Development of novel non-peptide HIV-1 protease inhibitors
Prof. Dr. Andreas Hilgeroth, Lisa Marie Seitz
In recent years, ongoing research in the field of HIV therapy has led to significant progress in the development of active substances that effectively inhibit the replication of the virus.
One promising approach is the development of non-peptide HIV-1 protease inhibitors, which represent an alternative structure to traditional peptide-based inhibitors and have the potential to improve the treatment of HIV infections.
Among these innovative classes of substances, dimerized 1,4-dihydropyridines occupy a special position, as the 1,4-dihydropyridine structure can excellently inhibit HIV-1 proteases due to its electronic structure and conformation.
Our working group is intensively involved in the following research areas:
- Investigation of structure/activity relationships of new 1,4-dihydropyridines
- X-ray structure analyses of HIV-1 protease and inhibitors
- Molecular modeling for lead structure optimization
- In vitro testing for HIV-1 protease inhibition
Literatur: A. Hilgeroth et al., J. Comput.-Aided Mol. Design 13, 233-242 (1999);
A. Hilgeroth, M. Wiese, A. Billich, J. Med. Chem. 42, 4729-4732 (1999);
A. Hilgeroth, Min. Rev. Med. Chem. 2, 235-247 (2002);
A. Hilgeroth et al., ChemBioChem 9, 874-878 (2008).