ReviewAnti-cancer agents in medicinal chemistry2010
Cilengitide: the first anti-angiogenic small molecule drug candidate design, synthesis and clinical evaluation.
Review in Anti-cancer agents in medicinal chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 255 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
255 citing papers in PubMed, 631 citations in OpenAlex.
- Treatment-associated imaging changes in newly diagnosed MGMT promoter-methylated glioblastoma undergoing chemoradiation with or without cilengitide.Neuro-oncology · 2024Trial
- Rewiring the tumor microenvironment: IGFBP2 at the Nexus of remodeling and therapy resistance?Biochimica et biophysica acta. Reviews on cancer · 2026Review
- Potential Role of the Urokinase-Type Plasminogen Activator Receptor-Integrin β3 Axis in Podocyte Adhesion Instability and Loss.Kidney international reports · 2026Article
- MiR-145-5p modulates collagen production and fibroblast behaviour after cardiac injury partially via COL5A1.Basic research in cardiology · 2026Article
- PEP-EDIT: a web server for the 3D generation and interactive editing of complex peptides.Nucleic acids research · 2026Article
- Backbone N-Methylation Improves PPCA-Binding of a Stylissatin A Analogue via Conformational Modulation.Chemistry, an Asian journal · 2026Article
- Surface decoration of solid lipid nanoparticles with cyclic RGD peptides for precision therapy in high-risk neuroblastoma.Drug delivery and translational research · 2026Article
- Metformin and cRGDfc-Modified Nanoparticles Loaded with Curcumin for Age-Related Macular Degeneration: In Vitro Pharmacodynamics and Molecular Mechanisms.Pharmaceutics · 2026Article
- Newly identified invasion drivers define the tumor front in oral squamous cell carcinoma.Cell death discovery · 2026Article
- Epithelial Integrins Coordinate Cellular Crosstalk Through the Regulation of Cytokines During Tissue Remodeling.International journal of molecular sciences · 2026Review
- Novel cilengitide derivatives suppress migration and invasion of temozolomide-resistant glioblastoma cells via MAPK/Akt pathway inhibition.Journal of neuro-oncology · 2026Article
- Overcoming Regorafenib Resistance in Colorectal Cancer: Synergistic Efficacy of Cilengitide in HT29 and WiDr Cells.Medeniyet medical journal · 2026Article
- Allosteric regulation of fibronectin binding by the anti-β1 integrin antibody TS2/16.PNAS nexus · 2026Article
- Small Particles, Big Impact: Inorganic Nanotechnology for Glioblastoma.Molecules (Basel, Switzerland) · 2026Review
- Identification of an αvβ3-targeting bicyclic peptide with atypical norArg-Gly-Asp sequence.Communications chemistry · 2026Article
- Integrin inhibition facilitates fibrocartilaginous transformation in connective tissue in osteoarthritis.Science advances · 2026Article
- Cancer-Associated Fibroblasts in the Treatment of Intrahepatic Cholangiocarcinoma: Present and Prospects.Journal of hepatocellular carcinoma · 2026Review
- Integrin β1 signaling at the crossroads of cellular plasticity, the tumor microenvironment, and therapy resistance in medulloblastoma.Frontiers in oncology · 2026Review
- Defining the role of integrins in melanoblast migrationMolecular biology of the cell · 2025Article
- Breast cancer cell coculture induces normal lung fibroblast transition to CAFs, promoting tumor cell dormancy and therapy resistance.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
195 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
3 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Cilengitide, a cyclic RGD pentapeptide, is currently in clinical phase III for treatment of glioblastomas and in phase II for several other tumors. This drug is the first anti-angiogenic small molecule targeting the integrins αvβ3, αvβ5 and αvβ1. It was developed by us in the early 90s by a novel procedure, the spatial screening. This strategy resulted in c(RGDfV), the first superactive αvβ3 inhibitor (100 to 1000 times increased activity over the linear reference peptides), which in addition exhibited high selectivity against the platelet receptor αIIbβ3. This cyclic peptide was later modified by N-methylation of one peptide bond to yield an even greater antagonistic activity in c(RGDf(NMe)V). This peptide was then dubbed Cilengitide and is currently developed as drug by the company Merck-Serono (Germany). This article describes the chemical development of Cilengitide, the biochemical background of its activity and a short review about the present clinical trials. The positive anti-angiogenic effects in cancer treatment can be further increased by combination with "classical" anti-cancer therapies. Several clinical trials in this direction are under investigation.
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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.