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Identification and Characterization of an Irreversible Inhibitor of CDK2
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- Anscombe, Elizabeth (författare)
- Univ Oxford, Dept Biochem, Oxford OX1 3QU, England.
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- Meschini, Elisa (författare)
- Newcastle Univ, Sch Chem, Northern Inst Canc Res, Newcastle Canc Ctr, Newcastle Upon Tyne NE1 7RU, Tyne & Wear, England.
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- Mora-Vidal, Regina (författare)
- Newcastle Univ, Newcastle Canc Ctr, Northern Inst Canc Res, Sch Med, Newcastle Upon Tyne NE2 4HH, Tyne & Wear, England.
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- Martin, Mathew P. (författare)
- Newcastle Univ, Newcastle Canc Ctr, Northern Inst Canc Res, Sch Med, Newcastle Upon Tyne NE2 4HH, Tyne & Wear, England.
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- Staunton, David (författare)
- Univ Oxford, Dept Biochem, Oxford OX1 3QU, England.
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- Geitmann, Matthis (författare)
- Uppsala universitet,Institutionen för kemi - BMC
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- Danielson, U. Helena (författare)
- Uppsala universitet,Institutionen för kemi - BMC
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- Stanley, Will A. (författare)
- Newcastle Univ, Newcastle Canc Ctr, Northern Inst Canc Res, Sch Med, Newcastle Upon Tyne NE2 4HH, Tyne & Wear, England.
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- Wang, Lan Z. (författare)
- Newcastle Univ, Newcastle Canc Ctr, Northern Inst Canc Res, Sch Med, Newcastle Upon Tyne NE2 4HH, Tyne & Wear, England.
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- Reuillon, Tristan (författare)
- Newcastle Univ, Sch Chem, Northern Inst Canc Res, Newcastle Canc Ctr, Newcastle Upon Tyne NE1 7RU, Tyne & Wear, England.
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- Golding, Bernard T. (författare)
- Newcastle Univ, Sch Chem, Northern Inst Canc Res, Newcastle Canc Ctr, Newcastle Upon Tyne NE1 7RU, Tyne & Wear, England.
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- Cano, Celine (författare)
- Newcastle Univ, Sch Chem, Northern Inst Canc Res, Newcastle Canc Ctr, Newcastle Upon Tyne NE1 7RU, Tyne & Wear, England.
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- Newell, David R. (författare)
- Newcastle Univ, Newcastle Canc Ctr, Northern Inst Canc Res, Sch Med, Newcastle Upon Tyne NE2 4HH, Tyne & Wear, England.
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- Noble, Martin E. M. (författare)
- Univ Oxford, Dept Biochem, Oxford OX1 3QU, England.
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- Wedge, Stephen R. (författare)
- Newcastle Univ, Newcastle Canc Ctr, Northern Inst Canc Res, Sch Med, Newcastle Upon Tyne NE2 4HH, Tyne & Wear, England.
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- Endicott, Jane A. (författare)
- Univ Oxford, Dept Biochem, Oxford OX1 3QU, England.
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- Griffin, Roger J. (författare)
- Newcastle Univ, Sch Chem, Northern Inst Canc Res, Newcastle Canc Ctr, Newcastle Upon Tyne NE1 7RU, Tyne & Wear, England.
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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
- Engelska.
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Ingår i: Chemistry and Biology. - : Elsevier BV. - 1074-5521 .- 1879-1301. ; 22:9, s. 1159-1164
- Relaterad länk:
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https://doi.org/10.1...
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https://uu.diva-port... (primary) (Raw object)
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https://doi.org/10.1...
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- 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.
Ämnesord
- NATURVETENSKAP -- Biologi -- Biokemi och molekylärbiologi (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences -- Biochemistry and Molecular Biology (hsv//eng)
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- art (ämneskategori)
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Till lärosätets databas
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Anscombe, Elizab ...
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Meschini, Elisa
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Mora-Vidal, Regi ...
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Martin, Mathew P ...
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Staunton, David
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Geitmann, Matthi ...
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visa fler...
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Danielson, U. He ...
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Stanley, Will A.
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Wang, Lan Z.
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Reuillon, Trista ...
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Golding, Bernard ...
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Cano, Celine
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Newell, David R.
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Noble, Martin E. ...
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Wedge, Stephen R ...
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Endicott, Jane A ...
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Griffin, Roger J ...
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- NATURVETENSKAP
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NATURVETENSKAP
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och Biologi
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och Biokemi och mole ...
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Chemistry and Bi ...
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Uppsala universitet