systems such as 2-phenylindoles, benzocarbazoles, benzofurans, and benzothiophenes we have synthesized a wide spectrum of ligands for the estrogen receptor. Depending on the structure of the side chains these agent are pure or partial antiestrogens and might be useful for the treatment of hormone-dependent breast cancer.

• Inhibitors of Steroid Sulfatase

In related work we converted some of the estrogen antagonists into sulfamates which can act as sulatase inhibitors. The objective of this study is the reduction of the levels of free estrogens in breast cancer cells by inhibition of the enzymatic hydrolysis of estrone sulfate.

• Development of Tubulin-Directed Agents

In a different project we search for small molecules capable of inhibiting the polymerisation of tubulin to functional microtubules. We have previously shown that 3-indolylcarbaldehydes and related structures strongly inhibit the growth of human tumor cells by interfering with the dynamic equilibrium between the dimeric and polymeric form of tubulin. Modifications of the lead structure should improve potency and render the compounds active in vivo.

• Chemically Induced Apoptosis

Recent publications

von Angerer, E. (2000): Tubulin as a target for anticancer drugs. Curr. Opin. Drug Discovery Dev. 3: 575-584.

Golob, T., Biberger, C., Walter, G., von Angerer, E. (2000): Antiestrogenic activities of 3,8- dihydroxy-6,11-dihydrobenzo[a]carbazoles with sulfur-containing side chains. Arch. Pharm. Pharm. Med. Chem. 333: 305-311.

von Angerer, E. (1999): New inhibitors of tubulin polymerisation. Exp.Opin.Ther.Patents, 9:1069-1081.

von Angerer, E. (1999): Structure-activity relationships. In: Handbook of Experimental Pharmacology, Vol. 135/1: Estrogens and Antiestrogens I, edited by M. Oettel, et al, pp. 81-108. Springer-Verlag, Berlin.

von Angerer, E. (1999): Antiestrogens and partial agonists. In: Handbook of Experimental Pharmacology, Vol. 135/1: Estrogens and Antiestrogens I, edited by M. Oettel, et al, pp. 55-80. Springer-Verlag, Berlin.

Newton, C.J., Schlatterer, K., Stalla, G.K., von Angerer, E., and Wowra, B. (1998): Pharmacological enhancement of radiosurgery response: Studies on an in vitro model system. J.Radiosurg., 1:51-56.

Leichtl, S. and von Angerer, E. (1998): 2-Phenylbenzo[b]thiophene-based antiestrogens with mammary tumor inhibiting activity. Arch.Pharm.Pharm.Med.Chem., 331:283-289.

Gastpar, R., Goldbrunner, M., Marko, D., and von Angerer, E. (1998): Methoxy-substituted 3-formyl-2-phenylindoles inhibit tubulin polymerization. J.Med.Chem., 41:4965-4972.

Biberger, C. and von Angerer, E. (1998): 1-Benzyl-2-phenylindole- and 1,2-diphenylindole-based antiestrogens. Estimation of agonist and antagonist activities in transfection assays. J.Steroid Biochem.Molec.Biol., 64:277-285.

Goldbrunner, M., Loidl, G., Polossek, T., Mannschreck, A., and von Angerer, E. (1997): Inhibition of tubulin polymerization by 5,6-dihydro-indolo[2,1-a]isoquinoline derivatives. J.Med.Chem., 40:3524-3533.

Hafner, F., Holler, E., and von Angerer, E. (1996): Effect of growth factors on estrogen mediated gene expression. J.Steroid.Biochem.Molec.Biol., 58:385-393.

Biberger, C. and von Angerer, E. (1996): 2-Phenylindoles with sulfur containing side chains. Estrogen receptor affinity, antiestrogenic potency, and antitumor activity. J.Steroid.Biochem.Molec.Biol., 58:31-43