Inverse agonist efficacy of selatogrel blunts constitutive P2Y12 receptor signaling by inducing the inactive receptor conformation

The potency of selatogrel, a reversible antagonist of the P2Y12 receptor, is affected by calcium concentration

(2021) Martine Baumann et al.   PLATELETS

Insights from In Vitro and Clinical Data to Guide Transition from the Novel P2Y12 Antagonist Selatogrel to Clopidogrel, Prasugrel, and Ticagrelor

(2021) Uta Schilling et al.   THROMBOSIS AND HAEMOSTASIS

Selatogrel, a reversible P2Y12 receptor antagonist, has reduced off-target interference with haemostatic factors in a mouse thrombosis model

(2021) Lydie Crescence et al.   THROMBOSIS RESEARCH

The P2Y12 Receptor Antagonist Selatogrel Dissolves Preformed Platelet Thrombi In Vivo

(2021) Lydie Crescence et al.   Journal of Clinical Medicine

Subcutaneous Selatogrel Inhibits Platelet Aggregation in Patients With Acute Myocardial Infarction

(2020) Peter Sinnaeve et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

ZOO: an automatic data-collection system for high-throughput structure analysis in protein microcrystallography

(2019) Kunio Hirata et al.   Acta Crystallographica Section D-Structural Biology

Novel Antiplatelet Therapies for Atherothrombotic Diseases

(2019) Arjun Majithia et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Absorption, distribution, metabolism, and excretion of the P2Y12 receptor antagonist selatogrel after subcutaneous administration in healthy subjects

(2019) Mike Ufer et al.   XENOBIOTICA

Pharmacodynamics, pharmacokinetics, and safety of single-dose subcutaneous administration of selatogrel, a novel P2Y12 receptor antagonist, in patients with chronic coronary syndromes

(2019) Robert F Storey et al.   EUROPEAN HEART JOURNAL

Clinical Pharmacology of the Reversible and Potent P2Y12 Receptor Antagonist ACT-246475 After Single Subcutaneous Administration in Healthy Male Subjects

(2018) Pierre-Eric Juif et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Deciphering biased inverse agonism of cangrelor and ticagrelor at P2Y12 receptor

(2018) Cédric Garcia et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Antiplatelet Agents for the Treatment and Prevention of Coronary Atherothrombosis

(2017) Carlo Patrono et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

Inverse agonism at the P2Y12 receptor and ENT1 transporter blockade contribute to platelet inhibition by ticagrelor

(2016) R. Aungraheeta et al.   BLOOD

Effects of P2Y12receptor antagonists beyond platelet inhibition - comparison of ticagrelor with thienopyridines

(2016) Sven Nylander et al.   BRITISH JOURNAL OF PHARMACOLOGY

Agonism, Antagonism, and Inverse Agonism Bias at the Ghrelin Receptor Signaling

(2015) Céline M'Kadmi et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

4-((R)-2-{[6-((S)-3-Methoxypyrrolidin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}-3-phosphonopropionyl)piperazine-1-carboxylic Acid Butyl Ester (ACT-246475) and Its Prodrug (ACT-281959), a Novel P2Y12 Receptor Antagonist with a Wider Therapeutic Window in the Rat Than Clopidogrel

(2015) Eva Caroff et al.   JOURNAL OF MEDICINAL CHEMISTRY

Agonist-bound structure of the human P2Y12 receptor

(2014) Jin Zhang et al.   NATURE

Structure of the human P2Y12 receptor in complex with an antithrombotic drug

(2014) Kaihua Zhang et al.   NATURE

Structure of the human P2Y12 receptor in complex with an antithrombotic drug

(2014) Bing Du et al.   Science China-Life Sciences

Deciphering biased-agonism complexity reveals a new active AT1 receptor entity

(2012) Aude Saulière et al.   Nature Chemical Biology

REFMAC5 for the refinement of macromolecular crystal structures

(2011) Garib N. Murshudov et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Diabetes and Antiplatelet Therapy in Acute Coronary Syndrome

(2011) José Luis Ferreiro et al.   CIRCULATION

XDS

(2010) Wolfgang Kabsch   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Features and development ofCoot

(2010) P. Emsley et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Ticagrelor versus Clopidogrel in Patients with Acute Coronary Syndromes

(2009) Lars Wallentin et al.   NEW ENGLAND JOURNAL OF MEDICINE

Interaction of the active metabolite of prasugrel, R-138727, with cysteine 97 and cysteine 175 of the human P2Y12receptor

(2008) I. ALGAIER et al.   JOURNAL OF THROMBOSIS AND HAEMOSTASIS

Studies on the role of the extracellular cysteines and oligomeric structures of the P2Y12receptor when interacting with antagonists

(2008) ZHONGREN DING et al.   JOURNAL OF THROMBOSIS AND HAEMOSTASIS