https://nova.newcastle.edu.au/vital/access/manager/Index ${session.getAttribute("locale")} 5 FMS-like tyrosine kinase 3 (FLT3) inhibitors: molecular docking and experimental studies https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:30110 50 values in the cell proliferation assay, CEP701 was the most potent inhibitor; sunitinib and PKC412 were ranked second and third, respectively. Sunitinib was the most selective inhibitor, followed by PKC421 and CEP701. The potency of sunitinib and to a lesser extent CEP701 in inhibition of FLT3 autophosphorylation was lower than the cell proliferation inhibition, indicating that inhibition of FLT3 downstream proteins may contribute to the cellular effects. It was shown in this study that the docking procedure was able to differentiate FLT3 inhibitors from ineffective compounds. Additionally, interaction with the phosphate binding region in the ATP-binding pocket increased potency at the cost of selectivity. These findings can be applied in designing highly effective and selective inhibitors for FLT3 and other related kinases.]]> Wed 15 Dec 2021 16:10:04 AEDT ]]> Evidence for the involvement of PECAM-1 in a receptor mediated signal-transduction pathway regulating capacitation-associated tyrosine phosphorylation in human spermatozoa https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:1527 Wed 11 Apr 2018 16:54:55 AEST ]]> CD151 (CD151 molecule (Raph blood group)) https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:6950 Wed 11 Apr 2018 15:52:55 AEST ]]> The migration and invasion of human prostate cancer cell lines involves CD151 expression https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:10728 0.05). There was greater motility of CD151-transfected vs. control cells, when transferring through migration chambers with or without matrigel-coated membranes (P<0.01, P<0.01). Fewer numbers of mutant-transfected cells were found on the membranes for both migration and invasion studies (P<0.01, P<0.01). CD151 knock-down PC3 cells showed decreased motility (P<0.01), but no change in proliferation (P>0.05). Our data show that CD151 does not change the proliferative properties of prostate cancer cells, but does promote migration and invasion, and suggest that CD151 plays a specific role in promoting prostate cancer cell motility.]]> Wed 11 Apr 2018 14:15:31 AEST ]]> Deletion of Cd151 reduces mammary tumorigenesis in the MMTV/PyMT mouse model https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:16760 −/− PyMT mice compared to Cd151+/+ PyMT littermate controls, this result was only approaching significance (Log-rank test P-value =0.0536). Interestingly, Cd151 deletion resulted in significantly reduced numbers and size of primary tumors but did not appear to affect the number or size of metastases in the MMTV/PyMT mice. Intriguingly, no differences in the expression of markers of cell proliferation, apoptosis and blood vessel density was observed in the primary tumors. Conclusion: The findings from this study provide additional evidence that CD151 acts to enhance tumor formation initiated by a range of oncogenes and strongly support its relevance as a potential therapeutic target to delay breast cancer progression.]]> Wed 11 Apr 2018 10:43:04 AEST ]]> Identification of Tspan9 as a novel platelet tetraspanin and the collagen receptor GPVI as a component of tetraspanin microdomains https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:6935 Wed 11 Apr 2018 09:35:42 AEST ]]> Tetraspanins in cancer https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:18180 Tue 23 Jun 2015 18:36:43 AEST ]]> Characterization of the early molecular changes in the glomeruli of Cd151-/- mice highlights induction of mindin and MMP-10 https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:33471 -/- mice compared to Cd151+/+ controls. This study identified 72 up-regulated and 183 down-regulated genes in FVB/N Cd151-/- compared to Cd151+/+ glomeruli (p<0.05). Further analysis highlighted induction of the matrix metalloprotease MMP-10 and the extracellular matrix protein mindin (encoded by Spon2) in the diseased FVB/N Cd151-/- GBM that did not occur in the C57BL/6 diseased-resistant strain. Interestingly, mindin was also detected in urinary samples of FVB/N Cd151-/- mice, underlining its potential value as a biomarker for glomerular diseases associated with GBM alterations. Gene set enrichment and pathway analysis of the microarray dataset showed enrichment in axon guidance and actin cytoskeleton signalling pathways as well as activation of inflammatory pathways. Given the known function of mindin, its early expression in the diseased GBM could represent a trigger of both further podocyte cytoskeletal changes and inflammation, thereby playing a key role in the mechanisms of disease progression.]]> Tue 03 Sep 2019 18:26:44 AEST ]]> Activation of protein phosphatase 2A in FLT3+ acute myeloid leukemia cells enhances the cytotoxicity of FLT3 tyrosine kinase inhibitors https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:27776 Thu 28 Oct 2021 13:04:26 AEDT ]]> Colocalization of the tetraspanins, CO-029 and CD151, with integrins in human pancreatic adenocarcinoma: Impact on cell motility https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:223 Thu 25 Jul 2013 09:09:37 AEST ]]> miR-518f-5p decreases tetraspanin CD9 protein levels and differentially affects non-tumourigenic prostate and prostate cancer cell migration and adhesion https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:33474 Thu 03 Feb 2022 12:18:02 AEDT ]]> Characterization of mice lacking the tetraspanin superfamily member CD151 https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:1881 Sat 24 Mar 2018 08:31:18 AEDT ]]> Wound healing is defective in mice lacking tetraspanin CD151 https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:1198 Sat 24 Mar 2018 08:28:36 AEDT ]]> Juxtamembrane mutant V560GKit is more sensitive to Imatinib (ST1571) compared with wild-type c-Kit whereas the kinase domain mutant D816VKit is resistant https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:1418 Sat 24 Mar 2018 08:28:14 AEDT ]]> Therapeutic targeting of c-KIT in cancer https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:14589 Sat 24 Mar 2018 08:20:46 AEDT ]]> Essential requirement for PP2A inhibition by the oncogenic receptor c-KIT suggests PP2A reactivation as a strategy to treat c-KIT⁺ cancers https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:11381 Sat 24 Mar 2018 08:11:51 AEDT ]]> Colony stimulating factor-1 receptor as a target for small molecule inhibitors https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:10405 Sat 24 Mar 2018 08:07:46 AEDT ]]> Genetic ablation of the tetraspanin CD151 reduces spontaneous metastatic spread of prostate cancer in the TRAMP model https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:20183 Sat 24 Mar 2018 07:51:43 AEDT ]]> Knockout of the tetraspanin Cd9 in the TRAMP model of de novo prostate cancer increases spontaneous metastases in an organ-specific manner https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:20184 Sat 24 Mar 2018 07:51:43 AEDT ]]> Expression of biologically active human colony stimulating factor-1 in Pichia pastoris https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:20167 Sat 24 Mar 2018 07:51:41 AEDT ]]> The role of the tetraspanin CD151 in primary keratinocyte and fibroblast functions: implications for wound healing https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:5569 Sat 24 Mar 2018 07:49:28 AEDT ]]> Probing the interaction of tetraspanin CD151 with integrin α3β1 using a panel of monoclonal antibodies with distinct reactivities toward the CD151-integrin α3β1 complex https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:5526 Sat 24 Mar 2018 07:46:40 AEDT ]]> Deletion of Cd151 results in a strain-dependent glomerular disease due to severe alterations of the glomerular basement membrane https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:5279 Sat 24 Mar 2018 07:46:27 AEDT ]]> An in vivo tumor model exploiting metabolic response as a biomarker for targeted drug development https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:130 Sat 24 Mar 2018 07:43:12 AEDT ]]> Src family kinases are involved in the differential signaling from two splice forms of c-Kit https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:3455 Sat 24 Mar 2018 07:20:30 AEDT ]]> Tetraspanin CD9 is regulated by MiR-518f-5p and functions in breast cell migration and in vivo tumor growth https://nova.newcastle.edu.au/vital/access/manager/Repository/uon:44184 Mon 10 Oct 2022 10:48:32 AEDT ]]>