Further validation of strecker-type alpha-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

Mikhail Krasavin, Stanislav Kalinin, Sergey Zozulya, Anastasia Griniukova, Petro Borysko, Andrea Angeli, Claudiu T. Supuran

Результат исследований: Научные публикации в периодических изданияхстатья

Выдержка

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.


Язык оригиналаАнглийский
Страницы (с-по)165-171
ЖурналJournal of Enzyme Inhibition and Medicinal Chemistry
Том35
Номер выпуска1
Ранняя дата в режиме онлайн22 ноя 2019
DOI
СостояниеОпубликовано - 2020

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title = "Further validation of strecker-type alpha-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",
author = "Mikhail Krasavin and Stanislav Kalinin and Sergey Zozulya and Anastasia Griniukova and Petro Borysko and Andrea Angeli and Supuran, {Claudiu T.}",
year = "2020",
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",

}

Further validation of strecker-type alpha-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.

В: Journal of Enzyme Inhibition and Medicinal Chemistry, Том 35, № 1, 2020, стр. 165-171.

Результат исследований: Научные публикации в периодических изданияхстатья

TY - JOUR

T1 - Further validation of strecker-type alpha-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.

PY - 2020

Y1 - 2020

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

U2 - 10.1080/14756366.2019.1693556

DO - 10.1080/14756366.2019.1693556

M3 - статья

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 -