g1 phase cell cycle checkpoints


Summary: Regulatory signaling systems that control the progression of the CELL CYCLE through the G1 PHASE and allow transition to S PHASE when the cells are ready to undergo DNA REPLICATION. DNA DAMAGE, or the deficiencies in specific cellular components or nutrients may cause the cells to halt before progressing through G1 phase.

Top Publications

  1. Zhao J, Zhao J, Jiao H. Synergistic growth-suppressive effects of quercetin and cisplatin on HepG2 human hepatocellular carcinoma cells. Appl Biochem Biotechnol. 2014;172:784-91 pubmed
  2. Wang R, Ma J, Wang M, Cui J, Wu W, Liu R, et al. A Human Long Non-Coding RNA ALT1 Controls the Cell Cycle of Vascular Endothelial Cells Via ACE2 and Cyclin D1 Pathway. Cell Physiol Biochem. 2017;43:1152-1167 pubmed publisher
    ..The results suggested the human long non-coding RNA ALT1 is a novel regulator for cell cycle of HUVECs via ACE2 and cyclin D1 pathway. ..
  3. Jiang L, Zhao Z, Zheng L, Xue L, Zhan Q, Song Y. Downregulation of miR-503 Promotes ESCC Cell Proliferation, Migration, and Invasion by Targeting Cyclin D1. Genomics Proteomics Bioinformatics. 2017;15:208-217 pubmed publisher
    ..Our study further identified CCND1 as the target gene of miR-503. Thus, miR-503 functions as a tumor suppressor and has an important role in ESCC by targeting CCND1. ..
  4. Hu W, Wei H, Li K, Li P, Lin J, Feng R. Downregulation of USP32 inhibits cell proliferation, migration and invasion in human small cell lung cancer. Cell Prolif. 2017;50: pubmed publisher
    ..Our results suggest for the first time that USP32 is important for SCLC progression and might be a potential target for molecular therapy of SCLC. ..
  5. Urbaniak A, Delgado M, Kacprzak K, Chambers T. Activity of resveratrol triesters against primary acute lymphoblastic leukemia cells. Bioorg Med Chem Lett. 2017;27:2766-2770 pubmed publisher
    ..Moreover, the compounds were only effective in cycling cells, with cells arrested in G1 phase being refractory. ..
  6. Sun C, Ma P, Wang Y, Liu W, Chen Q, Pan Y, et al. KLF15 Inhibits Cell Proliferation in Gastric Cancer Cells via Up-Regulating CDKN1A/p21 and CDKN1C/p57 Expression. Dig Dis Sci. 2017;62:1518-1526 pubmed publisher
    ..These findings demonstrate that KLF15 plays a significant role in GC progression and could be a therapeutic target for GC. ..
  7. Yothaisong S, Dokduang H, Anzai N, Hayashi K, Namwat N, Yongvanit P, et al. Inhibition of l-type amino acid transporter 1 activity as a new therapeutic target for cholangiocarcinoma treatment. Tumour Biol. 2017;39:1010428317694545 pubmed publisher
    ..Our study demonstrates that suppression of l-type amino acid transporter-1 activity using JPH203 might be used as a new therapeutic strategy for cholangiocarcinoma treatment. ..
  8. Mombach J, Bugs C, Chaouiya C. Modelling the onset of senescence at the G1/S cell cycle checkpoint. BMC Genomics. 2014;15 Suppl 7:S7 pubmed publisher
    ..This model qualitatively agrees with most experimental observations, including experiments involving mutations. Furthermore, it provides some predictions. ..
  9. Fu S, Tang Y, Huang X, Feng M, Xu A, Lan H. Smad7 protects against acute kidney injury by rescuing tubular epithelial cells from the G1 cell cycle arrest. Clin Sci (Lond). 2017;131:1955-1969 pubmed publisher
    ..In conclusion, Smad7 plays a protective role in AKI. Blockade of TGF-?/Smad3-p21/p27-induced G1 cell cycle arrest may be a key mechanism by which Smad7 treatment inhibits AKI. Thus, Smad7 may be a novel therapeutic agent for AKI. ..

More Information


  1. Omer F, Hashim N, Ibrahim M, Dehghan F, Yahayu M, Karimian H, et al. Beta-mangostin from Cratoxylum arborescens activates the intrinsic apoptosis pathway through reactive oxygen species with downregulation of the HSP70 gene in the HL60 cells associated with a G0/G1 cell-cycle arrest. Tumour Biol. 2017;39:1010428317731451 pubmed publisher
    ..Overall, the results for ?-mangostin showed an antiproliferative effect in HL60 via stopping the cell cycle at the G0/G1 phase and prompted the intrinsic apoptosis pathway...
  2. Beguelin W, Rivas M, Calvo Fernández M, Teater M, Purwada A, Redmond D, et al. EZH2 enables germinal centre formation through epigenetic silencing of CDKN1A and an Rb-E2F1 feedback loop. Nat Commun. 2017;8:877 pubmed publisher
    ..Here the authors use a 3D GC organoid and show EZH2 mediates germinal centre (GC) formation through epigenetic silencing of CDKN1A and release of cell cycle checkpoints. ..
  3. Takahashi N, Koyama S, Hasegawa S, Yamasaki M, Imai M. Anticancer efficacy of p-dodecylaminophenol against high-risk and refractory neuroblastoma cells in vitro and in vivo. Bioorg Med Chem Lett. 2017;27:4664-4672 pubmed publisher
    ..Compound 3 may have potential for clinical use in the treatment of refractory neuroblastoma with reduced side effects. ..
  4. Barzegar M, Ma S, Zhang C, Chen X, Gu Y, Shang C, et al. SKLB188 inhibits the growth of head and neck squamous cell carcinoma by suppressing EGFR signalling. Br J Cancer. 2017;117:1154-1163 pubmed publisher
    ..The results provide a basis for further clinical investigation of SKLB188 as a targeted therapy for HNSCC. Our findings may open a new avenue for development of novel EGFR inhibitors for treatment of HNSCC and other cancers. ..
  5. Poursani E, Mehravar M, Soltani B, Mowla S. Novel variant of OCT4B4 is differentially expressed in human embryonic stem and embryonic carcinoma cells. Gene. 2017;627:369-372 pubmed publisher
    ..Moreover, knocking down of OCT4B4 by shRNA resulted in increased accumulation of transfected cells in G0/G1 phase compared to the mock-transfected control cells. ..
  6. Miglionico R, Ostuni A, Armentano M, Milella L, Crescenzi E, Carmosino M, et al. ABCC6 knockdown in HepG2 cells induces a senescent-like cell phenotype. Cell Mol Biol Lett. 2017;22:7 pubmed publisher
    ..These findings show that the absence of ABCC6 profoundly changes the HepG2 phenotype, suggesting that the PXE syndrome is a complex metabolic disease that is not exclusively related to the absence of pyrophosphate in the bloodstream. ..
  7. Zhang R, Song L, Jiang B, Wang L, Wu N, Guo S, et al. Design of antitumor agents containing carbohydrate based on GLUT1, and evaluation of antiproliferative activity. Bioorg Med Chem Lett. 2017;27:2488-2492 pubmed publisher
    ..Moreover, compound 9 blocked A549 cells at the G0/G1 phase. The cellular uptake studies suggested that ribose-modified compound 9 could be taken through GLUT1 in A549 cell line. ..
  8. Li Y, Ye J, Chen Z, Wen J, Li F, Su P, et al. Annonaceous acetogenins mediated up-regulation of Notch2 exerts growth inhibition in human gastric cancer cells in vitro. Oncotarget. 2017;8:21140-21152 pubmed publisher
    ..Furthermore, Notch2-siRNA transfection and Notch2-cDNA were performed to investigate the role of Notch2 in the antitumor effect of ACGs. Up-regulation of Notch2 by ACGs is a potential therapeutic strategy for GC. ..
  9. Chen L, Zhang S, Wu J, Cui J, Zhong L, Zeng L, et al. circRNA_100290 plays a role in oral cancer by functioning as a sponge of the miR-29 family. Oncogene. 2017;36:4551-4561 pubmed publisher
    ..Taken together, it indicates that circRNAs may exert regulatory functions in OSCC and may be a potential target for OSCC therapy. ..
  10. Liu Z, Lou H, Xie K, Wang H, Chen N, Aparicio O, et al. Reconstructing cell cycle pseudo time-series via single-cell transcriptome data. Nat Commun. 2017;8:22 pubmed publisher
  11. Lewinska A, Adamczyk Grochala J, Kwasniewicz E, Deregowska A, Wnuk M. Ursolic acid-mediated changes in glycolytic pathway promote cytotoxic autophagy and apoptosis in phenotypically different breast cancer cells. Apoptosis. 2017;22:800-815 pubmed publisher
    ..Taken together, we have shown for the first time that UA at low micromolar range may promote its anticancer action by targeting glycolysis in phenotypically distinct breast cancer cells. ..
  12. Cho S, Lee H, Cho S, Kim B, Jung Y, Kim S. Particled Mica, STB-HO has chemopreventive potential via G1 arrest, and inhibition of proliferation and vascular endothelial growth factor receptor 2 in HCT colorectal cancer cells. BMC Complement Altern Med. 2013;13:189 pubmed publisher
    ..Collectively, these findings suggest that STB-HO has chemopreventive potential via G1 arrest and inhibition of proliferation and VEGFR2 in HCT116 colorectal cancer cells. ..
  13. Wang W, Zhao Y, Yao S, Cui X, Pan W, Huang W, et al. Nigericin Inhibits Epithelial Ovarian Cancer Metastasis by Suppressing the Cell Cycle and Epithelial-Mesenchymal Transition. Biochemistry (Mosc). 2017;82:933-941 pubmed publisher
    ..Nigericin may prove to be a novel therapeutic strategy that is effective in patients with metastatic EOC. ..
  14. Faria M, Matos P, Pereira T, Cabrera R, Cardoso B, Bugalho M, et al. RAC1b overexpression stimulates proliferation and NF-kB-mediated anti-apoptotic signaling in thyroid cancer cells. PLoS ONE. 2017;12:e0172689 pubmed publisher
  15. Vue B, Zhang X, Lee T, Nair N, Zhang S, Chen G, et al. 5- or/and 20-O-alkyl-2,3-dehydrosilybins: Synthesis and biological profiles on prostate cancer cell models. Bioorg Med Chem. 2017;25:4845-4854 pubmed publisher
    ..Our flow cytometry-based assays also demonstrate that 5-O-heptyl-2,3-dehydrosilybin effectively arrests the cell cycle in the G0/G1 phase and activates PC-3 cell apoptosis. ..
  16. Jakovljević K, Matić I, Stanojkovic T, Krivokuca A, Marković V, Joksović M, et al. Synthesis, antioxidant and antiproliferative activities of 1,3,4-thiadiazoles derived from phenolic acids. Bioorg Med Chem Lett. 2017;27:3709-3715 pubmed publisher
    ..Furthermore, compounds 3c, 3'c, 3'g and 3'h showed the ability to down-regulate the MMP2 and VEGFA expression levels in the treated HL-60 cells when compared with the control cell samples. ..
  17. Ribas R, Ghazoui Z, Gao Q, Pancholi S, Rani A, Dunbier A, et al. Identification of chemokine receptors as potential modulators of endocrine resistance in oestrogen receptor-positive breast cancers. Breast Cancer Res. 2014;16:447 pubmed publisher
    ..These data highlight CXCR7 as a potential therapeutic target warranting clinical investigation in endocrine-resistant BC. ..
  18. Zhu K, Zhang C. [Sensitivity of doxorubicin-resistant osteosarcoma cells to doxorubicin regulated by long non-coding RNA NR_036444]. Zhonghua Zhong Liu Za Zhi. 2017;39:250-255 pubmed publisher
  19. Yamashita N, Kondo M, Zhao S, Li W, Koike K, Nemoto K, et al. Picrasidine G decreases viability of MDA-MB 468 EGFR-overexpressing triple-negative breast cancer cells through inhibition of EGFR/STAT3 signaling pathway. Bioorg Med Chem Lett. 2017;27:2608-2612 pubmed publisher
    ..These results suggest that PG may contribute to the development of targeted therapy of patients with EGFR-overexpressing TNBC. ..
  20. Liang S, Yu H, Chen X, Shen T, Cui Z, Si G, et al. PDGF-BB/KLF4/VEGF Signaling Axis in Pulmonary Artery Endothelial Cell Angiogenesis. Cell Physiol Biochem. 2017;41:2333-2349 pubmed publisher
    ..Overall, our study contributes to a better understanding of PAH pathogenesis. ..
  21. Zhu S, Huang J, Peng W, Wu D, Luo M, Li Q, et al. Inhibition of smoothened decreases proliferation of synoviocytes in rheumatoid arthritis. Cell Mol Immunol. 2017;14:214-222 pubmed publisher
    ..05). The results suggest that Shh signaling plays an important role in RA-FLSs proliferation in a Smo-dependent manner and may contribute to synovial hyperplasia. Targeting Shh signaling may help control joint damage in patients with RA. ..
  22. Yang L, Wen Y, Lv G, Lin Y, Tang J, Lu J, et al. ?-Lipoic acid inhibits human lung cancer cell proliferation through Grb2-mediated EGFR downregulation. Biochem Biophys Res Commun. 2017;494:325-331 pubmed publisher
    ..Recently, ? -LA has been reported to inhibit the growth of various cancer cells, but the precise signaling pathways that mediate the effects of ? -LA on non-small cell lung cancer (NSCLC) development remain unclear...
  23. Long B, Wang L, Zheng F, Lai S, Xu D, Hu Y, et al. Targeting GLI1 Suppresses Cell Growth and Enhances Chemosensitivity in CD34+ Enriched Acute Myeloid Leukemia Progenitor Cells. Cell Physiol Biochem. 2016;38:1288-302 pubmed publisher
    ..The present findings suggested that Hh signaling was activated in AML progenitor cells. GLI1 acted as a potential target for AML therapy. ..
  24. Wang Y, Huang Z, Chen S, Wang C, Shan C, Yin Q, et al. Design, Synthesis, and Evaluation of New Selective NM23-H2 Binders as c-MYC Transcription Inhibitors via Disruption of the NM23-H2/G-Quadruplex Interaction. J Med Chem. 2017;60:6924-6941 pubmed publisher
    ..This work provides a new strategy to modulate c-MYC transcription for the development of selective anticancer drugs. ..
  25. Husain I, Bala K, Wani A, Makhdoomi U, Malik F, Sharma A. Arginase purified from endophytic Pseudomonas aeruginosa IH2: Induce apoptosis through both cell cycle arrest and MMP loss in human leukemic HL-60 cells. Chem Biol Interact. 2017;274:35-49 pubmed publisher
    ..Purified arginase did not exert cytotoxic effects on human noncancer cells. Our study strongly supports that arginase could be used as potent anticancer agent but further studies are required which are underway in our lab. ..
  26. Ye M, Huang W, Wu W, Liu Y, Ye S, Xu J. FM807, a curcumin analogue, shows potent antitumor effects in nasopharyngeal carcinoma cells by heat shock protein 90 inhibition. Oncotarget. 2017;8:15364-15376 pubmed publisher
    ..In conjunction with its low toxicity in NPC xenograft mice, these results provide a sound preclinical basis for further development of FM807 as a novel therapeutic agent in the treatment of NPC. ..
  27. Li W, Zhang H, Nie M, Tian Y, Chen X, Chen C, et al. Ursolic acid derivative FZU-03,010 inhibits STAT3 and induces cell cycle arrest and apoptosis in renal and breast cancer cells. Acta Biochim Biophys Sin (Shanghai). 2017;49:367-373 pubmed publisher
    ..In conclusion, our results suggest that the UA derivative FZU-03,010 is more potent in inhibiting cancer cell survival, and FZU-03,010 has the potential to be developed as a therapeutic for renal cell cancers and TNBCs. ..
  28. Deng M, Zeng C, Lu X, He X, Zhang R, Qiu Q, et al. miR-218 suppresses gastric cancer cell cycle progression through the CDK6/Cyclin D1/E2F1 axis in a feedback loop. Cancer Lett. 2017;403:175-185 pubmed publisher
    ..Taken together, our results describe a regulatory loop miR-218-CDK6/CyclinD1-E2F1 whose disruption may contribute to cell cycle progression in gastric cancer and indicate the potential application of miR-218 in cancer therapy. ..
  29. Xu J, Zhang R, Zhao J. The Novel Long Noncoding RNA TUSC7 Inhibits Proliferation by Sponging MiR-211 in Colorectal Cancer. Cell Physiol Biochem. 2017;41:635-644 pubmed publisher
    ..To summary, we demonstrated that TUSC7 is a potential tumor suppressor in CRC, and TUSC7 could inhibit CRC cell proliferation by completely sponging miR-211-3p. ..
  30. Mawas A, Amatya V, Suzuki R, Kushitani K, Mohi El Din M, Takeshima Y. PIM1 knockdown inhibits cell proliferation and invasion of mesothelioma cells. Int J Oncol. 2017;50:1029-1034 pubmed publisher
    ..Considering the mesothelioma as rapidly growing invasive cancer, downregulation of PIM1 may have a potential role for therapeutic management of malignant mesothelioma. ..
  31. Shi R, Zhang C, Wu Y, Wang X, Sun Q, Sun J, et al. CDCA2 promotes lung adenocarcinoma cell proliferation and predicts poor survival in lung adenocarcinoma patients. Oncotarget. 2017;8:19768-19779 pubmed publisher
    ..Moreover, the oncogenic activity of CDCA2 was also confirmed in vivo. In conclusion, CDCA2 promotes proliferation of LAC cells and predicts poor prognosis in LAC patients. CDCA2 might play a significant role in LAC progression. ..
  32. Peng Y, Qiu L, Xu D, Zhang L, Yu H, Ding Y, et al. M4IDP, a zoledronic acid derivative, induces G1 arrest, apoptosis and autophagy in HCT116 colon carcinoma cells via blocking PI3K/Akt/mTOR pathway. Life Sci. 2017;185:63-72 pubmed publisher
    ..This study also provides a better understanding of the antitumor effects and the underlying mechanisms of bisphosphonates in the field of CRC therapy. ..
  33. Magiera K, Tomala M, Kubica K, De Cesare V, Trost M, Zieba B, et al. Lithocholic Acid Hydroxyamide Destabilizes Cyclin D1 and Induces G0/G1 Arrest by Inhibiting Deubiquitinase USP2a. Cell Chem Biol. 2017;24:458-470.e18 pubmed publisher
    ..We show that LCA derivatives may be considered as future therapeutics for the treatment of cyclin D1-addicted p53-expressing and p53-defective cancer types. ..
  34. Nawale L, Dubey P, Chaudhari B, Sarkar D, Prabhune A. Anti-proliferative effect of novel primary cetyl alcohol derived sophorolipids against human cervical cancer cells HeLa. PLoS ONE. 2017;12:e0174241 pubmed publisher
    ..All these findings suggest that these SLCAs could be explored for their chemopreventive potential in cervical cancer. ..
  35. Takeuchi S, Kasamatsu A, Yamatoji M, Nakashima D, Endo Sakamoto Y, Koide N, et al. TEAD4-YAP interaction regulates tumoral growth by controlling cell-cycle arrest at the G1 phase. Biochem Biophys Res Commun. 2017;486:385-390 pubmed publisher
    ..Taken together, we concluded that TEAD4 might play an important role in tumoral growth and have potential to be a therapeutic target in OSCCs. ..
  36. Tadesse S, Zhu G, Mekonnen L, Lenjisa J, Yu M, Brown M, et al. A novel series of N-(pyridin-2-yl)-4-(thiazol-5-yl)pyrimidin-2-amines as highly potent CDK4/6 inhibitors. Future Med Chem. 2017;9:1495-1506 pubmed publisher
    ..Compounds 58 and 69 caused remarkable growth inhibition of melanoma cells, particularly the cells harboring multiple BRAF and NRAS mutations, via a CDK4/6-targeted mechanism of action. [Formula: see text]. ..
  37. Kim H, Chang J, Shao L, Han L, Iyer S, Manolagas S, et al. DNA damage and senescence in osteoprogenitors expressing Osx1 may cause their decrease with age. Aging Cell. 2017;16:693-703 pubmed publisher
    ..Together, these findings suggest that the decline in bone mass with age is the result of intrinsic defects in osteoprogenitor cells, leading to decreased osteoblast numbers and increased support of osteoclast formation. ..
  38. Câmara D, Porcacchia A, Costa A, Azevedo R, Kerkis I. Murine melanoma cells incomplete reprogramming using non-viral vector. Cell Prolif. 2017;50: pubmed publisher
    ..These cells represent an interesting model to study mechanism of cells malignancy as well as provide a novel tool for anti-cancer drugs screening. ..
  39. Karthik R, Manigandan V, Ebenezar K, Vijayashree R, Saravanan R. In vitro and in vivo anticancer activity of posterior salivary gland toxin from the cuttlefish Sepia pharaonis, Ehrenberg (1831). Chem Biol Interact. 2017;272:10-20 pubmed publisher
    ..The results of the present study showed that the PSG toxin exhibited immense promise as a potential peptide based anticancer agent, in future. ..
  40. Mo Q, Hu L, Weng J, Zhang Y, Zhou Y, Xu R, et al. Euptox A Induces G1 Arrest and Autophagy via p38 MAPK- and PI3K/Akt/mTOR-Mediated Pathways in Mouse Splenocytes. J Histochem Cytochem. 2017;65:543-558 pubmed publisher
    ..These findings provide new insights into the mechanisms involved in spleen toxicity caused by Euptox A in mice. ..
  41. Guo B, Zhao Z, Wang Z, Li Q, Wang X, Wang W, et al. MicroRNA-302b-3p Suppresses Cell Proliferation Through AKT Pathway by Targeting IGF-1R in Human Gastric Cancer. Cell Physiol Biochem. 2017;42:1701-1711 pubmed publisher
    ..These results indicate the tumor suppressor role of miR-302b-3p in the pathogenesis of gastric cancer. ..
  42. Xie W, Wu M, Fu T, Li X, Wang Z, Hu Y, et al. ICT1 predicts a poor survival and correlated with cell proliferation in diffuse large B-cell lymphoma. Gene. 2017;627:255-262 pubmed publisher
    ..Taken together, this study suggested that ICT1 may play an oncogenic role in human DLBCL by promoting cell proliferation and it might be a biomarker of unfavorable prognosis in DLBCL patients. ..
  43. Sun G, Zheng Z, Lee M, Xu Y, Kang S, Dong Z, et al. Chemoprevention of Colorectal Cancer by Artocarpin, a Dietary Phytochemical from Artocarpus heterophyllus. J Agric Food Chem. 2017;65:3474-3480 pubmed publisher
    ..Taken together, artocarpin, a bioactive component of A. heterophyllus, might merit investigation as a potential colorectal cancer chemopreventive agent. ..