ArticleMolecular medicine reports2015
Adapalene inhibits the activity of cyclin-dependent kinase 2 in colorectal carcinoma.
Article in Molecular medicine reports, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed, 63 citations in OpenAlex.
- Adapalene, an RAR agonist, exerts anti-inflammatory effects by regulating macrophage polarization through RAR[Formula: see text]-mediated signaling pathways.Scientific reports · 2026Article
- Unveiling the cytotoxic potential of four Callistemon fruit extracts against breast and colon cancer: a combined metabolomic and in silico approach.BMC complementary medicine and therapies · 2026Article
- Adapalene potentiates the cytotoxicity of anti-cancer drugs by enhancing cell cycle dysregulation and apoptosis in MKN-45 cells.Toxicology research · 2025Article
- Article
- Naringenin and its structural analogues inhibit CDK2: a combined MD-MMGBSA and protein-ligand interaction study for colon cancer.In silico pharmacology · 2025Article
- Cheminformatics-based screening and evaluation of phytochemicals as CDK2 inhibitors in colorectal cancer therapy.PloS one · 2025Article
- Molecular insights into kaempferol derivatives as potential inhibitors for CDK2 in colon cancer: pharmacophore modeling, docking, and dynamic analysis.Frontiers in chemistry · 2024Article
- Environmentally sensitive fluorescence of the topical retinoid adapalene.Frontiers in chemistry · 2024Article
- Article
- Current trends and future prospects of drug repositioning in gastrointestinal oncology.Frontiers in pharmacology · 2023Review
- Synthesis and Evaluation of Some New 4Pharmaceuticals (Basel, Switzerland) · 2022Article
- Modular and mechanistic changes across stages of colorectal cancer.BMC cancer · 2022Article
- Adapalene and Doxorubicin Synergistically Promote Apoptosis of TNBC Cells by Hyperactivation of the ERK1/2 Pathway Through ROS Induction.Frontiers in oncology · 2022Article
- Repurposing existing therapeutics, its importance in oncology drug development: Kinases as a potential target.British journal of clinical pharmacology · 2022Review
- Adapalene Inhibits Prostate Cancer Cell ProliferationFrontiers in pharmacology · 2022Article
- Adapalene inhibits the growth of triple-negative breast cancer cells by S-phase arrest and potentiates the antitumor efficacy of GDC-0941.Frontiers in pharmacology · 2022Article
- Virtual screening and drug repositioning of FDA-approved drugs from the ZINC database to identify the potential hTERT inhibitors.Frontiers in pharmacology · 2022Article
- Regulation Network of Colorectal-Cancer-Specific Enhancers in the Progression of Colorectal Cancer.International journal of molecular sciences · 2021Article
- COVID-19 pandemic is not the time of trial and error.The American journal of emergency medicine · 2021Article
- Discovery of vanoxerine dihydrochloride as a CDK2/4/6 triple-inhibitor for the treatment of human hepatocellular carcinoma.Molecular medicine (Cambridge, Mass.) · 2021Article
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Authors and funding
8 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Cyclin-dependent kinase 2 (CDK2) has been reported to be overexpressed in human colorectal cancer; it is responsible for the G1‑to‑S‑phase transition in the cell cycle and its deregulation is a hallmark of cancer. The present study was the first to use idock, a free and open‑source protein‑ligand docking software developed by our group, to identify potential CDK2 inhibitors from 4,311 US Food and Drug Administration‑approved small molecular drugs with a re‑purposing strategy. Among the top compounds identified by idock score, nine were selected for further study. Among them, adapalene (ADA; CD271,6‑[3‑(1‑adamantyl)‑4‑methoxyphenyl]‑2‑naphtoic acid) exhibited the highest anti‑proliferative effects in LOVO and DLD1 human colon cancer cell lines. Consistent with the expected properties of CDK2 inhibitors, the present study demonstrated that ADA significantly increased the G1‑phase population and decreased the expression of CDK2, cyclin E and retinoblastoma protein (Rb), as well as the phosphorylation of CDK2 (on Thr‑160) and Rb (on Ser‑795). Furthermore, the anti‑cancer effects of ADA were examined in vivo on xenograft tumors derived from DLD1 human colorectal cancer cells subcutaneously inoculated in BALB/C nude mice. ADA (20 mg/kg orally) exhibited marked anti‑tumor activity, comparable to that of oxaliplatin (40 mg/kg), and dose‑dependently inhibited tumor growth (P<0.05), while combined administration of ADA and oxaliplatin produced the highest therapeutic effect. To the best of our knowledge, the present study was the first to indicate that ADA inhibits CDK2 and is a potential candidate drug for the treatment of human colorectal cancer.
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