Literature DB >> 15025445

A highly potent and selective PKCalpha inhibitor generated via combinatorial modification of a peptide scaffold.

Jung Hwan Lee1, Sandip K Nandy, David S Lawrence.   

Abstract

A potent and highly selective inhibitor of protein kinase C alpha has been generated via the combinatorial modification of a consensus sequence peptide. The inhibitor displays a Ki of 800 pM versus variable peptide substrate and good selectivity versus other members of the PKC family, including PKCbeta (385-fold), PKCgamma (580-fold), PKCdelta (2730-fold), PKCepsilon (600-fold), PKCeta (1310-fold), PKCtheta (1210-fold), PKCiota (940-fold), and PKCzeta (640-fold). The parallel synthesis strategy employed is easily automated and straightforward to implement.

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Year:  2004        PMID: 15025445     DOI: 10.1021/ja037300b

Source DB:  PubMed          Journal:  J Am Chem Soc        ISSN: 0002-7863            Impact factor:   15.419


  8 in total

1.  Metabolism of peptide reporters in cell lysates and single cells.

Authors:  Angela Proctor; Qunzhao Wang; David S Lawrence; Nancy L Allbritton
Journal:  Analyst       Date:  2012-02-07       Impact factor: 4.616

2.  Visual snapshots of intracellular kinase activity at the onset of mitosis.

Authors:  Zhaohua Dai; Natalya G Dulyaninova; Sanjai Kumar; Anne R Bresnick; David S Lawrence
Journal:  Chem Biol       Date:  2007-11

3.  Development of an intracellularly acting inhibitory peptide selective for PKN.

Authors:  Kazuhiro Shiga; Kentaro Takayama; Shiroh Futaki; Jessica E Hutti; Lewis C Cantley; Katsuko Ueki; Yoshitaka Ono; Hideyuki Mukai
Journal:  Biochem J       Date:  2009-12-23       Impact factor: 3.857

Review 4.  The chemical biology of protein phosphorylation.

Authors:  Mary Katherine Tarrant; Philip A Cole
Journal:  Annu Rev Biochem       Date:  2009       Impact factor: 23.643

5.  Protein kinase Calpha mediates a novel form of plasticity in the accessory olfactory bulb.

Authors:  C Dong; D W Godwin; P A Brennan; A N Hegde
Journal:  Neuroscience       Date:  2009-07-04       Impact factor: 3.590

6.  SAR by oxime-containing peptide libraries: application to Tsg101 ligand optimization.

Authors:  Fa Liu; Andrew G Stephen; Abdul A Waheed; M Javad Aman; Eric O Freed; Robert J Fisher; Terrence R Burke
Journal:  Chembiochem       Date:  2008-08-11       Impact factor: 3.164

7.  SRC kinase regulation in progressively invasive cancer.

Authors:  Weichen Xu; Nancy Allbritton; David S Lawrence
Journal:  PLoS One       Date:  2012-11-07       Impact factor: 3.240

Review 8.  PKC in Regenerative Therapy: New Insights for Old Targets.

Authors:  Marta Rui; Rita Nasti; Emanuele Bignardi; Serena Della Volpe; Giacomo Rossino; Daniela Rossi; Simona Collina
Journal:  Pharmaceuticals (Basel)       Date:  2017-05-18
  8 in total

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