Genomes and Genes
platelet derived growth factor receptors
Summary: Specific receptors on cell membranes that react with PLATELET-DERIVED GROWTH FACTOR, its analogs, or antagonists. The alpha PDGF receptor (RECEPTOR, PLATELET-DERIVED GROWTH FACTOR ALPHA) and the beta PDGF receptor (RECEPTOR, PLATELET-DERIVED GROWTH FACTOR BETA) are the two principle types of PDGF receptors. Activation of the protein-tyrosine kinase activity of the receptors occurs by ligand-induced dimerization or heterodimerization of PDGF receptor types.
- Jones A, Cross N. Oncogenic derivatives of platelet-derived growth factor receptors. Cell Mol Life Sci. 2004;61:2912-23 pubmed..PDGFR signalling is inhibited by imatinib mesylate, and this compound has clear clinical activity in patients with myeloid malignancies, GIST and DFSP. ..
- Zymek P, Bujak M, Chatila K, Cieslak A, Thakker G, Entman M, et al. The role of platelet-derived growth factor signaling in healing myocardial infarcts. J Am Coll Cardiol. 2006;48:2315-23 pubmed..Acquisition of a mural coat and maturation of the vasculature promotes resolution of inflammation and stabilization of the scar. ..
- Zhang H, Bajraszewski N, Wu E, Wang H, Moseman A, Dabora S, et al. PDGFRs are critical for PI3K/Akt activation and negatively regulated by mTOR. J Clin Invest. 2007;117:730-8 pubmed..In conclusion, PDGFR is a major target of negative feedback regulation in cells with activated mTOR, which limits the growth potential of TSC tumors. ..
- Kim S, Uehara H, Yazici S, Busby J, Nakamura T, He J, et al. Targeting platelet-derived growth factor receptor on endothelial cells of multidrug-resistant prostate cancer. J Natl Cancer Inst. 2006;98:783-93 pubmed..001), which was followed by apoptosis of tumor cells. Tumor-associated endothelial cells, rather than tumor cells themselves, appear to be the target for imatinib in prostate cancer bone metastasis. ..
- Daniels C, Wilkes M, Edens M, Kottom T, Murphy S, Limper A, et al. Imatinib mesylate inhibits the profibrogenic activity of TGF-beta and prevents bleomycin-mediated lung fibrosis. J Clin Invest. 2004;114:1308-16 pubmed..Thus, Abl family members represent common targets for the modulation of profibrotic cytokine signaling. ..
- Pietras K, Hanahan D. A multitargeted, metronomic, and maximum-tolerated dose "chemo-switch" regimen is antiangiogenic, producing objective responses and survival benefit in a mouse model of cancer. J Clin Oncol. 2005;23:939-52 pubmed
- Abdollahi A, Li M, Ping G, Plathow C, Domhan S, Kiessling F, et al. Inhibition of platelet-derived growth factor signaling attenuates pulmonary fibrosis. J Exp Med. 2005;201:925-35 pubmed..This study points the way to a potential new approach for treating idiopathic or therapy-related forms of lung fibrosis. ..
- Motzer R, Hutson T, Tomczak P, Michaelson M, Bukowski R, Rixe O, et al. Sunitinib versus interferon alfa in metastatic renal-cell carcinoma. N Engl J Med. 2007;356:115-24 pubmed..gov numbers, NCT00098657 and NCT00083889 [ClinicalTrials.gov]). ..
- Haberler C, Gelpi E, Marosi C, Rossler K, Birner P, Budka H, et al. Immunohistochemical analysis of platelet-derived growth factor receptor-alpha, -beta, c-kit, c-abl, and arg proteins in glioblastoma: possible implications for patient selection for imatinib mesylate therapy. J Neurooncol. 2006;76:105-9 pubmed..The value of anti-tyrosine kinase immunolabeling as predictive factor for patient selection remains to be clarified by comparative analysis of tumor tissue of therapy-responders versus non-responders. ..
- Reigstad L, Varhaug J, Lillehaug J. Structural and functional specificities of PDGF-C and PDGF-D, the novel members of the platelet-derived growth factors family. FEBS J. 2005;272:5723-41 pubmed..PDGF-C is expressed in Ewing family sarcoma and PDGF-D is linked to lung, prostate and ovarian cancers. Both PDGF-C and -D play a role in progressive renal disease, glioblastoma/medulloblastoma and fibrosis in several organs. ..
- Takahashi Y, Morales F, Kreimann E, Georgescu M. PTEN tumor suppressor associates with NHERF proteins to attenuate PDGF receptor signaling. EMBO J. 2006;25:910-20 pubmed..These data indicate that, in normal cells, NHERF proteins recruit PTEN to PDGFR to restrict the activation of the PI3K. ..
- Zhang H, Cicchetti G, Onda H, Koon H, Asrican K, Bajraszewski N, et al. Loss of Tsc1/Tsc2 activates mTOR and disrupts PI3K-Akt signaling through downregulation of PDGFR. J Clin Invest. 2003;112:1223-33 pubmed..This is in contrast to PTEN, which is a negative upstream regulator of this pathway. ..
- Tada H, Ogushi F, Tani K, Nishioka Y, Miyata J, Sato K, et al. Increased binding and chemotactic capacities of PDGF-BB on fibroblasts in radiation pneumonitis. Radiat Res. 2003;159:805-11 pubmed
- Bergers G, Song S, Meyer Morse N, Bergsland E, Hanahan D. Benefits of targeting both pericytes and endothelial cells in the tumor vasculature with kinase inhibitors. J Clin Invest. 2003;111:1287-95 pubmed..Thus, combinatorial targeting of receptor tyrosine kinases shows promise for treating multiple stages in tumorigenesis, most notably the often-intractable late-stage solid tumor...
- Uehara H, Kim S, Karashima T, Shepherd D, Fan D, Tsan R, et al. Effects of blocking platelet-derived growth factor-receptor signaling in a mouse model of experimental prostate cancer bone metastases. J Natl Cancer Inst. 2003;95:458-70 pubmed..Using STI571 to inhibit PDGF-R phosphorylation may, especially in combination with paclitaxel, produce substantial therapeutic effects against prostate cancer bone metastasis. ..
- Zhuo Y, Zhang J, Laboy M, Lasky J. Modulation of PDGF-C and PDGF-D expression during bleomycin-induced lung fibrosis. Am J Physiol Lung Cell Mol Physiol. 2004;286:L182-8 pubmed..Moreover, there is in vivo phosphorylation of the PDGF-receptor that binds PDGF-C in response to bleomycin administration. These observations strongly suggest a role for PDGF-C in bleomycin-induced pulmonary fibrosis. ..
- Pietras K, Sjoblom T, Rubin K, Heldin C, Ostman A. PDGF receptors as cancer drug targets. Cancer Cell. 2003;3:439-43 pubmed
- Haglund K, Di Fiore P, Dikic I. Distinct monoubiquitin signals in receptor endocytosis. Trends Biochem Sci. 2003;28:598-603 pubmed
- Levitzki A. PDGF receptor kinase inhibitors for the treatment of PDGF driven diseases. Cytokine Growth Factor Rev. 2004;15:229-35 pubmed..The possible utilization of PDGFR kinase inhibitors as anti-restenosis agents is likely to move ahead of the utilization of these agents to treat human malignancies. ..
- Yu J, Ustach C, Kim H. Platelet-derived growth factor signaling and human cancer. J Biochem Mol Biol. 2003;36:49-59 pubmed
- Savikko J, Taskinen E, von Willebrand E. Chronic allograft nephropathy is prevented by inhibition of platelet-derived growth factor receptor: tyrosine kinase inhibitors as a potential therapy. Transplantation. 2003;75:1147-53 pubmed..On the basis of our findings, imatinib could be a potential intervention in preventing CAN in clinical kidney transplantation. ..
- Lei H, Velez G, Hovland P, Hirose T, Kazlauskas A. Plasmin is the major protease responsible for processing PDGF-C in the vitreous of patients with proliferative vitreoretinopathy. Invest Ophthalmol Vis Sci. 2008;49:42-8 pubmed publisher..These observations are the first report of an in vivo protease responsible for processing PDGF-C. In addition, plasmin was identified as a novel therapeutic target for patients with PVR. ..
- Chen Z, Lee F, Bhalla K, Wu J. Potent inhibition of platelet-derived growth factor-induced responses in vascular smooth muscle cells by BMS-354825 (dasatinib). Mol Pharmacol. 2006;69:1527-33 pubmed..These results suggest that BMS-354825 is a potent inhibitor of PDGF-stimulated VSMC activities and a potential agent for the development of a new therapy for vascular obstructive diseases such as restenosis. ..
- Sihto H, Franssila K, Tanner M, Vasama Nolvi C, Sarlomo Rikala M, Nupponen N, et al. Platelet-derived growth factor receptor family mutations in gastrointestinal stromal tumours. Scand J Gastroenterol. 2006;41:805-11 pubmed..GISTs with PDGFRA mutations often have reduced expression of the KIT protein in immunohistochemistry, suggesting that immunohistochemistry may be potentially useful in identification of such GISTs. ..
- Coyle D, Doyle B, Murphy J, O Donnell A, Gillick J, Puri P. Expression of connexin 26 and connexin 43 is reduced in Hirschsprung's disease. J Surg Res. 2016;206:242-251 pubmed publisher..Reduced expression of Cx26 and Cx43 is implicated in the pathophysiology of colonic dysmotility in the aganglionic bowel as well as, in the case of Cx26, the ganglionic bowel in HSCR. ..
- Chen Q, Zhang H, Liu Y, Adams S, Eilken H, Stehling M, et al. Endothelial cells are progenitors of cardiac pericytes and vascular smooth muscle cells. Nat Commun. 2016;7:12422 pubmed publisher..Our findings identify a novel and unexpected population of progenitors for coronary mural cells with potential relevance for heart function and disease conditions. ..
- Triplett T, Cardenas K, Lancaster J, Hu Z, Selden H, Jasso G, et al. Endogenous dendritic cells from the tumor microenvironment support T-ALL growth via IGF1R activation. Proc Natl Acad Sci U S A. 2016;113:E1016-25 pubmed publisher..Collectively, these studies provide the first evidence that endogenous tumor-associated DCs supply signals driving T-ALL growth, and implicate tumor-associated DCs and their mitogenic signals as auspicious therapeutic targets. ..
- Kajita M, Ikeda W, Tamaru Y, Takai Y. Regulation of platelet-derived growth factor-induced Ras signaling by poliovirus receptor Necl-5 and negative growth regulator Sprouty2. Genes Cells. 2007;12:345-57 pubmed..Thus, Necl-5 and Sprouty2 cooperatively regulate PDGF-induced Ras signaling. The roles of Necl-5 and Sprouty2 in contact inhibition for cell proliferation are also discussed. ..
- Gordon J, Martyanov V, Magro C, Wildman H, Wood T, Huang W, et al. Nilotinib (Tasigna™) in the treatment of early diffuse systemic sclerosis: an open-label, pilot clinical trial. Arthritis Res Ther. 2015;17:213 pubmed publisher..The findings of this pilot study warrant more conclusive evaluation. Clinicaltrials.gov NCT01166139 , July 1, 2010. ..
- Xiao Q, Zeng L, Zhang Z, Hu Y, Xu Q. Stem cell-derived Sca-1+ progenitors differentiate into smooth muscle cells, which is mediated by collagen IV-integrin alpha1/beta1/alphav and PDGF receptor pathways. Am J Physiol Cell Physiol. 2007;292:C342-52 pubmed
- Virakul S, Heutz J, Dalm V, Peeters R, Paridaens D, van den Bosch W, et al. Basic FGF and PDGF-BB synergistically stimulate hyaluronan and IL-6 production by orbital fibroblasts. Mol Cell Endocrinol. 2016;433:94-104 pubmed publisher..Multi-target therapy directed at the bFGF and PDGF pathways may potentially be of interest for the treatment of GO. ..
- Iwamoto R, Kataoka T, Furuhata A, Ono K, Hirota S, Kawada K, et al. Perivascular epithelioid cell tumor of the descending colon mimicking a gastrointestinal stromal tumor: a case report. World J Surg Oncol. 2016;14:285 pubmed..A final diagnosis of PEComa was made. PEComa should be included in the differential diagnosis of PDGFR?-positive spindle cell tumors in the wall of the gastrointestinal tract. ..
- Tachibana M, Ago T, Wakisaka Y, Kuroda J, Shijo M, Yoshikawa Y, et al. Early Reperfusion After Brain Ischemia Has Beneficial Effects Beyond Rescuing Neurons. Stroke. 2017;48:2222-2230 pubmed publisher..These effects might be associated with efficient peri-infarct reorganization and functional recovery. ..
- Hamadeh H, Todd M, Healy L, Meyer J, Kwok A, Higgins M, et al. Application of genomics for identification of systemic toxicity triggers associated with VEGF-R inhibitors. Chem Res Toxicol. 2010;23:1025-33 pubmed publisher..Finally, we illustrate that in vivo gene expression profiles can serve as a complementary assessor of this activity and simultaneously help provide an assessment of on or off-target biological activity. ..
- Wang C, Yao X, Chen H, Lai J, Guo X, Su H, et al. Novel mutations of PDGFRB cause primary familial brain calcification in Chinese families. J Hum Genet. 2017;62:697-701 pubmed publisher..The prevalence of PDGFRB mutations in Chinese PFBC patients seems to be quite low, indicating that PDGFRB is not a major causative gene of PFBC in Chinese population. ..
- Cabral B, da Silva A, de Ávila R, Cortez A, Luzin R, Lião L, et al. A novel chalcone derivative, LQFM064, induces breast cancer cells death via p53, p21, KIT and PDGFRA. Eur J Pharm Sci. 2017;107:1-15 pubmed publisher..In conclusion, LQFM064 (4) was capable of inducing breast cancer cells death via different cytotoxic pathways. Thus, it is a promising alternative for the treatment of neoplasias, especially in terms of the drug resistance development. ..
- Bando Y, Sakashita H, Taira F, Miyake G, Ogasawara Y, Sakiyama K, et al. Origin and development of septoclasts in endochondral ossification of mice. Histochem Cell Biol. 2018;149:645-654 pubmed publisher..Our results suggest that septoclasts are originated from pericytes and involved in the blood vessel invasion during formation of the primary ossification center. ..
- Bahm I, Barriga E, Frolov A, Theveneau E, Frankel P, Mayor R. PDGF controls contact inhibition of locomotion by regulating N-cadherin during neural crest migration. Development. 2017;144:2456-2468 pubmed publisher..Finally, we show that once NC cells have undergone EMT, the same PDGF-A/PDGFR? works as an NC chemoattractant, guiding their directional migration. ..
- Kassouf W, Dinney C, Brown G, McConkey D, Diehl A, Bar Eli M, et al. Uncoupling between epidermal growth factor receptor and downstream signals defines resistance to the antiproliferative effect of Gefitinib in bladder cancer cells. Cancer Res. 2005;65:10524-35 pubmed
- Mizukami Y, Sugawara K, Kira Y, Tsuruta D. Sorafenib stimulates human skin type mast cell degranulation and maturation. J Dermatol Sci. 2017;88:308-319 pubmed publisher..This activation appears to be related to PI3K signaling and SCF production, which could be a new targets for treating sorafenib-induced adverse reactions. ..
- Roskoski R. The role of small molecule platelet-derived growth factor receptor (PDGFR) inhibitors in the treatment of neoplastic disorders. Pharmacol Res. 2018;129:65-83 pubmed publisher..Although type II inhibitors may be more selective, most - if not all - inhibit more than one target protein kinase and the differences are a matter of degree only. ..
- Ferraresi V, Nuzzo C, Zoccali C, Marandino F, Vidiri A, Salducca N, et al. Chordoma: clinical characteristics, management and prognosis of a case series of 25 patients. BMC Cancer. 2010;10:22 pubmed publisher..Adequate surgery still remains the only curative treatment of chordoma. Interesting clinical data on advanced disease with molecularly targeted therapies were reported...
- Borkham Kamphorst E, Meurer S, Gressner A, Weiskirchen R. Disruption of intermolecular disulfide bonds in PDGF-BB dimers by N-acetyl-L-cysteine does not prevent PDGF signaling in cultured hepatic stellate cells. Biochem Biophys Res Commun. 2005;338:1711-8 pubmed..Therefore, we conclude that the PDGF monomer is still active. The described antifibrotic effects are therefore mainly attributable to the structural impairment of TGF-beta signaling components reported previously. ..
- Juratli T, Geiger K, Weigel P, von der Hagen M, Daubner D, Pinzer T, et al. A five year-old child with clear cell petro-clival meningioma: case report with clinical and histopathological long-term follow-up. Childs Nerv Syst. 2015;31:2193-8 pubmed publisher..Further evaluation of these growth factors in clear cell meningioma is required to establish the optimal treatment of these aggressive tumors. ..
- Kinoshita K, Nakagawa K, Hamada J, Hida Y, Tada M, Kondo S, et al. Imatinib mesylate inhibits the proliferation-stimulating effect of human lung cancer-associated stromal fibroblasts on lung cancer cells. Int J Oncol. 2010;37:869-77 pubmed..Our results suggest that imatinib has antitumor activity which is exerted by reducing the proliferation-stimulating effect of CAFs on lung cancer cells, as well as inhibiting the proliferation of CAFs, by way of blocking PDGF signaling. ..
- Hilberg F, Roth G, Krssak M, Kautschitsch S, Sommergruber W, Tontsch Grunt U, et al. BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008;68:4774-82 pubmed publisher..These distinctive pharmacokinetic and pharmacodynamic properties may help explain clinical observations with BIBF 1120, currently entering phase III clinical development. ..
- Artemenko Y, Gagnon A, Sorisky A. Catalytically inactive SHIP2 inhibits proliferation by attenuating PDGF signaling in 3T3-L1 preadipocytes. J Cell Physiol. 2009;218:228-36 pubmed publisher..Overall, our findings indicate that SHIP2 PDR/AAA reduces preadipocyte proliferation by attenuating PDGFR signaling. ..
- Cha B, Shi W, Yonezawa T, Teruya T, Nagai K, Woo J. An inhibitory effect of chrysoeriol on platelet-derived growth factor (PDGF)-induced proliferation and PDGF receptor signaling in human aortic smooth muscle cells. J Pharmacol Sci. 2009;110:105-10 pubmed..These findings suggest that in addition to its antioxidant and anti-inflammatory activities, chrysoeriol may be used for the prevention and treatment of vascular diseases and during restenosis after coronary angioplasty. ..
- Chen C, Hung C, Lee S, Lo H, Wu P, Wu W. Lycopene binding compromised PDGF-AA/-AB signaling and migration in smooth muscle cells and fibroblasts: prediction of the possible lycopene binding site within PDGF. Naunyn Schmiedebergs Arch Pharmacol. 2010;381:401-14 pubmed publisher..The results, together with our previous findings, suggest lycopene special affinity/effect for PDGF family and its possible application in prevention in vascular diseases and malignancy. ..
- Roth G, Heckel A, Colbatzky F, Handschuh S, Kley J, Lehmann Lintz T, et al. Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). J Med Chem. 2009;52:4466-80 pubmed publisher..The triple angiokinase inhibitor 3 is currently in phase III clinical trials for the treatment of nonsmall cell lung cancer. ..
- Chetty R, Vajpeyi R. Vasculopathic changes, a somatostatin-producing neuroendocrine carcinoma and a jejunal gastrointestinal stromal tumor in a patient with type 1 neurofibromatosis. Endocr Pathol. 2009;20:177-81 pubmed publisher..These abnormal vessels were within and close to the somatostatinoma only and were not found away from the tumor. It is thought that the vasculopathy is related to NF-1 with abnormal neurofibromin possibly playing a role...
- Carapancea M, Alexandru O, Fetea A, Dragutescu L, Castro J, Georgescu A, et al. Growth factor receptors signaling in glioblastoma cells: therapeutic implications. J Neurooncol. 2009;92:137-47 pubmed publisher..Our results showed that GB cells are in general resistant to treatment and illustrate the difficulties in predicting the treatment response in malignant gliomas. ..
- Pestana I, Vazquez Padron R, Aitouche A, Pham S. Nicotinic and PDGF-receptor function are essential for nicotine-stimulated mitogenesis in human vascular smooth muscle cells. J Cell Biochem. 2005;96:986-95 pubmed..PDGF-BB/PDGF-R interaction is vital in nicotine's mitogenic actions on human aortic smooth muscle cells. ..
- Wilhelm S, Adnane L, Newell P, Villanueva A, Llovet J, Lynch M. Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling. Mol Cancer Ther. 2008;7:3129-40 pubmed publisher..In particular, preclinical evidence that supports the different mechanisms of action of sorafenib is discussed. ..
- Ongkeko W, Altuna X, Weisman R, Wang Rodriguez J. Expression of protein tyrosine kinases in head and neck squamous cell carcinomas. Am J Clin Pathol. 2005;124:71-6 pubmed..None of the kinase expressions correlated with disease-free survival. The expression of the kinases raises the possibility of treatment of HNSCC by tyrosine and serine-threonine kinase inhibitors...
- Thorarinsdottir H, Santi M, McCarter R, Rushing E, Cornelison R, Jales A, et al. Protein expression of platelet-derived growth factor receptor correlates with malignant histology and PTEN with survival in childhood gliomas. Clin Cancer Res. 2008;14:3386-94 pubmed publisher..Deficient PTEN expression is associated with worse overall survival in HGG. ..
- Arifi S, El Sayadi H, Dufresne A, Ray Coquard I, Fayette J, Meeus P, et al. [Imatinib and solid tumours]. Bull Cancer. 2008;95:99-106 pubmed publisher..We review the current data regarding the activity of imatinib in solid tumors, including GIST. ..
- Gonzalo T, Beljaars L, van de Bovenkamp M, Temming K, van Loenen A, Reker Smit C, et al. Local inhibition of liver fibrosis by specific delivery of a platelet-derived growth factor kinase inhibitor to hepatic stellate cells. J Pharmacol Exp Ther. 2007;321:856-65 pubmed..We therefore conclude that delivery of a PDGF-kinase inhibitor to HSC is a promising technology to attenuate liver fibrogenesis. ..
- Tung W, Sun C, Hsieh H, Wang S, Horng J, Yang C. EV71 induces VCAM-1 expression via PDGF receptor, PI3-K/Akt, p38 MAPK, JNK and NF-kappaB in vascular smooth muscle cells. Cell Signal. 2007;19:2127-37 pubmed..These findings suggest that in VSMCs, EV71-induced VCAM-1 expression was mediated through activation of PDGFR, PI3-K/Akt, p38 MAPK, JNK, and NF-kappaB pathways. ..
- Hlushchuk R, Baum O, Gruber G, Wood J, Djonov V. The synergistic action of a VEGF-receptor tyrosine-kinase inhibitor and a sensitizing PDGF-receptor blocker depends upon the stage of vascular maturation. Microcirculation. 2007;14:813-25 pubmed
- Zhang Z, Meier K. New assignments for multitasking signal transduction inhibitors. Mol Pharmacol. 2006;69:1510-2 pubmed
- Kurup S, Abramsson A, Li J, Lindahl U, Kjellen L, Betsholtz C, et al. Heparan sulphate requirement in platelet-derived growth factor B-mediated pericyte recruitment. Biochem Soc Trans. 2006;34:454-5 pubmed..The present paper summarizes our studies on the importance of HS structure in this regulatory process. ..
- Row P, Clague M, Urbé S. Growth factors induce differential phosphorylation profiles of the Hrs-STAM complex: a common node in signalling networks with signal-specific properties. Biochem J. 2005;389:629-36 pubmed
- DeAngelo D, Stone R, Heaney M, Nimer S, Paquette R, Klisovic R, et al. Phase 1 clinical results with tandutinib (MLN518), a novel FLT3 antagonist, in patients with acute myelogenous leukemia or high-risk myelodysplastic syndrome: safety, pharmacokinetics, and pharmacodynamics. Blood. 2006;108:3674-81 pubmed..Tandutinib at the MTD (525 mg twice daily) should be evaluated more extensively in patients with AML with FLT3-ITD mutations to better define its antileukemic activity. ..
- Strachan R, Allen J, Sheffler D, Roth B. p90 Ribosomal S6 kinase 2, a novel GPCR kinase, is required for growth factor-mediated attenuation of GPCR signaling. Biochemistry. 2010;49:2657-71 pubmed publisher..g., neuropsychiatric and neurodevelopmental disorders). ..
- Lewis N, Lewis L, Eder J, Reddy N, Guo F, Pierce K, et al. Phase I study of the safety, tolerability, and pharmacokinetics of oral CP-868,596, a highly specific platelet-derived growth factor receptor tyrosine kinase inhibitor in patients with advanced cancers. J Clin Oncol. 2009;27:5262-9 pubmed publisher..The recommended dosage of 100 mg twice daily with food was well tolerated. Additional development as a single agent in selected populations or in combination with chemotherapy in broader populations is warranted. ..
- Hollborn M, Petto C, Steffen A, Trettner S, Bendig A, Wiedemann P, et al. Effects of thrombin on RPE cells are mediated by transactivation of growth factor receptors. Invest Ophthalmol Vis Sci. 2009;50:4452-9 pubmed publisher..Thrombin stimulates the secretion of VEGF-A, the expression of FLT1, and the chemotaxis of RPE cells via transactivation of TGF-beta and PDGF receptors, respectively. ..
- Venkatesan B, Ghosh Choudhury N, Das F, Mahimainathan L, Kamat A, Kasinath B, et al. Resveratrol inhibits PDGF receptor mitogenic signaling in mesangial cells: role of PTP1B. FASEB J. 2008;22:3469-82 pubmed publisher..PTP1B significantly inhibited PDGF-induced DNA synthesis without inducing apoptosis. These results for the first time provide evidence that the stilbene resveratrol targets PTP1B to inhibit PDGFR mitogenic signaling. ..
- Kumamoto H, Ooya K. Immunohistochemical detection of insulin-like growth factors, platelet-derived growth factor, and their receptors in ameloblastic tumors. J Oral Pathol Med. 2007;36:198-206 pubmed..Altered expression of the ligands and receptors in ameloblastic tumors may be involved in oncogenesis, malignant potential, and tumor cell differentiation. ..
- Zhou H, Wang D, Baldini L, Ennis E, Jain R, Carie A, et al. Structure-activity studies on a library of potent calixarene-based PDGF antagonists that inhibit PDGF-stimulated PDGFR tyrosine phosphorylation. Org Biomol Chem. 2006;4:2376-86 pubmed..The effect of lower-rim alkylation, linker and number of interacting head groups on the calixarene scaffold on PDGF affinity and cellular activity has been investigated. ..
- McTigue D, Tripathi R, Wei P. NG2 colocalizes with axons and is expressed by a mixed cell population in spinal cord lesions. J Neuropathol Exp Neurol. 2006;65:406-20 pubmed..Thus, spinal contusion produces an NG2-rich environment into which axons grow and in which the source of NG2 appears considerably different from that in surrounding spared tissue. ..
- Borner M. [Molecular targets in colon cancer]. Ther Umsch. 2006;63:243-8 pubmed..In this article, we will review molecular targets, which are under active clinical investigation in colon cancer. ..
- Cesta M, Ryman Rasmussen J, Wallace D, Masinde T, Hurlburt G, Taylor A, et al. Bacterial lipopolysaccharide enhances PDGF signaling and pulmonary fibrosis in rats exposed to carbon nanotubes. Am J Respir Cell Mol Biol. 2010;43:142-51 pubmed publisher..Our findings also suggest that individuals with pre-existing pulmonary inflammation are at greater risk for the potential adverse effects of MWCNT. ..
- Ignatiuk A, Quickfall J, Hawrysh A, Chamberlain M, Anderson D. The smaller isoforms of ankyrin 3 bind to the p85 subunit of phosphatidylinositol 3'-kinase and enhance platelet-derived growth factor receptor down-regulation. J Biol Chem. 2006;281:5956-64 pubmed..These results suggest that Ank3 plays an important role in lysosomal-mediated receptor down-regulation, likely through a p85-Ank3 interaction. ..
- Monine M, Haugh J. Cell population-based model of dermal wound invasion with heterogeneous intracellular signaling properties. Cell Adh Migr. 2008;2:137-46 pubmed
- Cui J, Lei H, Samad A, Basavanthappa S, Maberley D, Matsubara J, et al. PDGF receptors are activated in human epiretinal membranes. Exp Eye Res. 2009;88:438-44 pubmed publisher..These findings identify PDGF-A, -AB and C as the best therapeutic targets within the PDGF family. ..
- Dy G, Adjei A. Systemic cancer therapy: evolution over the last 60 years. Cancer. 2008;113:1857-87 pubmed publisher..The key approaches and evidence pertinent to the clinical development of these novel agents are presented in this review. ..
- Ogawa J, Kanegane H, Tsuneyama K, Kanezaki R, Futatani T, Nomura K, et al. Platelet-derived growth factor may be associated with fibrosis in a Down syndrome patient with transient myeloproliferative disorder. Eur J Haematol. 2008;81:58-64 pubmed publisher..The finding indicates that the PDGF pathway may play an important role in the fibrosis of several organs in patients with TMD. ..