Research graph
References from Optimization of next-generation CXCR4 ligands for radiotheranostic applications. Local targets link to admitted publications; unresolved targets remain external evidence.
[18F]RPS-544: a PET tracer for imaging the chemokine receptor CXCR4
10.1016/j.nucmedbio.2018.01.004 · 2018 · External reference
[18F]Fluoroethyltriazolyl monocyclam derivatives as imaging probes for the chemokine receptor CXCR4
10.3390/molecules24081612 · 2019 · External reference
Mavorixafor, an orally bioavailable CXCR4 antagonist, increases immune cell infiltration and inflammatory status of tumor microenvironment in patients with melanoma
10.1158/2767-9764.crc-22-0090 · 2022 · External reference
WHIM syndromes with different genetic anomalies are accounted for by impaired CXCR4 desensitization to CXCL12
10.1182/blood-2004-06-2289 · 2005 · External reference
Cancer and the chemokine network
10.1038/nrc1388 · 2004 · External reference
The HIV coreceptors CXCR4 and CCR5 are differentially expressed and regulated on human T lymphocytes
10.1073/pnas.94.5.1925 · 1996 · External reference
Investigating the chemokine receptor 4 as potential theranostic target in adrenocortical cancer patients
10.1097/rlu.0000000000001435 · 2017 · External reference
BL-8040 CXCR4 antagonist is safe and demonstrates antileukemic activity in combination with cytarabine for the treatment of relapsed/refractory acute myelogenous leukemia: an open-label safety and efficacy phase 2a study
10.1002/cncr.33338 · 2021 · External reference
CXCR4-directed endoradiotherapy with [177Lu]Pentixather added to total body irradiation for myeloablative conditioning in patients with relapsed/refractory acute myeloid leukemia
10.7150/thno.101215 · 2025 · External reference
Development and evaluation of an 18F-radiolabeled monocyclam derivative for imaging CXCR4 expression
10.1021/acs.molpharmaceut.9b00069 · 2019 · External reference
Synthesis and structure−activity relationships of azamacrocyclic C-X-C chemokine receptor 4 antagonists: analogues containing a single azamacrocyclic ring are potent inhibitors of T-cell tropic (X4) HIV-1 replication
10.1021/jm901530b · 2010 · External reference
Polyfunctionality of the CXCR4/CXCL12 axis in health and disease: implications for therapeutic interventions in cancer and immune-mediated diseases
10.1096/fj.202001273r · 2021 · External reference
Imaging of C-X-C Motif chemokine receptor 4 expression in 690 patients with solid or hematologic neoplasms using 68Ga-PentixaFor PET
10.2967/jnumed.121.263693 · 2022 · External reference
C-X-C motif chemokine receptor 4–targeted radioligand therapy in patients with advanced T-cell lymphoma
10.2967/jnumed.122.264207 · 2023 · External reference
Regulation of CXCR4 signaling
10.1016/j.bbamem.2006.11.002 · 2007 · External reference
The intricate role of CXCR4 in cancer
10.1016/b978-0-12-411638-2.00002-1 · 2014 · External reference
CXCR4 inhibition in tumor microenvironment facilitates anti-programmed death receptor-1 immunotherapy in sorafenib-treated hepatocellular carcinoma in mice
10.1002/hep.27665 · 2015 · External reference
PET imaging of CXCR4 expression using [18F]AlF-NOTA-QHY-04 for hematologic malignancy and solid tumors
10.7150/thno.99025 · 2024 · External reference
Targeting CXCR4 with 212Pb/203Pb-pentixather significantly increases overall survival in small cell lung cancer
10.1667/rade-24-00232.1 · 2025 · External reference
Optimal design, anti-tumour efficacy and tolerability of anti-CXCR4 antibody drug conjugates
10.1038/s41598-019-38745-x · 2019 · External reference
Solution structure and basis for functional activity of stromal cell‐derived factor‐1; dissociation of CXCR4 activation from binding and inhibition of HIV‐1
10.1093/emboj/16.23.6996 · 1997 · External reference
The bicyclam AMD3100 story
10.1038/nrd1134 · 2003 · External reference
Imaging CXCR4 expression in human cancer xenografts: evaluation of monocyclam 64Cu-AMD3465
10.2967/jnumed.110.085613 · 2011 · External reference
Design, synthesis, and functionalization of dimeric peptides targeting chemokine receptor CXCR4
10.1021/jm2009716 · External reference
PET imaging of CXCR4 receptors in cancer by a new optimized ligand
10.1002/cmdc.201100320 · External reference
Exploring the N-terminal region of C-X-C motif chemokine 12 (CXCL12): identification of plasma-stable cyclic peptides as novel, potent C-X-C chemokine receptor type 4 (CXCR4) antagonists
10.1021/acs.jmedchem.6b00695 · 2016 · External reference
Structure–activity relationships and biological characterization of a novel, potent, and serum stable C-X-C chemokine receptor type 4 (CXCR4) antagonist
10.1021/acs.jmedchem.7b01062 · 2017 · External reference
CXCR4 PET/CT predicts left ventricular recovery 8 months after acute myocardial infarction
10.2967/jnumed.125.270807 · 2025 · External reference
A phase III, multicenter, randomized, double-blind, placebo-controlled, comparative trial of AMD3100 (Plerixafor)+G-CSF vs. G-CSF+Placebo for mobilization in multiple myeloma (MM) patients for autologous hematopoietic stem cell (aHSC) transplantation
10.1182/blood.v110.11.445.445 · 2007 · External reference
AMD3100, a small molecule inhibitor of HIV-1 entry via the CXCR4 co-receptor
10.1038/nm0198-072 · 1998 · External reference
C-X-C Motif chemokine receptor 4–Directed scintigraphy using [99mTc]Tc-Pentixatec in primary aldosteronism: a proof-of-concept study
10.2967/jnumed.124.268169 · 2024 · External reference
Design, synthesis, and biological characterization of a new class of symmetrical polyamine-based small molecule CXCR4 antagonists
10.1016/j.ejmech.2020.112410 · 2020 · External reference
A novel small molecule CXCR4 antagonist potently mobilizes hematopoietic stem cells in mice and monkeys
10.1186/s13287-020-02073-z · 2021 · External reference
A fragment integrational approach to GPCR inhibition: identification of a high affinity small molecule CXCR4 antagonist
10.1016/j.ejmech.2022.114150 · 2022 · External reference
CXCR4 inhibition counteracts immunosuppressive properties of metastatic NSCLC stem cells
10.3389/fimmu.2020.02168 · 2020 · External reference
Molecular-size reduction of a potent CXCR4-Chemokine antagonist using orthogonal combination of conformation- and sequence-based libraries
10.1002/anie.200351024 · 2003 · External reference
Functional nodules in primary aldosteronism: identification of CXCR4 expression with 68Ga-pentixafor PET/CT
10.1007/s00330-022-09058-x · 2023 · External reference
Molecular interactions of cyclam and bicyclam non-peptide antagonists with the CXCR4 chemokine receptor
10.1074/jbc.m010429200 · 2001 · External reference
Metal ion enhanced binding of AMD3100 to Asp262 in the CXCR4 receptor
10.1021/bi0264770 · 2003 · External reference
Phase I/II trial of the CXCR4 inhibitor plerixafor in combination with bortezomib as a chemosensitization strategy in relapsed/refractory multiple myeloma
10.1002/ajh.25627 · 2019 · External reference
PET of CXCR4 expression by a 68Ga-Labeled highly specific targeted contrast agent
10.2967/jnumed.111.098798 · 2011 · External reference
Chemokines and chemokine receptors: positioning cells for host defense and immunity
10.1146/annurev-immunol-032713-120145 · 2014 · External reference
Development of a 111In-labeled peptide derivative targeting a chemokine receptor, CXCR4, for imaging tumors
10.1016/j.nucmedbio.2006.01.006 · 2006 · External reference
Biokinetics and dosimetry of [177Lu]Lu-Pentixather
10.2967/jnumed.121.262295 · 2021 · External reference
Mutation of Asp171 and Asp262 of the chemokine receptor CXCR4 impairs its coreceptor function for human immunodeficiency Virus-1 entry and abrogates the antagonistic activity of AMD3100
10.1016/s0026-895x(24)23060-1 · 2001 · External reference
AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor
10.1016/j.bcp.2005.05.035 · 2005 · External reference
Pharmacokinetics and safety of AMD-3100, a novel antagonist of the CXCR-4 chemokine receptor, in human volunteers
10.1128/aac.44.6.1667-1673.2000 · 2000 · External reference
Imaging the cytokine receptor CXCR4 in atherosclerotic plaques with the radiotracer 68Ga-Pentixafor for PET
10.2967/jnumed.116.179663 · 2017 · External reference
64Cu-AMD3100—A novel imaging agent for targeting chemokine receptor CXCR4
10.1016/j.bmc.2009.01.014 · 2009 · External reference
CXCR4+ cells are increased in lung tissue of patients with idiopathic pulmonary fibrosis
10.1186/s12931-020-01467-0 · 2020 · External reference
The unique structural and functional features of CXCL12
10.1038/cmi.2017.107 · 2018 · External reference
Spatial myeloid landscape of large artery atherosclerotic and cardioembolic thrombi retrieved by mechanical thrombectomy
10.1096/fj.202501658rr · 2025 · External reference
Mechanisms of lymphatic metastasis
10.1172/jci71606 · 2014 · External reference
CXCR4 signaling regulates metastasis of chemoresistant melanoma cells by a lymphatic metastatic niche
10.1158/0008-5472.can-10-2591 · 2010 · External reference
Imaging inflammation in atherosclerosis with CXCR4-directed 68Ga-pentixafor PET/CT: correlation with 18F-FDG PET/CT
10.2967/jnumed.119.234484 · 2020 · External reference
[99mTc]Tc-PentixaTec: development, extensive pre-clinical evaluation, and first human experience
10.1007/s00259-023-06395-x · 2023 · External reference
Radioactive main group and rare Earth metals for imaging and therapy
10.1021/acs.chemrev.8b00294 · 2019 · External reference
Pharmacokinetic modeling of the hepatobiliary transport mediated by cooperation of uptake and efflux transporters
10.3109/03602530903491824 · 2010 · External reference
Clinical applications of theranostics
10.1007/978-3-032-21415-7_17 · 2026 · External reference
High-contrast CXCR4-Targeted 18F-PET imaging using a potent and selective antagonist
10.1021/acs.molpharmaceut.0c00785 · 2021 · External reference
Targeting refractory mantle cell lymphoma for imaging and therapy using C-X-C chemokine receptor type 4 radioligands
10.1158/1078-0432.ccr-21-3284 · External reference
[18F]Trifluoroborate-based CXCR4-targeting PET agents based on a potent and novel pharmacophore. [Abstract]
External reference
Reducing the kidney uptake of high contrast CXCR4 PET imaging agents via linker modifications
10.3390/pharmaceutics14071502 · External reference
Development of an optimized CXCR4-targeting theranostic pair
10.2967/jnumed.125.269933 · 2026 · External reference
CXCR4-directed endoradiotherapy induces high response rates in extramedullary relapsed multiple myeloma
10.7150/thno.19050 · External reference
[68Ga]Pentixafor-PET/CT for imaging of chemokine receptor CXCR4 expression in multiple myeloma - comparison to [18F]FDG and laboratory values
10.7150/thno.16576 · External reference
Feasibility of CXCR4-directed radioligand therapy in advanced diffuse large B-cell lymphoma
10.2967/jnumed.118.210997 · 2019 · External reference
[68Ga]Ga/[177Lu]Lu-BL01, a novel theranostic pair for targeting C-X-C chemokine receptor 4
10.1021/acs.molpharmaceut.9b00808 · 2019 · External reference
Predicting binding affinities for GPCR ligands using free-energy perturbation
10.1021/acsomega.6b00086 · 2016 · External reference
18F-Radiolabeling and evaluation of an AMD3465 derivative for PET imaging of CXCR4 in a mouse breast tumor model
10.1021/acs.bioconjchem.4c00167 · 2024 · External reference
[99mTc]-PentixaTec SPECT/CT for imaging of chemokine receptor 4 expression after myocardial infarction
2024 · External reference
Double-edged role of the CXCL12/CXCR4 axis in experimental myocardial infarction
10.1016/j.jacc.2011.08.033 · 2011 · External reference
Mobilization of hematopoietic progenitor cells in healthy volunteers by AMD3100, a CXCR4 antagonist
10.1182/blood-2003-02-0663 · 2003 · External reference
Cryo-EM structure of monomeric CXCL12-bound CXCR4 in the active state
10.1016/j.celrep.2024.114578 · 2024 · External reference
Structural basis of CXCR4 assembly and regulation
10.1016/j.celrep.2025.115255 · 2025 · External reference
Dynamics study on the anti-human immunodeficiency virus chemokine viral macrophage-inflammatory Protein-II (VMIP-II) reveals a fully monomeric protein
10.1021/bi9812726 · 1999 · External reference
68Ga-Pentixafor PET/CT for imaging of chemokine receptor 4 expression in waldenström macroglobulinemia/lymphoplasmacytic lymphoma: comparison to 18F-FDG PET/CT
10.2967/jnumed.119.226134 · 2019 · External reference
D-peptide-based probe for CXCR4-targeted molecular imaging and radionuclide therapy
10.3390/pharmaceutics13101619 · 2021 · External reference
At the bedside: profiling and treating patients with CXCR4-expressing cancers
10.1002/jlb.5bt1219-714r · 2021 · External reference
Side effects of CXC-chemokine receptor 4–directed endoradiotherapy with pentixather before hematopoietic stem cell transplantation
10.2967/jnumed.118.223420 · 2019 · External reference
CXCR4 PET imaging of mantle cell lymphoma using [68Ga]Pentixafor: comparison with [18F]FDG-PET
10.7150/thno.48620 · 2021 · External reference
New lyophilized kit for rapid radiofluorination of peptides
10.1021/bc200608e · 2012 · External reference
Click chemistry and radiochemistry: the first 10 years
10.1021/acs.bioconjchem.6b00561 · 2016 · External reference
10.1038/s44386-025-00019-0 · 2025 · Admitted local publication
CXCR4 signaling in the regulation of stem cell migration and development
10.1016/j.jneuroim.2008.04.008 · 2008 · External reference
Discovery and characterization of novel small-molecule CXCR4 receptor agonists and antagonists
10.1038/srep30155 · 2016 · External reference
Chemokines and chemokine receptors: new targets for cancer immunotherapy
10.3389/fimmu.2019.00379 · 2019 · External reference
CXCR4-targeted PET imaging using 64Cu-AMD3100 for detection of waldenström macroglobulinemia
10.1080/15384047.2019.1665405 · 2020 · External reference
Design, synthesis, and pharmacological evaluation of second-generation tetrahydroisoquinoline-based CXCR4 antagonists with favorable ADME properties
10.1021/acs.jmedchem.8b00450 · 2018 · External reference
Molecular imaging of CXCR4 receptor expression in human cancer xenografts with [64Cu]AMD3100 positron emission tomography
10.1158/0008-5472.can-09-4396 · 2010 · External reference
A new class of PentixaFor- and PentixaTher-based theranostic agents with enhanced CXCR4-targeting efficiency
10.7150/thno.45537 · 2020 · External reference
A benzenesulfonamide derivative as a novel PET radioligand for CXCR4
10.1016/j.bmc.2019.115240 · 2020 · External reference
Identification of LY2510924, a novel cyclic peptide CXCR4 antagonist that exhibits antitumor activities in solid tumor and breast cancer metastatic models
10.1158/1535-7163.mct-14-0850 · 2015 · External reference
Preclinical evaluation of [64Cu]NOTA-CP01 as a PET imaging agent for metastatic esophageal squamous cell carcinoma
10.1021/acs.molpharmaceut.1c00600 · 2021 · External reference
Preclinical development of a novel class of CXCR4 antagonist impairing solid tumors growth and metastases
10.1371/journal.pone.0074548 · 2013 · External reference
The influence of different metal-chelate conjugates of pentixafor on the CXCR4 affinity
10.1186/s13550-016-0193-8 · 2016 · External reference
[64Cu]NOTA-pentixather enables high resolution PET imaging of CXCR4 expression in a preclinical lymphoma model
10.1186/s41181-016-0020-6 · 2017 · External reference
AMD3100: a versatile platform for CXCR4 Targeting68 Ga-based radiopharmaceuticals
10.1021/acs.bioconjchem.5b00689 · 2016 · External reference
Crystal structure of the chemokine receptor CXCR4 in complex with a viral chemokine
10.1126/science.1261064 · 2015 · External reference
In vivo validation of 68Ga-labeled AMD3100 conjugates for PET imaging of CXCR4
10.1016/j.nucmedbio.2023.108335 · 2023 · External reference
A small-molecule antagonist of CXCR4 inhibits intracranial growth of primary brain tumors
10.1073/pnas.2235846100 · 2003 · External reference
Structural mechanisms underlying the modulation of CXCR4 by diverse small-molecule antagonists
10.1073/pnas.2425795122 · 2025 · External reference
Structural insights into CXCR4 modulation and oligomerization
10.1038/s41594-024-01397-1 · 2025 · External reference
[177Lu]pentixather: comprehensive preclinical characterization of a first CXCR4-directed endoradiotherapeutic agent
10.7150/thno.19119 · 2017 · External reference
Validation of [125I]CPCR4.3 as an investigative tool for the sensitive and specific detection of hCXCR4 and mCXCR4 expression in vitro and in vivo
10.1186/s13550-019-0545-2 · 2019 · External reference
Radiopharmaceutical therapy in cancer: clinical advances and challenges
10.1038/s41573-020-0073-9 · 2020 · External reference
Discovery of novel small molecule orally bioavailable C−X−C chemokine receptor 4 antagonists that are potent inhibitors of T-Tropic (X4) HIV-1 replication
10.1021/jm100073m · 2010 · External reference
CXCR4 regulates growth of both primary and metastatic breast cancer
10.1158/0008-5472.can-04-1844 · 2004 · External reference
Second generation Al18F-labeled D-amino acid peptide for CXCR4 targeted molecular imaging
10.1016/j.nucmedbio.2024.108906 · 2024 · External reference
Selective PET imaging of CXCR4 using the Al18F-labeled antagonist LY2510924
10.1007/s00259-024-07025-w · 2025 · External reference
Radiosynthesis and preclinical evaluation of a 68Ga-labeled tetrahydroisoquinoline-based ligand for PET imaging of C-X-C chemokine receptor type 4 in an animal model of glioblastoma
10.1186/s41181-024-00290-y · 2024 · External reference
C-terminal–modified LY2510924: a versatile scaffold for targeting C-X-C chemokine receptor type 4
10.1038/s41598-019-51754-0 · 2019 · External reference
Exploratory studies on development of the chemokine receptor CXCR4 antagonists toward downsizing
10.4137/pmc.s422 · 2008 · External reference
Distinct functional sites for human immunodeficiency virus type 1 and stromal cell-derived factor 1α on CXCR4 transmembrane helical domains
10.1128/jvi.79.20.12667-12673.2005 · 2005 · External reference
Novel peptide-based PET probe for non-invasive imaging of C-X-C chemokine receptor type 4 (CXCR4) in tumors
10.1021/acs.jmedchem.1c00066 · 2021 · External reference
Discovery of tetrahydroisoquinoline-based CXCR4 antagonists
10.1021/ml400183q · 2013 · External reference
Synthesis and evaluation of novel C-X-C chemokine receptor 4-Targeted radiotracers for oncological imaging
10.1021/acs.jmedchem.5c00735 · 2025 · External reference
Design, preclinical evaluation, and clinical translation of [68Ga]Ga/[177Lu]Lu-JH120061, A novel radiopharmaceutical targeting CXCR4
10.1158/1078-0432.ccr-26-0292 · 2026 · External reference
Positron emission tomography imaging of tumors expressing the human chemokine receptor CXCR4 in mice with the use of 64Cu-AMD3100
10.1007/s11307-010-0466-y · 2012 · External reference
Disclosing the CXCR4 expression in lymphoproliferative diseases by targeted molecular imaging
10.7150/thno.11251 · 2015 · External reference
Structures of the CXCR4 chemokine receptor in complex with small molecule and cyclic peptide antagonists
10.1126/science.1194396 · 2010 · External reference
A synthetic bivalent ligand of CXCR4 inhibits HIV infection
10.1016/j.bbrc.2013.05.038 · 2013 · External reference
The CXCR4-targeted theranostics era: a comprehensive review of a decade of progress (2015–2025)
10.7150/thno.130266 · 2026 · External reference
CXCR4-Targeted radiopharmaceuticals for the imaging and therapy of malignant tumors
10.3390/molecules28124707 · 2023 · External reference
68Ga/161Tb-Labeled CXCR4-Targeted probe with enhanced positive charge: improved affinity and longer tumor retention without survival benefit in mice models
10.1021/acs.jmedchem.5c03763 · 2026 · External reference
CXCR4 mediated recognition of HIV envelope spike and inhibition by CXCL12
10.1038/s41467-025-63815-2 · 2025 · External reference
A novel peptide antagonist of CXCR4 derived from the N-Terminus of viral chemokine vMIP-II
10.1021/bi992750v · 2000 · External reference
Exploring the stereochemistry of CXCR4-Peptide recognition and inhibiting HIV-1 entry with d-Peptides derived from chemokines
10.1074/jbc.m202063200 · 2002 · External reference
The chemokine superfamily revisited
10.1016/j.immuni.2012.05.008 · 2012 · External reference
