A Chemical Epitope-Targeting Strategy for Protein Capture Agents: The Serine 474 Epitope of the Kinase Akt2

Nag, Arundhati and Das, Samir and Yu, Mary Beth and Deyle, Kaycie M. and Millward, Steven W. and Heath, James R. (2013) A Chemical Epitope-Targeting Strategy for Protein Capture Agents: The Serine 474 Epitope of the Kinase Akt2. Angewandte Chemie International Edition, 52 (52). pp. 13975-13979. ISSN 1433-7851. PMCID PMC4059071. doi:10.1002/anie.201305882. https://resolver.caltech.edu/CaltechAUTHORS:20131204-154453202

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Abstract

Target and click: Peptide ligands targeted to the C-terminal motif of the kinase Akt2 were obtained by combining phosphate recognition of a dinuclear zinc(II) complex with in situ click chemistry to target this epitope. The peptide ligands (shown as XXXXX) selectively bind the C-terminal polypeptide of Akt2, and are selective for Akt2 relative to the Akt1 and Akt3 isoforms. The ligands differentially modulate Akt2 activity.

Item Type:

Article

Related URLs:

URL	URL Type	Description
http://dx.doi.org/10.1002/anie.201305882	DOI	Article
http://onlinelibrary.wiley.com/doi/10.1002/anie.201305882/abstract	Publisher	Article
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4059071/	PubMed Central	Article

ORCID:

Author	ORCID
Heath, James R.	0000-0001-5356-4385

Additional Information:

© 2013 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim. Received: July 7, 2013; Revised: September 23, 2013. Article first published online: 19 Nov. 2013. This work was supported by the Institute for Collaborative Biotechnologies through grant W911NF-09-0001 from the U.S. Army Research Office. Additional personnel or facilities support from the National Cancer Institute (5U54 CA119347: J.R.H. PI), the Grand Duchy of Luxembourg, and the Bill and Melinda Gates Foundation is acknowledged.

Funders:

Funding Agency	Grant Number
Army Research Office (ARO)	W911NF-09-0001
NIH	5U54 CA119347
Grand Duchy of Luxembourg	UNSPECIFIED
Bill and Melinda Gates Foundation	UNSPECIFIED
National Cancer Institute	UNSPECIFIED

Subject Keywords:

click chemistry; drug design; inhibitors; kinases; peptides

Issue or Number:

PubMed Central ID:

PMC4059071

DOI:

10.1002/anie.201305882

Record Number:

CaltechAUTHORS:20131204-154453202

Persistent URL:

https://resolver.caltech.edu/CaltechAUTHORS:20131204-154453202

Official Citation:

Nag, A., Das, S., Yu, M. B., Deyle, K. M., Millward, S. W. and Heath, J. R. (2013), A Chemical Epitope-Targeting Strategy for Protein Capture Agents: The Serine 474 Epitope of the Kinase Akt2. Angew. Chem. Int. Ed., 52: 13975–13979. doi: 10.1002/anie.201305882

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No commercial reproduction, distribution, display or performance rights in this work are provided.

ID Code:

42839

Collection:

CaltechAUTHORS

Deposited By:

Tony Diaz

Deposited On:

05 Dec 2013 00:38

Last Modified:

10 Nov 2021 16:29

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