The chemokines CXCL8 and CXCL12: molecular and functional properties, role in disease and efforts towards pharmacological intervention

S Cambier, M Gouwy, P Proost - Cellular & Molecular Immunology, 2023 - nature.com
Chemokines are an indispensable component of our immune system through the regulation
of directional migration and activation of leukocytes. CXCL8 is the most potent human …

CXCR4/CXCL12 activities in the tumor microenvironment and implications for tumor immunotherapy

R Mezzapelle, M Leo, F Caprioglio, LS Colley… - Cancers, 2022 - mdpi.com
Simple Summary Chemokines are small soluble proteins that control and regulate cell
trafficking within and between tissues by binding to their receptors. Among them, CXCL12 …

Structures of atypical chemokine receptor 3 reveal the basis for its promiscuity and signaling bias

YC Yen, CT Schafer, M Gustavsson, SA Eberle… - Science …, 2022 - science.org
Both CXC chemokine receptor 4 (CXCR4) and atypical chemokine receptor 3 (ACKR3) are
activated by the chemokine CXCL12 yet evoke distinct cellular responses. CXCR4 is a …

Structural insights into CXCR4 modulation and oligomerization

K Saotome, LL McGoldrick, JH Ho, TF Ramlall… - Nature Structural & …, 2024 - nature.com
Activation of the chemokine receptor CXCR4 by its chemokine ligand CXCL12 regulates
diverse cellular processes. Previously reported crystal structures of CXCR4 revealed the …

Discovery and pharmacophoric characterization of chemokine network inhibitors using phage-display, saturation mutagenesis and computational modelling

S Vales, J Kryukova, S Chandra… - Nature …, 2023 - nature.com
CC and CXC-chemokines are the primary drivers of chemotaxis in inflammation, but
chemokine network redundancy thwarts pharmacological intervention. Tick evasins …

Understanding the mechanisms that facilitate specificity, not redundancy, of chemokine‐mediated leukocyte recruitment

DP Dyer - Immunology, 2020 - Wiley Online Library
Chemokines (chemotactic cytokines) and their receptors are critical to recruitment and
positioning of cells during development and the immune response. The chemokine system …

The dimeric form of CXCL12 binds to atypical chemokine receptor 1

JC Gutjahr, KS Crawford, DR Jensen, P Naik… - Science …, 2021 - science.org
The pleiotropic chemokine CXCL12 is involved in diverse physiological and
pathophysiological processes, including embryogenesis, hematopoiesis, leukocyte …

Cryo-EM structure of monomeric CXCL12-bound CXCR4 in the active state

Y Liu, A Liu, X Li, Q Liao, W Zhang, L Zhu, DY Richard - Cell Reports, 2024 - cell.com
CXCR4 binding of its endogenous agonist CXCL12 leads to diverse functions, including
bone marrow retention of hematopoietic progenitors and cancer metastasis. However, the …

Perspective: implications of ligand–receptor binding kinetics for therapeutic targeting of G protein-coupled receptors

WJC van der Velden, LH Heitman… - ACS pharmacology & …, 2020 - ACS Publications
The concept of ligand–receptor binding kinetics has been broadly applied in drug
development pipelines focusing on G protein-coupled receptors (GPCRs). The ligand …

Functional anatomy of the full-length CXCR4-CXCL12 complex systematically dissected by quantitative model-guided mutagenesis

BS Stephens, T Ngo, I Kufareva, TM Handel - Science signaling, 2020 - science.org
Because of their prominent roles in development, cancer, and HIV, the chemokine receptor
CXCR4 and its ligand CXCL12 have been the subject of numerous structural and functional …