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

The Crystal Structure Elucidation of a Tetrapeptide Analog of Somatostatin DOTA-Phe-D-Trp-Lys-Thr-OMe Full article

Journal

Crystals
ISSN: 2073-4352

Output data

Year: 2021, Volume: 12, Number: 1, Article number : 12, Pages count : DOI: 10.3390/cryst12010012

Authors

Diusenova Sabina ^1,2 , Arkhipov Sergey ^2,3,4 , Avdeev Dmitry ⁵ , Dorovatovskii Pavel ⁶ , Khachatryan Derenik ⁷ , Lazarenko Vladimir ⁶ , Medvedev Michael ⁸ , Nikolaeva Alena ⁶ , Ovchinnikov Mikhail ⁵ , Sidorova Maria ⁵ , Zubavichus Yan ⁴

Affiliations

1	Boreskov Institute of Catalysis SB RAS, 630090 Novosibirsk, Russia
2	Faculty of Natural Sciences, Department of Solid State Chemistry, Novosibirsk State University, 630090 Novosibirsk, Russia
3	State Research Center of Virology and Biotechnology VECTOR of the Federal Service for Surveillance in Consumer Rights Protection and Human Well-being (FSRI SRC VB VECTOR), 630559 Koltsovo, Russia
4	Synchrotron Radiation Facility SKIF, G.K. Boreskov Institute of Catalysis SB RAS, 630559 Koltsovo, Russia
5	National Medical Research Center for Cardiology, Ministry of Health of the Russian Federation, 121552 Moscow, Russia
6	National Research Center, Kurchatov Institute, 123189 Moscow, Russia
7	Institute for Chemical Reagents and High Purity Chemical Substances of NRC, 107076 Moscow, Russia
8	N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, 119991 Moscow, Russia

Herewith, we report for the first time the crystal structure of tetrapeptide FwKT (Phe-D-Trp-Lys-Thr), which is considered to represent an epitope for biomedically relevant hormone somatostatin. The target molecule was successfully crystalized, solved and refined as a conjugate of the tetrapeptide moiety bearing a protective group DOTA 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, especially for peptide receptor radionuclide therapy (PRRT) applications.

Diusenova S. , Arkhipov S. , Avdeev D. , Dorovatovskii P. , Khachatryan D. , Lazarenko V. , Medvedev M. , Nikolaeva A. , Ovchinnikov M. , Sidorova M. , Zubavichus Y.
The Crystal Structure Elucidation of a Tetrapeptide Analog of Somatostatin DOTA-Phe-D-Trp-Lys-Thr-OMe
Crystals. 2021. V.12. N1. 12 . DOI: 10.3390/cryst12010012 WOS Scopus OpenAlex

≡ Web of science:	WOS:000758173200001
≡ Scopus:	2-s2.0-85121751393
≡ OpenAlex:	W4200335960