Ministry of Education, Science and Technological Development of the Republic of Serbia (grant No. 172009)

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Ministry of Education, Science and Technological Development of the Republic of Serbia (grant No. 172009)

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Publications

Design and synthesis of Hsp90 PROTAC degraders as potential anticancer agents

Koravović, Mladen; Tasić, Gordana; Mayasundari, Anand; Min, Jaeki; Keramatnia, Fatemeh; Fischer, Marcus; Ranković, Zoran; Savić, Vladimir

(2019)

TY  - CONF
AU  - Koravović, Mladen
AU  - Tasić, Gordana
AU  - Mayasundari, Anand
AU  - Min, Jaeki
AU  - Keramatnia, Fatemeh
AU  - Fischer, Marcus
AU  - Ranković, Zoran
AU  - Savić, Vladimir
PY  - 2019
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/4011
AB  - Hsp90 (Heat Shock Protein 90) is a chaperon protein which plays role in protein folding and maintaining protein structures. It is overexpressed in cancer and stabilizes many oncoproteins and as such represents a good target for developing anticancer drugs. The majority of approved drugs today operate by occupancy-driven pharmacology. The PROTAC approach as a strategy in creating novel drugs utilizes event-driven pharmacology in which target proteins are degraded. In recent years it emerged as very attractive and conceptually novel approach in drug discovery and development. PROTACs are molecules with two warheads connected with a linker with general structure: Ligand(protein of interest)-Linker-Ligand(E3 ligase). One warhead binds the protein of interest (POI) and the other one binds E3 ligase, while the linker brings these two parts in close proximity permitting ubiquitination and subsequent degradation of the protein. Two classes of compounds were studied: pyrrolopyrimidine and thienopyrimidine derivatives. Both classes of compounds were reported in the literature and their structure is modified in order to investigate whether linker introduction deteriorate binding of those molecules to Hsp90.
C3  - Konkurs za izbor najboljih naučno-istraživačkih radova studenata doktorskih akademskih studija
T1  - Design and synthesis of Hsp90 PROTAC degraders as potential anticancer agents
UR  - https://hdl.handle.net/21.15107/rcub_farfar_4011
ER  - 
@conference{
author = "Koravović, Mladen and Tasić, Gordana and Mayasundari, Anand and Min, Jaeki and Keramatnia, Fatemeh and Fischer, Marcus and Ranković, Zoran and Savić, Vladimir",
year = "2019",
abstract = "Hsp90 (Heat Shock Protein 90) is a chaperon protein which plays role in protein folding and maintaining protein structures. It is overexpressed in cancer and stabilizes many oncoproteins and as such represents a good target for developing anticancer drugs. The majority of approved drugs today operate by occupancy-driven pharmacology. The PROTAC approach as a strategy in creating novel drugs utilizes event-driven pharmacology in which target proteins are degraded. In recent years it emerged as very attractive and conceptually novel approach in drug discovery and development. PROTACs are molecules with two warheads connected with a linker with general structure: Ligand(protein of interest)-Linker-Ligand(E3 ligase). One warhead binds the protein of interest (POI) and the other one binds E3 ligase, while the linker brings these two parts in close proximity permitting ubiquitination and subsequent degradation of the protein. Two classes of compounds were studied: pyrrolopyrimidine and thienopyrimidine derivatives. Both classes of compounds were reported in the literature and their structure is modified in order to investigate whether linker introduction deteriorate binding of those molecules to Hsp90.",
journal = "Konkurs za izbor najboljih naučno-istraživačkih radova studenata doktorskih akademskih studija",
title = "Design and synthesis of Hsp90 PROTAC degraders as potential anticancer agents",
url = "https://hdl.handle.net/21.15107/rcub_farfar_4011"
}
Koravović, M., Tasić, G., Mayasundari, A., Min, J., Keramatnia, F., Fischer, M., Ranković, Z.,& Savić, V.. (2019). Design and synthesis of Hsp90 PROTAC degraders as potential anticancer agents. in Konkurs za izbor najboljih naučno-istraživačkih radova studenata doktorskih akademskih studija.
https://hdl.handle.net/21.15107/rcub_farfar_4011
Koravović M, Tasić G, Mayasundari A, Min J, Keramatnia F, Fischer M, Ranković Z, Savić V. Design and synthesis of Hsp90 PROTAC degraders as potential anticancer agents. in Konkurs za izbor najboljih naučno-istraživačkih radova studenata doktorskih akademskih studija. 2019;.
https://hdl.handle.net/21.15107/rcub_farfar_4011 .
Koravović, Mladen, Tasić, Gordana, Mayasundari, Anand, Min, Jaeki, Keramatnia, Fatemeh, Fischer, Marcus, Ranković, Zoran, Savić, Vladimir, "Design and synthesis of Hsp90 PROTAC degraders as potential anticancer agents" in Konkurs za izbor najboljih naučno-istraživačkih radova studenata doktorskih akademskih studija (2019),
https://hdl.handle.net/21.15107/rcub_farfar_4011 .