Structure-Based Optimization of Novel Azepane Derivatives as PKB Inhibitors

MOLSCRIPT: a program to produce both detailed and schematic plots of protein structures

1991 • 14,222 citations

The phosphatidylinositol 3-Kinase–AKT pathway in human cancer

2002 • 5,914 citations

Cellular survival: a play in three Akts

1999 • 4,229 citations

Oncogenic kinase signalling

2001 • 3,632 citations

An extensively modified version of MolScript that includes greatly enhanced coloring capabilities

1997 • 1,724 citations

Oxidation of long-chain and related alcohols to carbonyls by dimethyl sulfoxide "activated" by oxalyl chloride

1978 • 1,616 citations

The PI3K–PDK1 connection: more than just a road to PKB

2000 • 1,563 citations

Reverse phase protein microarrays which capture disease progression show activation of pro-survival pathways at the cancer invasion front

2001 • 954 citations

AKT plays a central role in tumorigenesis

2001 • 932 citations

The Regulation and Activities of the Multifunctional Serine/Threonine Kinase Akt/PKB

1999 • 882 citations

Serine/Threonine Protein Kinases and Apoptosis

2000 • 692 citations

MAB, a generally applicable molecular force field for structure modelling in medicinal chemistry

1995 • 573 citations

Crystal structure of an activated Akt/Protein Kinase B ternary complex with GSK3-peptide and AMP-PNP

2002 • 492 citations

Molecular Mechanism for the Regulation of Protein Kinase B/Akt by Hydrophobic Motif Phosphorylation

2002 • 416 citations

Phosphotransferase and substrate binding mechanism of the cAMP-dependent protein kinase catalytic subunit from porcine heart as deduced from the 2.0 A structure of the complex with Mn2+ adenylyl imidodiphosphate and inhibitor peptide PKI(5-24).

1993 • 399 citations

(S)-13-[(Dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16,21-dimetheno- 1H,13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-dione (LY333531) and Related Analogues: Isozyme Selective Inhibitors of Protein Kinase Cβ

1996 • 336 citations

Elevated Akt Activity Protects the Prostate Cancer Cell Line LNCaP from TRAIL-induced Apoptosis

2001 • 272 citations

A Blue Luminescent Star-Shaped ZnII Complex that Can Detect Benzene This work was supported by the Natural Sciences and Engineering Research Council of Canada and the Xerox Research Foundation.

2001 • 224 citations

Novel PI Analogues Selectively Block Activation of the Pro-survival Serine/Threonine Kinase Akt

2003 • 198 citations

Akt kinases in breast cancer and the results of adjuvant therapy

2003 • 164 citations

Protein Kinase A in Complex with Rho-Kinase Inhibitors Y-27632, Fasudil, and H-1152P

2003 • 159 citations

Pro-survival Function of Akt/Protein Kinase B in Prostate Cancer Cells

2001 • 108 citations

Crystal Structure of the Potent Natural Product Inhibitor Balanol in Complex with the Catalytic Subunit of cAMP-Dependent Protein Kinase

1999 • 96 citations

Determinants of Ligand Binding to cAMP-Dependent Protein Kinase

1999 • 74 citations

Fusarium merismoides Corda NR 6356, the source of the protein kinase C inhibitor, azepinostatin. Taxonomy, yield improvement, fermentation and biological activity.

1994 • 72 citations

Molecular design and biological activity of potent and selective protein kinase inhibitors related to balanol

1995 • 64 citations

X-ray Crystal Structure of a Bisubstrate Inhibitor Bound to the Enzyme Catechol-O-methyltransferase: A Dramatic Effect of Inhibitor Preorganization on Binding Affinity We thank F. Hoffmann–La Roche for generous support of this work. We are grateful to P. Malherbe for the cloning of COMT, P. Caspers for the expression of COMT, A. Cesura for enzyme purification, B. Wipf for fermentation, and H. W. Lahm for sequencing.

2001 • 62 citations

Structure-Based Design, Synthesis, and in vitro Evaluation of Bisubstrate Inhibitors for CatecholO-Methyltransferase (COMT)

2000 • 60 citations

Bisubstrate inhibitors for the enzyme catechol-O-methyltransferase (COMT): influence of inhibitor preorganisation and linker length between the two substrate moieties on binding affinity

2002 • 53 citations

Inhibition of Protein Kinases by Balanol: Specificity within the Serine/Threonine Protein Kinase Subfamily

1999 • 52 citations

Mutants of Protein Kinase A that Mimic the ATP-binding Site of Protein Kinase B (AKT)

2003 • 50 citations

Synthesis of natural polyhydroxystilbenes

1986 • 50 citations

Synthesis and Protein Kinase Inhibitory Activity of Balanol Analogues with Modified Benzophenone Subunits

2002 • 48 citations

Palladium-catalyzed three carbon chain extension reactions with acrolein acetals. A convenient synthesis of conjugated dienals

1981 • 33 citations

Differential Effects of Phosphatidylinositol-3/Akt-Kinase Inhibition on Apoptotic Sensitization to Cytokines in LNCaP and PC-3 Prostate Cancer Cells

2001 • 23 citations

Differential and Selective Inhibition of Protein Kinase A and Protein Kinase C in Intact Cells by Balanol Congeners

1999 • 16 citations

Potent and selective PKC inhibitory 5-membered ring analogs of balanol with replacement of the carboxamide moiety

1996 • 16 citations

Preneoplasia in mouse models

2003 • 2 citations

Kinetische und strukturelle Untersuchungen zur Funktion ausgewählter konservierter Aminosäurereste der katalytischen Untereinheit C[alpha] der Proteinkinase A

2002 • 1 citations