Turning Receptors On and Off with Intracellular Pepducins: New Insights into G-protein-coupled Receptor Drug Development

Targeting Protease-Activated Receptor-1 with Cell-Penetrating Pepducins in Lung Cancer

(2011) Jaroslaw Cisowski et al.   AMERICAN JOURNAL OF PATHOLOGY

Targeting CXCR4 with cell-penetrating pepducins in lymphoma and lymphocytic leukemia

(2011) K. O'Callaghan et al.   BLOOD

Peptide Structure Stabilization by Membrane Anchoring and its General Applicability to the Development of Potent Cell-Permeable Inhibitors

(2011) Liv Johannessen et al.   CHEMBIOCHEM

Membrane-tethered peptides patterned after the TRP domain (TRPducins) selectively inhibit TRPV1 channel activity

(2011) Pierluigi Valente et al.   FASEB JOURNAL

Direct Interaction between an Allosteric Agonist Pepducin and the Chemokine Receptor CXCR4

(2011) Jay M. Janz et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The down regulation of neutrophil oxidative metabolism by S100A8 and S100A9: Implication of the protease-activated receptor-2

(2011) Herve Y. Sroussi et al.   MOLECULAR IMMUNOLOGY

Interdicting protease-activated receptor-2-driven inflammation with cell-penetrating pepducins

(2011) L. M. Sevigny et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Identification of a Metalloprotease-Chemokine Signaling System in the Ovarian Cancer Microenvironment: Implications for Antiangiogenic Therapy

(2010) A. Agarwal et al.   CANCER RESEARCH

Activation of human monocytes by a formyl peptide receptor 2-derived pepducin

(2010) Ha Young Lee et al.   FEBS LETTERS

Structural basis of G protein–coupled receptor–G protein interactions

(2010) Jianxin Hu et al.   Nature Chemical Biology

Discovery of a CXCR4 agonist pepducin that mobilizes bone marrow hematopoietic cells

(2010) B. Tchernychev et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structures of the CXCR4 Chemokine GPCR with Small-Molecule and Cyclic Peptide Antagonists

(2010) B. Wu et al.   SCIENCE

Structure of the Human Dopamine D3 Receptor in Complex with a D2/D3 Selective Antagonist

(2010) E. Y. T. Chien et al.   SCIENCE

G Protein Subunit G 13 Binds to Integrin  IIb 3 and Mediates Integrin "Outside-In" Signaling

(2010) H. Gong et al.   SCIENCE

Luminal Cathepsin G and Protease-Activated Receptor 4

(2009) Marta Dabek et al.   AMERICAN JOURNAL OF PATHOLOGY

Triggering of proteinase-activated receptor 4 leads to joint pain and inflammation in mice

(2009) Jason J. McDougall et al.   ARTHRITIS AND RHEUMATISM

Blockade of PAR1 Signaling with Cell-Penetrating Pepducins Inhibits Akt Survival Pathways in Breast Cancer Cells and Suppresses Tumor Survival and Metastasis

(2009) E. Yang et al.   CANCER RESEARCH

Met receptor tyrosine kinase transactivation is involved in proteinase-activated receptor-2-mediated hepatocellular carcinoma cell invasion

(2009) R. Kaufmann et al.   CARCINOGENESIS

Platelet Matrix Metalloprotease-1 Mediates Thrombogenesis by Activating PAR1 at a Cryptic Ligand Site

(2009) Vishal Trivedi et al.   CELL

Fecal proteases from diarrheic-IBS and ulcerative colitis patients exert opposite effect on visceral sensitivity in mice

(2009) Anita Annaházi et al.   PAIN

The ATP-gated P2X1Receptor Plays a Pivotal Role in Activation of Aspirin-treated Platelets by Thrombin and Epinephrine

(2008) Magnus Grenegård et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Targeting a metalloprotease-PAR1 signaling system with cell-penetrating pepducins inhibits angiogenesis, ascites, and progression of ovarian cancer

(2008) A. Agarwal et al.   MOLECULAR CANCER THERAPEUTICS

Structure of a β1-adrenergic G-protein-coupled receptor

(2008) Tony Warne et al.   NATURE

Crystal structure of opsin in its G-protein-interacting conformation

(2008) Patrick Scheerer et al.   NATURE

Crystal structure of the ligand-free G-protein-coupled receptor opsin

(2008) Jung Hee Park et al.   NATURE

Structural diversity of G protein-coupled receptors and significance for drug discovery

(2008) Malin C. Lagerström et al.   NATURE REVIEWS DRUG DISCOVERY

The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist

(2008) V.-P. Jaakola et al.   SCIENCE

A Specific Cholesterol Binding Site Is Established by the 2.8 Å Structure of the Human β2-Adrenergic Receptor

(2008) Michael A. Hanson et al.   STRUCTURE