Design a syntéza nerapalogových alosterických inhibitorů mTOR

Jan Gebrt

Bachelor's thesis

Design and synthesis of non-rapalog allosteric mTOR inhibitors

Abstract:

The Bachelor Thesis focuses on the design and synthesis of substances derived from the compound WRX606 that belongs to the group of so-called non-rapalog inhibitors of mTOR protein complex (mechanistic target of rapamycin) which affects a broad spectrum of signaling pathways in the human body. Dysregulated activity of this complex results in undesirable changes in mentioned cascades leading to the acceleration of cellur senescence and potential development of severe neurodegenerative diseases (Alzheimer’s and Parkinson’s disease) or type 2 diabetes mellitus. Non-rapalog inhibitors represent a group of substances with theoretically favourable pharmacokinetic parameters comparing to previously studied rapamycin. Therefore, further development of compounds from mentioned group and consequent testing of their biological activity can open a path to discovery of new drug candidate applicable in preventative therapy of age-related diseases and prolongation of healthspan.

Keywords

non-rapalog inhibitors, drug development, mTOR, senescence, neurodegenerative diseases, ageing

Language used: English

Date on which the thesis was submitted / produced: 9. 5. 2023

Thesis defence

• Date of defence: 6. 6. 2023
• Supervisor: Mgr. Eugenie Nepovimová, Ph.D.
• Reader: RNDr. Patrik Olekšák, PhD.

University of Hradec Králové

Faculty of Science

Bachelor programme / field:
Chemie / Toxikologie a analýza škodlivin