Allosteric Activation of a G Protein-coupled Receptor with Cell-penetrating Receptor Mimetics

Development and Characterization of Pepducins as Gs-biased Allosteric Agonists

(2014) Richard Carr et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structure of a Class C GPCR Metabotropic Glutamate Receptor 1 Bound to an Allosteric Modulator

(2014) H. Wu et al.   SCIENCE

Recent developments in biased agonism

(2013) James W Wisler et al.   CURRENT OPINION IN CELL BIOLOGY

Palmitoylation of Protease-activated Receptor-1 Regulates Adaptor Protein Complex-2 and -3 Interaction with Tyrosine-based Motifs and Endocytic Sorting

(2013) Isabel Canto et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Activation and allosteric modulation of a muscarinic acetylcholine receptor

(2013) Andrew C. Kruse et al.   NATURE

Emerging paradigms in GPCR allostery: implications for drug discovery

(2013) Denise Wootten et al.   NATURE REVIEWS DRUG DISCOVERY

Crystal structure of oligomeric β1-adrenergic G protein–coupled receptors in ligand-free basal state

(2013) Jianyun Huang et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

FRET-based imaging of transbilayer movement of pepducin in living cells by novel intracellular bioreductively activatable fluorescent probes

(2013) Mieko Tsuji et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Pepducin targeting the C-X-C chemokine receptor type 4 acts as a biased agonist favoring activation of the inhibitory G protein

(2013) J. Quoyer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Restructuring G-Protein- Coupled Receptor Activation

(2012) Martin Audet et al.   CELL

Suppression of Arterial Thrombosis Without Affecting Hemostatic Parameters With a Cell-Penetrating PAR1 Pepducin

(2012) Ping Zhang et al.   CIRCULATION

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

(2012) Katie O'Callaghan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structure of the human κ-opioid receptor in complex with JDTic

(2012) Huixian Wu et al.   NATURE

High-resolution crystal structure of human protease-activated receptor 1

(2012) Cheng Zhang et al.   NATURE

Biased Signaling Pathways in  2-Adrenergic Receptor Characterized by 19F-NMR

(2012) J. J. Liu et al.   SCIENCE

The allosteric vestibule of a seven transmembrane helical receptor controls G-protein coupling

(2012) Andreas Bock et al.   Nature Communications

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

Bivalirudin Is a Dual Inhibitor of Thrombin and Collagen-Dependent Platelet Activation in Patients Undergoing Percutaneous Coronary Intervention

(2011) Carey Kimmelstiel et al.   Circulation-Cardiovascular Interventions

A matrix metalloprotease-PAR1 system regulates vascular integrity, systemic inflammation and death in sepsis

(2011) Sarah L. Tressel et al.   EMBO Molecular Medicine

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

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

Crystal structure of metarhodopsin II

(2011) Hui-Woog Choe et al.   NATURE

Structure of a nanobody-stabilized active state of the β2 adrenoceptor

(2011) Søren G. F. Rasmussen et al.   NATURE

Crystal structure of the β2 adrenergic receptor–Gs protein complex

(2011) Søren G. F. Rasmussen et al.   NATURE

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 an antithrombotic allosteric modulator that acts through helix 8 of PAR1

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

Diversity and modularity of G protein-coupled receptor structures

(2011) Vsevolod Katritch et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Rapid Binding and Transmembrane Diffusion of Pepducins in Phospholipid Bilayers

(2010) Kellen B. Fontanini et al.   BIOPHYSICAL JOURNAL

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

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

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

(2009) Vishal Trivedi et al.   CELL

The effect of ligand efficacy on the formation and stability of a GPCR-G protein complex

(2009) X. J. Yao et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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