Design, synthesis, and evaluation of peptidomimetics containing Freidinger lactams as STAT3 inhibitors
Abstract
The STAT3 oncogene is a promising molecular target for the design of a new class of anticancer drugs. In this letter, we describe the design, synthesis, and evaluation of peptidomimetics containing Freidinger lactams as novel STAT3 inhibitors. Compound 3 binds to STAT3 with a K(i) value of 190nM and is a promising lead compound for further design and optimization.
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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 [104]
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 [104]
Cites
Transcription factors as targets for cancer therapy
Darnell, J. E. (2002) · Nature Reviews Cancer · doi:10.1038/nrc906 · Cited by 1,194 · see citing works
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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
“104 Such molecules are designed to disrupt STAT3 dimerization, thus preventing its translocation to the nucleus and transcription.”
- Authors
- Gomez, C., Bai, L., Zhang, J., Nikolovska-Coleska, Z., Chen, J., Yi, H., & Wang, S.
- Affiliations
- University of Michigan (US)
- Corresponding author
- Wang, Shaomeng
- Venue
- Bioorganic & Medicinal Chemistry Letters
- Publisher
- Elsevier BV
- Published
- 2009-03
- Volume
- 19
- Issue
- 6
- Pages
- 1733-1736
- ISSN
- 0960-894X (ISSN-L)
- OpenAlex
- W2145237802
- Cited by
- 26
- References
- 1
- Citations by year
- 2024: 1 · 2021: 2 · 2019: 1 · 2018: 3 · 2017: 1 · 2015: 3 · 2013: 4 · 2012: 1
- FWCI
- 2.33
- 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
- Physical Sciences › Chemistry › Organic Chemistry › Synthesis and biological activity
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
- Keywords
- STAT3 inhibitor, peptidomimetics, anticancer drug design, lead compounds, kinase inhibition
- MeSH terms
- Antineoplastic Agents, Chemistry, Pharmaceutical, Drug Screening Assays, Antitumor, Humans, Kinetics, Lactams, Models, Chemical, Phosphopeptides, Phosphorylation, Protein Conformation, Structure-Activity Relationship, Drug Design, Molecular Structure, Biomimetics, STAT3 Transcription Factor
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