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 …

A nonpromoting phorbol from the samoan medicinal plant Homalanthus nutans inhibits cell killing by HIV-1

…, J Ishitoya, Z Szallasi, NE Lewin… - Journal of medicinal …, 1992 - ACS Publications
Results Isolation and Identification of Prostratin. The crude organic-soluble extract of H. nutans
was subjected to a four-step solvent partition protocol. 6 The hexanesoluble and carbon …

Characterization of functional vanilloid receptors expressed by mast cells

T Bı́ró, M Maurer, S Modarres, NE Lewin… - Blood, The Journal …, 1998 - ashpublications.org
Capsaicin and its ultrapotent analog resiniferatoxin (RTX) act through specific vanilloid
receptors on sensory neurons. The C-type receptor is coupled to 45 Ca uptake, whereas the R-…

[HTML][HTML] Residues in the second cysteine-rich region of protein kinase C δ relevant to phorbol ester binding as revealed by site-directed mutagenesis

MG Kazanietz, S Wang, GWA Milne, NE Lewin… - Journal of Biological …, 1995 - Elsevier
Phorbol esters bind with high affinity to protein kinase C (PKC) isozymes as well as to two
novel receptors, n-chimaerin and Unc-13. The cysteine-rich regions present in these proteins …

Convergent assembly of highly potent analogues of bryostatin 1 via pyran annulation: bryostatin look-alikes that mimic phorbol ester function

…, W Li, CC Sanchez, N Kedei, NE Lewin… - Journal of the …, 2008 - ACS Publications
Highly potent bryostatin analogues which contain the complete bryostatin core structure
have been synthesized using a pyran annulation approach as a key strategic element. The A …

β2-Chimaerin is a novel target for diacylglycerol: binding properties and changes in subcellular localization mediated by ligand binding to its C1 domain

…, PM Blumberg, NE Lewin… - Proceedings of the …, 1999 - National Acad Sciences
The members of the chimaerin family of Rac-GTPase-activating proteins possess a single
C1 domain with high homology to those present in protein kinase C (PKC) isozymes. This …

Antineoplastic Agents. 340. Isolation and Structural Elucidation of Bryostatins 16− 18

…, CL Herald, JC Coll, Y Kamano, NE Lewin… - Journal of natural …, 1996 - ACS Publications
Separation of two trace cancer cell growth inhibitory (P388 leukemia) fractions from about
1000 kg of wet Gulf of Mexico Bugula neritina (Bryozoa) has led to the isolation of bryostatins …

Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator …

…, K Bogi, P Acs, S Modarres, NE Lewin… - Journal of medicinal …, 1997 - ACS Publications
Protein kinase C (PKC) is a complex enzyme system comprised of at least 11 isozymes that
serves to mediate numerous extracellular signals which generate lipid second messengers. …

Binding of [26-3H] bryostatin 1 and analogs to calcium-dependent and calcium-independent protein kinase C isozymes.

MG Kazanietz, NE Lewin, F Gao, GR Pettit… - Molecular …, 1994 - ASPET
In this study we explored the pattern of protein kinase C (PKC) isozyme selectivity of the
bryostatins, a unique class of PKC activators that induce only a subset of the typical phorbol …

[HTML][HTML] Characterization of the Cysteine-rich Region of the Caenorhabditiselegans Protein Unc-13 as a High Affinity Phorbol Ester Receptor: ANALYSIS OF LIGAND …

MG Kazanietz, NE Lewin, JD Bruns… - Journal of Biological …, 1995 - ASBMB
The Caenorhabditiselegans Unc-13 protein is a novel member of the phorbol ester receptor
family having a single cysteine-rich region with high homology to those present in protein …