ArticleBioorganic & medicinal chemistry letters2011
Shp2 protein tyrosine phosphatase inhibitor activity of estramustine phosphate and its triterpenoid analogs.
Article in Bioorganic & medicinal chemistry letters, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 49 citations in OpenAlex.
- Screening of tyrosine phosphatase SHP2 (PTPN11) inhibitors from natural products with therapeutic potential for receptor tyrosine kinase-driven cancer.Journal of pharmaceutical analysis · 2026Article
- Targeting SHP2 with Natural Products: Exploring Saponin-Based Allosteric Inhibitors and Their Therapeutic Potential.Current issues in molecular biology · 2025Review
- Targeting RET Solvent-Front Mutants with Alkynyl Nicotinamide-Based Inhibitors.Molecular cancer therapeutics · 2023Article
- The heterogeneous transition state of resistance to RET kinase inhibitors converges on ERK1/2-driven Aurora A/B kinases.Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy · 2023Article
- PD-1 blockade delays tumor growth by inhibiting an intrinsic SHP2/Ras/MAPK signalling in thyroid cancer cells.Journal of experimental & clinical cancer research : CR · 2021Article
- Tyrosine phosphatase SHP2 inhibitors in tumor-targeted therapies.Acta pharmaceutica Sinica. B · 2021Review
- Unveiling the Molecular Basis of the Noonan Syndrome-Causing Mutation T42A of SHP2.International journal of molecular sciences · 2020Article
- Improving Obesity and Insulin Resistance by Targeting Skeletal Muscle MKP-1.Journal of cellular signaling · 2020Article
- SHP-2-Induced Activation of c-Myc Is Involved in PDGF-B-Regulated Cell Proliferation and Angiogenesis in RMECs.Frontiers in physiology · 2020Article
- Structural basis of resistance of mutant RET protein-tyrosine kinase to its inhibitors nintedanib and vandetanib.The Journal of biological chemistry · 2019Article
- Drug resistance profiles of mutations in the RET kinase domain.British journal of pharmacology · 2018Article
- Protein tyrosine phosphatases in cardiac physiology and pathophysiology.Heart failure reviews · 2018Review
- The impact of structural biology in medicine illustrated with four case studies.Journal of molecular medicine (Berlin, Germany) · 2018Review
- Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases.Nature · 2016Article
- Inhibition of SHP2-mediated dephosphorylation of Ras suppresses oncogenesis.Nature communications · 2015Article
- Therapeutic potential of targeting the oncogenic SHP2 phosphatase.Journal of medicinal chemistry · 2014Article
- Small molecule inhibitors of SHP2 tyrosine phosphatase discovered by virtual screening.Bioorganic & medicinal chemistry letters · 2011Article
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Authors and funding
9 authors at 4 institutions in 1 country.
Funding
Abstract
Shp2 protein tyrosine phosphate (PTP) is a novel target for anticancer drug discovery. We identified estramustine phosphate as a Shp2 PTP inhibitor from the National Cancer Institute Approved Oncology Drug set. A focused structure-activity relationship study indicated that the 17-phosphate group is required for the Shp2 PTP inhibitor activity of estramustine phosphate. A search for estramustine phosphate analogs led to identification of two triterpenoids, enoxolone, and celastrol, having Shp2 PTP inhibitor activity. With the previously reported PTP1B inhibitor trodusquemine, our study reveals steroids and triterpenoids with negatively charged phosphate, carboxylate, or sulfonate groups as novel pharmacophores of selective PTP inhibitors.
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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.