Oxyl radicals, redox-sensitive signalling cascades and antioxidants

M Genestra - Cellular signalling, 2007 - Elsevier
Oxidative stress is an increase in the reduction potential or a large decrease in the reducing
capacity of the cellular redox couples. A particularly destructive aspect of oxidative stress is …

Kinomics—structural biology and chemogenomics of kinase inhibitors and targets

M Vieth, RE Higgs, DH Robertson, M Shapiro… - … et Biophysica Acta (BBA …, 2004 - Elsevier
Classifying kinases based entirely on small molecule selectivity data is a new approach to
drug discovery that allows scientists to understand relationships between targets. This …

Characterization of the interaction of ingenol 3-angelate with protein kinase C

N Kedei, DJ Lundberg, A Toth, P Welburn, SH Garfield… - Cancer research, 2004 - AACR
Abstract Ingenol 3-angelate (I3A) is one of the active ingredients in Euphorbia peplus, which
has been used in traditional medicine. Here, we report the initial characterization of I3A as a …

Diacylglycerol (DAG)-lactones, a new class of protein kinase C (PKC) agonists, induce apoptosis in LNCaP prostate cancer cells by selective activation of PKCα

ML Garcia-Bermejo, FC Leskow, T Fujii, Q Wang… - Journal of Biological …, 2002 - ASBMB
Phorbol esters, the archetypical (PKC) activators, induce apoptosis in androgen-sensitive
LNCaP prostate cancer cells. In this study we evaluate the effect of a novel class of PKC …

Automated docking of ligands to an artificial active site: augmenting crystallographic analysis with computer modeling

RJ Rosenfeld, DS Goodsell, RA Musah… - Journal of Computer …, 2003 - Springer
The W191G cavity of cytochrome c peroxidase is useful as a model system for introducing
small molecule oxidation in an artificially created cavity. A set of small, cyclic, organic cations …

Synthetic diacylglycerols (DAG) and DAG-lactones as activators of protein kinase C (PK-C)

VE Marquez, PM Blumberg - Accounts of chemical research, 2003 - ACS Publications
The central role of protein kinase C (PK-C) in cellular signal transduction has established it
as an important therapeutic target for cancer and other diseases. We have developed a …

Wealth of opportunity-the C1 domain as a target for drug development

PM Blumberg, N Kedei, NE Lewin, D Yang… - Current drug …, 2008 - ingentaconnect.com
The diacylglycerol-responsive C1 domains of protein kinase C and of the related classes of
signaling proteins represent highly attractive targets for drug development. The signaling …

Dual role of prostratin in inhibition of infection and reactivation of human immunodeficiency virus from latency in primary blood lymphocytes and lymphoid tissue

A Biancotto, JC Grivel, F Gondois-Rey… - Journal of …, 2004 - Am Soc Microbiol
To design strategies to purge latent reservoirs of human immunodeficiency virus type 1 (HIV-
1), we investigated mechanisms by which a non-tumor-promoting phorbol ester, prostratin …

Design, synthesis, and biological activity of isophthalic acid derivatives targeted to the C1 domain of protein kinase C

GB af Gennas, V Talman, O Aitio… - Journal of medicinal …, 2009 - ACS Publications
Protein kinase C (PKC) is a widely studied molecular target for the treatment of cancer and
other diseases. We have approached the issue of modifying PKC function by targeting the …

Protein kinase C regulates mitochondrial targeting of Nur77 and its family member Nor‐1 in thymocytes undergoing apoptosis

J Thompson, ML Burger, H Whang… - European journal of …, 2010 - Wiley Online Library
Nur77 orphan steroid receptor and its family member Nor‐1 are required for apoptosis of
developing T cells. In thymocytes, signals from the TCR complex induce Nur77 and Nor‐1 …