The Crystal Structure Elucidation of a Tetrapeptide Analogue of Somatostatin DOTA-Phe-D-Trp-Lys-Thr-OMe | Sciact - CRIS-system of Boreskov Institute of Catalysis

The Crystal Structure Elucidation of a Tetrapeptide Analogue of Somatostatin DOTA-Phe-D-Trp-Lys-Thr-OMe Conference Abstracts

Conference

International Workshop on Chemical Crystallography and Structural Biology “The Third Struchkov Meeting”
15-19 Nov 2021 , Online

Source

International Workshop on Chemical Crystallography and Structural Biology “The 3rd Struchkov Meeting”: Book of Abstracts. Moscow, November 15-19, 2021
Compilation, RUDN University. Moscow.2021. 100 c.

Output data

Year: 2021, Pages: 78-79 Pages count : 2

Authors

Diusenova S. ^1,2 , Arkhipov S.G. ^1,2 , Lazarenko V.A. ³ , Avdeev D. ⁵ , Khachatryan D. ⁴ , Medvedev M.G. ⁶ , Dorovatovskii P.V. ³ , Nikolaeva A. ³ , Ovchinnikov M.V. ⁵ , Sidorova M. ⁵ , Zubavichus Y.V. ¹

Affiliations

1	Boreskov Institute of Catalysis SB RAS, 630090, Novosibirsk, Russia
2	Novosibirsk State University, 630090, Novosibirsk, Russia
3	National Research Center «Kurchatov Institute», 123189, Moscow, Russia
4	Institute for Chemical Reagents and High Purity Chemical Substances of NRC «Kurchatov Institute», 107076, Moscow, Russia
5	National Medical Research Center for Cardiology, Ministry of Health of the Russian Federation, 121552, Moscow, Russia
6	N.D. Zelinsky Institute of Organic Chemistry RAS, 119991, Moscow, Russia

Herewith, we report for the very first time the crystal structure of tetrapeptide FwKT (PheD-Trp-Lys-Thr), which is considered to represent an epitope for biomedically relevant hormone somatostatin. This peptide is interesting because all drugs based on somatostatin analogs have been developed on the basis of its pharmacophore sequence Phe-Trp-Lys-Thr which is responsible for their binding to somatostatin receptors (sstr), the overexpression of which is observed in tumor cells. The target molecule was successfully crystalized, solved and refined as a conjugate of the tetrapeptide moiety bearing a protective group DOTA (1,4,7,10-tetraazacyclododecane - 1,4,7,10-tetraacetic acid) at the N-terminus and methylated at the O-terminus. The combination of a hormone active site and a powerful chelator make the substance a highly prospective targeted drug delivery system.

Diusenova S. , Arkhipov S.G. , Lazarenko V.A. , Avdeev D. , Khachatryan D. , Medvedev M.G. , Dorovatovskii P.V. , Nikolaeva A. , Ovchinnikov M.V. , Sidorova M. , Zubavichus Y.V.
The Crystal Structure Elucidation of a Tetrapeptide Analogue of Somatostatin DOTA-Phe-D-Trp-Lys-Thr-OMe
In compilation International Workshop on Chemical Crystallography and Structural Biology “The 3rd Struchkov Meeting”: Book of Abstracts. Moscow, November 15-19, 2021. – RUDN University., 2021. – C.78-79. РИНЦ

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