Results 101 to 110 of about 2,928 (195)

Inhibition of constitutive activity of the atypical chemokine receptor ACKR3 by the small-molecule inverse agonist VUF16840

bioRxiv
The atypical chemokine receptor 3 (ACKR3) has emerged as a promising drug target for the treatment of cancer, cardiovascular, and autoimmune diseases. In this study, we present the pharmacological characterization of VUF16840, the first small-molecule ...
R. Bosma, Desislava Nesheva, M. Rijnsburger, Rick Riemens, Justyna M. Adamska, M. Meyrath, Simon Mobach, C. Buzink, Iwan J. P. de Esch, M. Szpakowska, M. Wijtmans, A. Chevigné, H. Vischer, Rob Leurs   +13 more
semanticscholar   +1 more source

Abstracts

Molecular Oncology, Volume 20, Issue S1, Page 1-692, August 2026.
Abstracts submitted to the ‘EACR 2026 Congress: Innovative Cancer Science’, from 08–11 June 2026 and accepted by the Congress Organising Committee are published in this Supplement of Molecular Oncology, an affiliated journal of the European Association for Cancer Research (EACR).
wiley   +1 more source

Atypical Ligand Binding and Activation Modes of ACKR3/CXCR7

, 2018
The atypical chemokine receptor ACKR3/CXCR7 plays crucial roles in numerous physiological processes but also in viral infection and cancer. ACKR3 shows strong propensity for activation and, unlike classical chemokine receptors, can respond to chemokines ...
Szpakowska, Martyna, Meyrath, Max Marc Roger, Counson, Manuel, Chevigné, Andy, Reynders, Nathan, Steyaert, Jan, Hanson, Julien   +6 more
core   +1 more source

Le déchiffrage de l'interactome de CXCR4 et ACKR3 révèle la régulation par ACKR3 de l'activité des jonctions Gap

, 2018
Le récepteur atypique ACKR3 et le récepteur CXCR4 sont des récepteurs couplés aux protéines G appartenant à la famille des récepteurs CXC des chimiokines.
Fumagalli, Amos
core   +1 more source

Diversity and inter-connections in the CXCR4 chemokine receptor/ligand family: molecular perspectives

Frontiers in Immunology, 2015
CXCR4 and its ligand CXCL12 mediate the homing of progenitor cells in the bone marrow and their recruitment to sites of injury, as well as affect processes such as cell arrest, survival and angiogenesis.
Lukas ePawig, Christina eKlasen, Christian eWeber, Jürgen eBernhagen, Heidi eNoels   +4 more
doaj   +1 more source

Decreased ACKR3 (CXCR7) function causes oculomotor synkinesis in mice and humans

Human Molecular Genetics, 2019
Abstract Oculomotor synkinesis is the involuntary movement of the eyes or eyelids with a voluntary attempt at a different movement. The chemokine receptor CXCR4 and its ligand CXCL12 regulate oculomotor nerve development; mice with loss of either molecule have oculomotor synkinesis.
Mary C, Whitman, Noriko, Miyake, Elaine H, Nguyen, Jessica L, Bell, Paola M, Matos Ruiz, Wai-Man, Chan, Silvio Alessandro, Di Gioia, Nisha, Mukherjee, Brenda J, Barry, T M, Bosley, Arif O, Khan, Elizabeth C, Engle   +11 more
openaire   +3 more sources

Peroxynitrite Exposure of CXCL12 Impairs Monocyte, Lymphocyte and Endothelial Cell Chemotaxis, Lymphocyte Extravasation in vivo and Anti-HIV-1 Activity

Frontiers in Immunology, 2018
CXCL12 is a chemotactic cytokine that attracts many different cell types for homeostasis and during inflammation. Under stress conditions, macrophages and granulocytes produce factors such as peroxynitrite as a consequence of their oxidative response ...
Rik Janssens, Rik Janssens, Daiane Boff, Daiane Boff, Pieter Ruytinx, Anneleen Mortier, Vincent Vanheule, Olav Larsen, Olav Larsen, Viktorija Daugvilaite, Mette M. Rosenkilde, Sam Noppen, Sandra Liekens, Dominique Schols, Ingrid De Meester, Ghislain Opdenakker, Sofie Struyf, Mauro M. Teixeira, Flávio A. Amaral, Paul Proost   +19 more
doaj   +1 more source

Entwicklung von ACKR3-spezifischen Agonisten und deren pharmakologische Wirksamkeit

Thrombozyten spielen eine zentrale Rolle in der Hämostase und Thrombose, sind jedoch auch maßgeblich an inflammatorischen Prozessen beteiligt. Neben klassischen Aktivierungsrezeptoren wurden in den letzten Jahren zunehmend Chemokinrezeptoren auf ...
Kolb, Kyra
core   +1 more source

Structural basis for selectivity and antagonism in extracellular GPCR-nanobodies

Nature Communications
G protein-coupled receptors (GPCRs) are pivotal therapeutic targets, but their complex structure poses challenges for effective drug design. Nanobodies, or single-domain antibodies, have emerged as a promising therapeutic strategy to target GPCRs ...
Roman R. Schlimgen, Francis C. Peterson, Raimond Heukers, Martine J. Smit, John D. McCorvy, Brian F. Volkman   +5 more
doaj   +1 more source

Diastereomer-Dependent Modulation of Atypical Chemokine Receptor 3 (ACKR3) in 3-Azabicyclo[3.1.0]hexane-Based Ligands

Atypical chemokine receptor 3 (ACKR3) is a β-arrestin-biased scavenger receptor that is involved in cancer and inflammatory diseases. Motivated by the clinical development of the ACKR3 ligand ACT-1004-1239 for multiple sclerosis (MS), we designed ...
Rob Leurs, Helga E. de Vries, Luna Melo Alcerreca, Iwan J.P. de Esch, Maikel Wijtmans, Yaroslav V. Nikolaev, Tomasz M. Stepniewski, Merel Rijnsburger, István Szabó, Maurice C.M.L. Buzink, Britt Hurks, Henry F. Vischer, Laura H.A. Wijffelaars, Desislava Nesheva, Susanne M.A. van der Pol   +14 more
core   +1 more source