Identification of a High-Affinity Phosphopeptide Inhibitor of Stat3
Abstract
Stat3 is a latent transcription factor that exhibits elevated activity in a variety of human cancers. To find a lead peptide for peptidomimetic drug development we synthesized and tested phosphopeptides derived from known receptor docking sites and found Y(p)LPQTV as the optimal sequence. SAR studies showed that each residue from pY to pY+3 provided binding energy.
Integrity signals
Registry
Cites
Statistics
Claims the paper makes
Claims other papers make about this one
Each is checked against this paper’s own text: does it say what the citing paper says it does?
Small molecules, peptides, or peptidomimetic compounds targeting the STAT3 SH2 domain are designed to disrupt STAT3 dimerization, preventing its translocation to the nucleus and transcription.
“Such molecules are designed to disrupt STAT3 dimerization, thus preventing its translocation to the nucleus and transcription.”
From Critical analysis of the potential for targeting STAT3 in human malignancy (2013) · cites this paper as [102]
STAT3 may be targeted via its SH2 domain by small molecules, peptides, or peptidomimetic compounds.
“STAT3 may be targeted via its SH2 domain by small molecules, peptides, or peptidomimetic compounds.101–104”
From Critical analysis of the potential for targeting STAT3 in human malignancy (2013) · cites this paper as [102]
Cites
Bowman, T., Garcia, R., Turkson, J., & Jove, R. (2000) · Oncogene · doi:10.1038/sj.onc.1203527 · Cited by 1,743 · see citing works
The role of STATs in transcriptional control and their impact on cellular function
Bromberg, J., & Darnell, J. E. (2000) · Oncogene · doi:10.1038/sj.onc.1203476 · Cited by 1,201 · see citing works
Flagged first, then by citations
Cited by
Sorted by citations
Zhang, X., Yue, P., Fletcher, S., Zhao, W., Gunning, P. T., & Turkson, J. (2010) · Biochemical Pharmacology · doi:10.1016/j.bcp.2010.01.001 · Cited by 179 · see citing works
Disruption of protein–protein interactions: Towards new targets for chemotherapy
Loregian, A., & Palù, G. (2005) · Journal of Cellular Physiology · doi:10.1002/jcp.20356 · Cited by 108 · see citing works
Critical analysis of the potential for targeting STAT3 in human malignancy
Grandis, J., & Peyser (2013) · OncoTargets and Therapy · doi:10.2147/ott.s47903 · Cited by 24 · see citing works
- Authors
- Ren, Z., Cabell, L. A., Schaefer, T. S., & McMurray, J. S.
- Affiliations
- The University of Texas MD Anderson Cancer Center (US)
- Corresponding author
- McMurray, John S
- ORCID
- Ren, Zhiyong
- Venue
- Bioorganic & Medicinal Chemistry Letters
- Publisher
- Elsevier BV
- Published
- 2003-02
- Volume
- 13
- Issue
- 4
- Pages
- 633-636
- ISSN
- 0960-894X (ISSN-L)
- OpenAlex
- W2004029306
- Cited by
- 128
- References
- 2
- Citations by year
- 2025: 4 · 2024: 2 · 2023: 1 · 2022: 4 · 2021: 4 · 2020: 5 · 2019: 5 · 2018: 4 · 2017: 1 · 2016: 5 · 2015: 6 · 2014: 10 · 2013: 10 · 2012: 5
- FWCI
- 2.25
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Bioorganic & Medicinal Chemistry Letters (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Oncology › Cytokine Signaling Pathways and Interactions
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
- Physical Sciences › Computer Science › Computational Theory and Mathematics › Computational Drug Discovery Methods
- Keywords
- STAT3, structure-activity relationship, binding energy, transcription factor inhibition, cancer
- MeSH terms
- Amino Acid Sequence, Antineoplastic Agents, DNA, DNA-Binding Proteins, Humans, Phosphopeptides, Protein Binding, Structure-Activity Relationship, Transcription Factors, Trans-Activators, src Homology Domains, Dimerization, Inhibitory Concentration 50, STAT3 Transcription Factor
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
