Research output: Contribution to journal › Article › peer-review
The crystal structure elucidation of a tetrapeptide analog of somatostatin dota-phe-d-trp-lys-thr-ome. / Diusenova, Sabina; Arkhipov, Sergey; Avdeev, Dmitry et al.
In: Crystals, Vol. 12, No. 1, 12, 01.2022.Research output: Contribution to journal › Article › peer-review
}
TY - JOUR
T1 - The crystal structure elucidation of a tetrapeptide analog of somatostatin dota-phe-d-trp-lys-thr-ome
AU - Diusenova, Sabina
AU - Arkhipov, Sergey
AU - Avdeev, Dmitry
AU - Dorovatovskii, Pavel
AU - Khachatryan, Derenik
AU - Lazarenko, Vladimir
AU - Medvedev, Michael
AU - Nikolaeva, Alena
AU - Ovchinnikov, Mikhail
AU - Sidorova, Maria
AU - Zubavichus, Yan
N1 - Funding Information: Funding: This research was partially funded by Russian Ministry of Science and Education via the budget project of SRF SKIF, Boreskov Institute of Catalysis and by the Ministry of Science and Higher Education of the Russian Federation in the implementation of the research program “Use of synchrotron radiation for virologic research” within the framework of the Federal Scientific and Technical Program for the Development of Synchrotron and Neutron Research and Research Infrastructure for 2019–2027 (Agreement No. 075-15-2021-1355 (12 October 2021)). Publisher Copyright: © 2021 by the authors. Licensee MDPI, Basel, Switzerland.
PY - 2022/1
Y1 - 2022/1
N2 - 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.
AB - 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.
KW - Analogue
KW - DOTA
KW - PRRT
KW - Somatostatin
KW - XRD
UR - http://www.scopus.com/inward/record.url?scp=85121751393&partnerID=8YFLogxK
U2 - 10.3390/cryst12010012
DO - 10.3390/cryst12010012
M3 - Article
AN - SCOPUS:85121751393
VL - 12
JO - Crystals
JF - Crystals
SN - 2073-4352
IS - 1
M1 - 12
ER -
ID: 35175484