Abstract
We report the rational design of novel neurotensin mimetics through use of the Multiple Template Approach. This approach is based on our notion that a flexible peptide can be replaced by a partially flexible molecule, identified through testing a comparatively small number of molecules possessing a different intrinsic availability of conformations of the native peptide. The Multiple Template Approach has culminated in the discovery of a pharmacologically unprecedented agent, which behaves as a neurotensin antagonist at low concentration and as a full neurotensin agonist at high concentration.
Original language | English (US) |
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Pages (from-to) | 433-440 |
Number of pages | 8 |
Journal | Journal of Computer-Aided Molecular Design |
Volume | 8 |
Issue number | 4 |
DOIs | |
State | Published - Aug 1994 |
Keywords
- Drug design
- Multiple Template Approach
- Neurotensin agonist
- Neurotensin antagonist
ASJC Scopus subject areas
- Drug Discovery
- Computer Science Applications
- Physical and Theoretical Chemistry