ArticleACS medicinal chemistry letters2011
Agonists for the Chemokine Receptor CXCR4.
Article in ACS medicinal chemistry letters, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
15 citing papers in PubMed.
- A Randomized, Open-Label Phase 2 Study of the CXCR4 Inhibitor LY2510924 in Combination with Sunitinib Versus Sunitinib Alone in Patients with Metastatic Renal Cell Carcinoma (RCC).Targeted oncology · 2016Trial
- Discovery of Novel 2-Morpholine Tetrahydroisoquinoline CXCR4 Antagonists with Unique Properties.Journal of medicinal chemistry · 2026Article
- Article
- Chemical Synthesis of TFF3 Reveals Novel Mechanistic Insights and a Gut-Stable Metabolite.Journal of medicinal chemistry · 2021Article
- Development of CXCR4 modulators based on the lead compound RB-108.European journal of medicinal chemistry · 2019Article
- Improving the inhibitory effect of CXCR4 peptide antagonist in tumor metastasis with an acetylated PAMAM dendrimer.RSC advances · 2018Article
- Discovery ofACS medicinal chemistry letters · 2018Article
- Anti-inflammatory hybrids of secondary amines and amide-sulfamide derivatives.European journal of medicinal chemistry · 2018Article
- Novel anti-inflammatory agents targeting CXCR4: Design, synthesis, biological evaluation and preliminary pharmacokinetic study.European journal of medicinal chemistry · 2017Article
- What Do Structures Tell Us About Chemokine Receptor Function and Antagonism?Annual review of biophysics · 2017Review
- Design, synthesis, and biological characterization of novel PEG-linked dimeric modulators for CXCR4.Bioorganic & medicinal chemistry · 2016Article
- Improving chemotherapeutic efficiency in acute myeloid leukemia treatments by chemically synthesized peptide interfering with CXCR4/CXCL12 axis.Scientific reports · 2015Article
- Structural biology. Crystal structure of the chemokine receptor CXCR4 in complex with a viral chemokine.Science (New York, N.Y.) · 2015Article
- Small molecule inhibitors of CXCR4.Theranostics · 2013Review
- Drug discovery research targeting the CXC chemokine receptor 4 (CXCR4).Journal of medicinal chemistry · 2012Review
Corrections and comments
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Authors and funding
9 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The development of agonists for the chemokine receptor CXCR4 could provide promising therapeutic candidates. On the basis of previously forwarded two site model of chemokine-receptor interactions, we hypothesized that linking the agonistic N-terminus of SDF-1 to the T140 backbone would yield new high-affinity agonists of CXCR4. We developed chimeras with the agonistic SDF-1 N-terminus grafted to a T140 side chain and tested their binding affinity and chemotactic agonist activity. While chimeras with the peptide grafted onto position 12 of T140 remained high-affinity antagonists, those bearing the peptide on position 14 were in part agonists. One chimera was a full CXCR4 agonist with 25 nM affinity, and several chimeras showed low nanomolar affinities with partial agonist activity. Our results confirmed that we have developed high-affinity agonists of CXCR4.
Identifiers
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.