Standard

Further validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors : hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement. / Krasavin, Mikhail; Kalinin, Stanislav; Zozulya, Sergey; Griniukova, Anastasia; Borysko, Petro; Angeli, Andrea; Supuran, Claudiu T.

In: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol. 35, No. 1, 01.01.2020, p. 165-171.

Research output: Contribution to journal › Article › peer-review

Harvard

Krasavin, M, Kalinin, S, Zozulya, S, Griniukova, A, Borysko, P, Angeli, A & Supuran, CT 2020, 'Further validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors: hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement', Journal of Enzyme Inhibition and Medicinal Chemistry, vol. 35, no. 1, pp. 165-171. https://doi.org/10.1080/14756366.2019.1693556

APA

Krasavin, M., Kalinin, S., Zozulya, S., Griniukova, A., Borysko, P., Angeli, A., & Supuran, C. T. (2020). Further validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors: hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement. Journal of Enzyme Inhibition and Medicinal Chemistry, 35(1), 165-171. https://doi.org/10.1080/14756366.2019.1693556

Vancouver

Krasavin M, Kalinin S, Zozulya S, Griniukova A, Borysko P, Angeli A et al. Further validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors: hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement. Journal of Enzyme Inhibition and Medicinal Chemistry. 2020 Jan 1;35(1):165-171. https://doi.org/10.1080/14756366.2019.1693556

Author

Krasavin, Mikhail ; Kalinin, Stanislav ; Zozulya, Sergey ; Griniukova, Anastasia ; Borysko, Petro ; Angeli, Andrea ; Supuran, Claudiu T. / Further validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors : hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement. In: Journal of Enzyme Inhibition and Medicinal Chemistry. 2020 ; Vol. 35, No. 1. pp. 165-171.

BibTeX

@article{8d9e892ace844ac7a05d49ecae67a1a3,
title = "Further validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors: hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement",
abstract = "Testing of an expanded, 800-compound set of analogues of the earlier described Strecker-type alpha-aminonitriles (selected from publicly available Enamine Ltd. Screening Collection) in thermal shift assay against bovine carbonic anhydrase (bCA) led to further validation of this new class of inhibitors and identification a new, refined chemotype represented by inhibitors with 10-improved potency.",
keywords = "Differential scanning fluorimetry, thermal shift assay, protein affinity, carbonic anhydrase II, AFFINITY, DESIGN, SITE, Humans, Structure-Activity Relationship, Fluorometry, Dose-Response Relationship, Drug, Animals, Nitriles/chemical synthesis, Carbonic Anhydrase Inhibitors/chemical synthesis, Cattle, Molecular Structure, Carbonic Anhydrase II/antagonists & inhibitors, Drug Evaluation, Preclinical",
author = "Mikhail Krasavin and Stanislav Kalinin and Sergey Zozulya and Anastasia Griniukova and Petro Borysko and Andrea Angeli and Supuran, {Claudiu T.}",
note = "Funding Information: This research was supported by the Russian Federation Government Megagrant 14.W03.031.0025. The authors are grateful to Dr. Vladimir Sharoyko for helpful discussions regarding the TSA data interpretation. We thank the Research Centre for Magnetic Resonance of Saint Petersburg State University Research Park for screening compound quality control using 1H NMR spectroscopy. Publisher Copyright: {\textcopyright} 2019, {\textcopyright} 2019 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group.",
year = "2020",
month = jan,
day = "1",
doi = "10.1080/14756366.2019.1693556",
language = "Английский",
volume = "35",
pages = "165--171",
journal = "Journal of Enzyme Inhibition and Medicinal Chemistry",
issn = "1475-6366",
publisher = "Taylor & Francis",
number = "1",

}

RIS

TY - JOUR

T1 - Further validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors

T2 - hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement

AU - Krasavin, Mikhail

AU - Kalinin, Stanislav

AU - Zozulya, Sergey

AU - Griniukova, Anastasia

AU - Borysko, Petro

AU - Angeli, Andrea

AU - Supuran, Claudiu T.

N1 - Funding Information: This research was supported by the Russian Federation Government Megagrant 14.W03.031.0025. The authors are grateful to Dr. Vladimir Sharoyko for helpful discussions regarding the TSA data interpretation. We thank the Research Centre for Magnetic Resonance of Saint Petersburg State University Research Park for screening compound quality control using 1H NMR spectroscopy. Publisher Copyright: © 2019, © 2019 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group.

PY - 2020/1/1

Y1 - 2020/1/1

N2 - Testing of an expanded, 800-compound set of analogues of the earlier described Strecker-type alpha-aminonitriles (selected from publicly available Enamine Ltd. Screening Collection) in thermal shift assay against bovine carbonic anhydrase (bCA) led to further validation of this new class of inhibitors and identification a new, refined chemotype represented by inhibitors with 10-improved potency.

AB - Testing of an expanded, 800-compound set of analogues of the earlier described Strecker-type alpha-aminonitriles (selected from publicly available Enamine Ltd. Screening Collection) in thermal shift assay against bovine carbonic anhydrase (bCA) led to further validation of this new class of inhibitors and identification a new, refined chemotype represented by inhibitors with 10-improved potency.

KW - Differential scanning fluorimetry

KW - thermal shift assay

KW - protein affinity

KW - carbonic anhydrase II

KW - AFFINITY

KW - DESIGN

KW - SITE

KW - Humans

KW - Structure-Activity Relationship

KW - Fluorometry

KW - Dose-Response Relationship, Drug

KW - Animals

KW - Nitriles/chemical synthesis

KW - Carbonic Anhydrase Inhibitors/chemical synthesis

KW - Cattle

KW - Molecular Structure

KW - Carbonic Anhydrase II/antagonists & inhibitors

KW - Drug Evaluation, Preclinical

UR - http://www.scopus.com/inward/record.url?scp=85075540753&partnerID=8YFLogxK

UR - https://www.mendeley.com/catalogue/6134a708-b0b1-3207-bd5c-e428d6d5ffdd/

U2 - 10.1080/14756366.2019.1693556

DO - 10.1080/14756366.2019.1693556

M3 - статья

C2 - 31752557

VL - 35

SP - 165

EP - 171

JO - Journal of Enzyme Inhibition and Medicinal Chemistry

JF - Journal of Enzyme Inhibition and Medicinal Chemistry

SN - 1475-6366

IS - 1

ER -

ID: 49497360