ArticleChemistry & biology2012
Identification and characterization of small molecule antagonists of pRb inactivation by viral oncoproteins.
Article in Chemistry & biology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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
17 citing papers in PubMed, 33 citations in OpenAlex.
- Targeting LxCxE Cleft Pocket of Retinoblastoma Protein in Immunosuppressive Macrophages Inhibits Ovarian Cancer Progression.Cancer immunology research · 2025Article
- Review
- Small Molecule Inhibitors of Human Papillomavirus: A Review of Research from 1997 to 2021.Current medicinal chemistry · 2024Review
- Structural basis for tunable affinity and specificity of LxCxE-dependent protein interactions with the retinoblastoma protein family.Structure (London, England : 1993) · 2022Article
- Structure and function of MuvB complexes.Oncogene · 2022Review
- YAP-Mediated Recruitment of YY1 and EZH2 Represses Transcription of Key Cell-Cycle Regulators.Cancer research · 2020Article
- Theileria parasites subvert E2F signaling to stimulate leukocyte proliferation.Scientific reports · 2020Article
- Basic Science, Epidemiology, and Screening for Anal Intraepithelial Neoplasia and Its Relationship to Anal Squamous Cell Cancer.Clinics in colon and rectal surgery · 2018Review
- Recruitment of Antigen Presenting Cells to Skin Draining Lymph Node From HPV16E7-Expressing Skin Requires E7-Rb Interaction.Frontiers in immunology · 2018Article
- Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.Journal of medicinal chemistry · 2016Article
- A Strategy for Direct Chemical Activation of the Retinoblastoma Protein.ACS chemical biology · 2016Article
- Review
- Molecular Determinants for the Inactivation of the Retinoblastoma Tumor Suppressor by the Viral Cyclin-dependent Kinase UL97.The Journal of biological chemistry · 2015Article
- Structural mechanisms of DREAM complex assembly and regulation.Genes & development · 2015Article
- Proteome-wide analysis of human disease mutations in short linear motifs: neglected players in cancer?Molecular bioSystems · 2014Article
- Identification and characterization of small molecule human papillomavirus E6 inhibitors.ACS chemical biology · 2014Article
- Molecular mechanisms underlying RB protein function.Nature reviews. Molecular cell biology · 2013Review
Corrections and comments
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Authors and funding
10 authors at 3 institutions in 1 country.
Funding
Abstract
The retinoblastoma protein pRb is essential for regulating many cellular activities through its binding and inhibition of E2F transcription activators, and pRb inactivation leads to many cancers. pRb activity can be perturbed by viral oncoproteins including human papillomavirus (HPV) that share an LxCxE motif. Because there are no treatments for existing HPV infection leading to nearly all cervical cancers and other cancers to a lesser extent, we screened for compounds that inhibit the ability of HPV-E7 to disrupt pRb/E2F complexes. This lead to the identification of thiadiazolidinedione compounds that bind to pRb with mid-high nanomolar dissociation constants, are competitive with the binding of viral oncoproteins containing an LxCxE motif, and are selectively cytotoxic in HPV-positive cells alone and in mice. These inhibitors provide a promising scaffold for the development of therapies to treat HPV-mediated pathologies.
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What OpenQuestion holds
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.