Identification and Characterization of an Irreversible Inhibitor of CDK2

↓ Direkt till sidans innehåll
↓ Direkt till sidans sekundära innehåll (sidomenyn)

Search: id:"swepub:oai:DiVA.org:uu-268711" > Identification and ...

1 of 1
Previous record
Next record
To hitlist

Identification and Characterization of an Irreversible Inhibitor of CDK2

Anscombe, Elizabeth (author): Univ Oxford, Dept Biochem, Oxford OX1 3QU, England.

Meschini, Elisa (author): Newcastle Univ, Sch Chem, Northern Inst Canc Res, Newcastle Canc Ctr, Newcastle Upon Tyne NE1 7RU, Tyne & Wear, England.

Mora-Vidal, Regina (author): Newcastle Univ, Newcastle Canc Ctr, Northern Inst Canc Res, Sch Med, Newcastle Upon Tyne NE2 4HH, Tyne & Wear, England.

Martin, Mathew P. (author): Newcastle Univ, Newcastle Canc Ctr, Northern Inst Canc Res, Sch Med, Newcastle Upon Tyne NE2 4HH, Tyne & Wear, England.

Staunton, David (author): Univ Oxford, Dept Biochem, Oxford OX1 3QU, England.

Geitmann, Matthis (author): Uppsala universitet,Institutionen för kemi - BMC

Danielson, U. Helena (author): Uppsala universitet,Institutionen för kemi - BMC

Stanley, Will A. (author): Newcastle Univ, Newcastle Canc Ctr, Northern Inst Canc Res, Sch Med, Newcastle Upon Tyne NE2 4HH, Tyne & Wear, England.

Wang, Lan Z. (author): Newcastle Univ, Newcastle Canc Ctr, Northern Inst Canc Res, Sch Med, Newcastle Upon Tyne NE2 4HH, Tyne & Wear, England.

Reuillon, Tristan (author): Newcastle Univ, Sch Chem, Northern Inst Canc Res, Newcastle Canc Ctr, Newcastle Upon Tyne NE1 7RU, Tyne & Wear, England.

Golding, Bernard T. (author): Newcastle Univ, Sch Chem, Northern Inst Canc Res, Newcastle Canc Ctr, Newcastle Upon Tyne NE1 7RU, Tyne & Wear, England.

Cano, Celine (author): Newcastle Univ, Sch Chem, Northern Inst Canc Res, Newcastle Canc Ctr, Newcastle Upon Tyne NE1 7RU, Tyne & Wear, England.

Newell, David R. (author): Newcastle Univ, Newcastle Canc Ctr, Northern Inst Canc Res, Sch Med, Newcastle Upon Tyne NE2 4HH, Tyne & Wear, England.

Noble, Martin E. M. (author): Univ Oxford, Dept Biochem, Oxford OX1 3QU, England.

Wedge, Stephen R. (author): Newcastle Univ, Newcastle Canc Ctr, Northern Inst Canc Res, Sch Med, Newcastle Upon Tyne NE2 4HH, Tyne & Wear, England.

Endicott, Jane A. (author): Univ Oxford, Dept Biochem, Oxford OX1 3QU, England.

Griffin, Roger J. (author): Newcastle Univ, Sch Chem, Northern Inst Canc Res, Newcastle Canc Ctr, Newcastle Upon Tyne NE1 7RU, Tyne & Wear, England.

show less...

Univ Oxford, Dept Biochem, Oxford OX1 3QU, England Newcastle Univ, Sch Chem, Northern Inst Canc Res, Newcastle Canc Ctr, Newcastle Upon Tyne NE1 7RU, Tyne & Wear, England. (creator_code:org_t)

Elsevier BV, 2015
2015
English.
In: Chemistry and Biology. - : Elsevier BV. - 1074-5521 .- 1879-1301. ; 22:9, s. 1159-1164

Related links:: https://doi.org/10.1...; show more...; https://uu.diva-port... (primary) (Raw object); https://doi.org/10.1...; https://urn.kb.se/re...; https://doi.org/10.1...; show less...

Journal article (peer-reviewed)

Abstract Subject headings

Irreversible inhibitors that modify cysteine or lysine residues within a protein kinase ATP binding site offer, through their distinctive mode of action, an alternative to ATP-competitive agents. 4-((6-(Cyclo-hexylmethoxy)-9H-purin-2-yl) amino) benzenesulfonamide (NU6102) is a potent and selective ATP-competitive inhibitor of CDK2 in which the sulfonamide moiety is positioned close to a pair of lysine residues. Guided by the CDK2/NU6102 structure, we designed 6-(cyclohexylmethoxy)-N-(4-(vinylsulfonyl) phenyl)-9H- purin-2-amine (NU6300), which binds covalently to CDK2 as shown by a co-complex crystal structure. Acute incubation with NU6300 produced a durable inhibition of Rb phosphorylation in SKUT-1B cells, consistent with it acting as an irreversible CDK2 inhibitor. NU6300 is the first covalent CDK2 inhibitor to be described, and illustrates the potential of vinyl sulfones for the design of more potent and selective compounds.

Find in a library

Chemistry and Biology (Search for host publication in LIBRIS)

To the university's database

1 of 1
Previous record
Next record
To hitlist

Find more in SwePub

By the author/editor: Anscombe, Elizab ...; Meschini, Elisa; Mora-Vidal, Regi ...; Martin, Mathew P ...; Staunton, David; Geitmann, Matthi ...; show more...; Danielson, U. He ...; Stanley, Will A.; Wang, Lan Z.; Reuillon, Trista ...; Golding, Bernard ...; Cano, Celine; Newell, David R.; Noble, Martin E. ...; Wedge, Stephen R ...; Endicott, Jane A ...; Griffin, Roger J ...; show less...

About the subject

NATURAL SCIENCES: NATURAL SCIENCES; and Biological Scien ...; and Biochemistry and ...

Articles in the publication: Chemistry and Bi ...

By the university: Uppsala University

Search outside SwePub

Extend your search to:: Google; Google Book Search; Google Scholar

Kungliga biblioteket hanterar dina personuppgifter i enlighet med EU:s dataskyddsförordning (2018), GDPR. Läs mer om hur det funkar här.
Så här hanterar KB dina uppgifter vid användning av denna tjänst.

LIBRIS.kb.se

Identification and Characterization of an Irreversible Inhibitor of CDK2

Subject headings

Publication and Content Type

Find in a library

To the university's database

Find more in SwePub

Search outside SwePub