CXC chemokine receptor 4 (CXCR4) blockade in cancer treatment
CXC chemokine receptor type 4 (CXCR4) is a member of the G protein-coupled receptors
(GPCRs) superfamily and is specific for CXC chemokine ligand 12 (CXCL12, also known as …
(GPCRs) superfamily and is specific for CXC chemokine ligand 12 (CXCL12, also known as …
Waldenström macroglobulinemia: a review of pathogenesis, current treatment, and future prospects
B Ghafoor, SS Masthan, M Hameed, HH Akhtar… - Annals of …, 2024 - Springer
Waldenström macroglobulinemia (WM) is a chronic B-cell lymphoproliferative disorder
characterized by lymphoplasmacytic cell overgrowth in the bone marrow and increased …
characterized by lymphoplasmacytic cell overgrowth in the bone marrow and increased …
Phase 1 study of ibrutinib and the CXCR4 antagonist ulocuplumab in CXCR4-mutated Waldenström macroglobulinemia
SP Treon, K Meid, ZR Hunter, CA Flynn… - Blood, The Journal …, 2021 - ashpublications.org
MYD88 and CXCR4 mutations are common in Waldenström macroglobulinemia (WM).
Mutated CXCR4 (CXCR4Mut) impacts BTK-inhibitor response. We conducted a phase 1 trial …
Mutated CXCR4 (CXCR4Mut) impacts BTK-inhibitor response. We conducted a phase 1 trial …
[HTML][HTML] Fatty acid conjugated EPI-X4 derivatives with increased activity and in vivo stability
Dysregulation of the CXCL12/CXCR4 axis is implicated in autoimmune, inflammatory, and
oncogenic diseases, positioning CXCR4 as a pivotal therapeutic target. We evaluated …
oncogenic diseases, positioning CXCR4 as a pivotal therapeutic target. We evaluated …
Computational modeling and experimental validation of the EPI-X4/CXCR4 complex allows rational design of small peptide antagonists
Abstract EPI-X4, a 16-mer fragment of albumin, is a specific endogenous antagonist and
inverse agonist of the CXC-motif-chemokine receptor 4 (CXCR4) and thus a key regulator of …
inverse agonist of the CXC-motif-chemokine receptor 4 (CXCR4) and thus a key regulator of …
Advanced EPI-X4 derivatives covalently bind human serum albumin resulting in prolonged plasma stability
Advanced derivatives of the E ndogenous P eptide I nhibitor of CX CR 4 (EPI-X4) have
shown therapeutic efficacy upon topical administration in animal models of asthma and …
shown therapeutic efficacy upon topical administration in animal models of asthma and …
Development of N-Terminally Modified Variants of the CXCR4-Antagonistic Peptide EPI-X4 for Enhanced Plasma Stability
M Harms, R Fabech Hansson, A Gilg… - Journal of Medicinal …, 2023 - ACS Publications
EPI-X4, a natural peptide CXCR4 antagonist, shows potential for treating inflammation and
cancer, but its short plasma stability limits its clinical application. We aimed to improve the …
cancer, but its short plasma stability limits its clinical application. We aimed to improve the …
Development of a new class of CXCR4-targeting radioligands based on the endogenous antagonist EPI-X4 for oncological applications
RH Gaonkar, YT Schmidt, R Mansi… - Journal of Medicinal …, 2023 - ACS Publications
The peptide fragment of human serum albumin that was identified as an inhibitor of C–X–C
motif chemokine receptor 4 (CXCR4), termed EPI-X4, was investigated as a scaffold for the …
motif chemokine receptor 4 (CXCR4), termed EPI-X4, was investigated as a scaffold for the …
Dimerization of the peptide CXCR4-antagonist on macromolecular and supramolecular protraction arms affords increased potency and enhanced plasma stability
Peptides are prime drug candidates due to their high specificity of action but are
disadvantaged by low proteolytic stability. Here, we focus on the development of stabilized …
disadvantaged by low proteolytic stability. Here, we focus on the development of stabilized …
Peptide Bispecifics Inhibiting HIV-1 Infection by an Orthogonal Chemical and Supramolecular Strategy
Viral infections pose a significant threat to human health, and effective antiviral strategies
are urgently needed. Antiviral peptides have emerged as a promising class of therapeutic …
are urgently needed. Antiviral peptides have emerged as a promising class of therapeutic …