Discovery of imidazopyridine-pyrazoline-hybrid structure as SHP-1 agonist that suppresses phospho-STAT3 signaling in human breast cancer cells
Signal transducer and activator of transcription 3 (STAT3) promotes breast cancer malignancy and controls key processes including proliferation, differentiation, and survival in breast cancer cells. Although many methods for treating breast cancer have been improved, there is still a need to discove...
Ausführliche Beschreibung
Autor*in: |
Yang, Min Hee [verfasserIn] Sethi, Gautam [verfasserIn] Ravish, Akshay [verfasserIn] Mohan, Arun Kumar [verfasserIn] Pandey, Vijay [verfasserIn] Lobie, Peter E. [verfasserIn] Basappa, Shreeja [verfasserIn] Basappa, Basappa [verfasserIn] Ahn, Kwang Seok [verfasserIn] |
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Format: |
E-Artikel |
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Sprache: |
Englisch |
Erschienen: |
2023 |
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Schlagwörter: |
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Übergeordnetes Werk: |
Enthalten in: Chemico-biological interactions - Amsterdam [u.a.] : Elsevier Science, 1969, 386 |
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Übergeordnetes Werk: |
volume:386 |
DOI / URN: |
10.1016/j.cbi.2023.110780 |
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Katalog-ID: |
ELV065595084 |
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520 | |a Signal transducer and activator of transcription 3 (STAT3) promotes breast cancer malignancy and controls key processes including proliferation, differentiation, and survival in breast cancer cells. Although many methods for treating breast cancer have been improved, there is still a need to discover and develop new methods for breast cancer treatment. Therefore, we synthesized a new compound 2-(4-(2,3-dichlorophenyl)piperazin-1-yl)-1-(3-(2,6-dimethylimidazo[1,2-a]pyridin-3-yl)-5-(3-nitrophenyl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone (DIP). We aimed to evaluate the anti-cancer effect of DIP in breast cancer cells and clarify its mode of action. We noted that DIP abrogated STAT3 activation and STAT3 upstream kinases janus-activated kinase (JAK) and Src kinases. In addition, DIP promoted the levels of SHP-1 protein and acts as SHP-1 agonist. Further, silencing of SHP-1 gene reversed the DIP-induced attenuation of STAT3 activation and apoptosis. DIP also induced apoptosis through modulating PARP cleavage and oncogenic proteins. Moreover, DIP also significantly enhanced the apoptotic effects of docetaxel through the suppression of STAT3 activation in breast cancer cells. | ||
650 | 4 | |a DIP | |
650 | 4 | |a STAT3 | |
650 | 4 | |a Apoptosis | |
650 | 4 | |a Breast cancer | |
650 | 4 | |a Docetaxel | |
700 | 1 | |a Sethi, Gautam |e verfasserin |4 aut | |
700 | 1 | |a Ravish, Akshay |e verfasserin |0 (orcid)0000-0001-6068-9290 |4 aut | |
700 | 1 | |a Mohan, Arun Kumar |e verfasserin |0 (orcid)0009-0009-2058-8386 |4 aut | |
700 | 1 | |a Pandey, Vijay |e verfasserin |0 (orcid)0000-0001-8704-0694 |4 aut | |
700 | 1 | |a Lobie, Peter E. |e verfasserin |4 aut | |
700 | 1 | |a Basappa, Shreeja |e verfasserin |4 aut | |
700 | 1 | |a Basappa, Basappa |e verfasserin |4 aut | |
700 | 1 | |a Ahn, Kwang Seok |e verfasserin |0 (orcid)0000-0002-2882-0612 |4 aut | |
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10.1016/j.cbi.2023.110780 doi (DE-627)ELV065595084 (ELSEVIER)S0009-2797(23)00447-7 DE-627 ger DE-627 rda eng 570 540 VZ BIODIV DE-30 fid PHARM DE-84 fid 35.70 bkl 44.39 bkl Yang, Min Hee verfasserin aut Discovery of imidazopyridine-pyrazoline-hybrid structure as SHP-1 agonist that suppresses phospho-STAT3 signaling in human breast cancer cells 2023 nicht spezifiziert zzz rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Signal transducer and activator of transcription 3 (STAT3) promotes breast cancer malignancy and controls key processes including proliferation, differentiation, and survival in breast cancer cells. Although many methods for treating breast cancer have been improved, there is still a need to discover and develop new methods for breast cancer treatment. Therefore, we synthesized a new compound 2-(4-(2,3-dichlorophenyl)piperazin-1-yl)-1-(3-(2,6-dimethylimidazo[1,2-a]pyridin-3-yl)-5-(3-nitrophenyl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone (DIP). We aimed to evaluate the anti-cancer effect of DIP in breast cancer cells and clarify its mode of action. We noted that DIP abrogated STAT3 activation and STAT3 upstream kinases janus-activated kinase (JAK) and Src kinases. In addition, DIP promoted the levels of SHP-1 protein and acts as SHP-1 agonist. Further, silencing of SHP-1 gene reversed the DIP-induced attenuation of STAT3 activation and apoptosis. DIP also induced apoptosis through modulating PARP cleavage and oncogenic proteins. Moreover, DIP also significantly enhanced the apoptotic effects of docetaxel through the suppression of STAT3 activation in breast cancer cells. DIP STAT3 Apoptosis Breast cancer Docetaxel Sethi, Gautam verfasserin aut Ravish, Akshay verfasserin (orcid)0000-0001-6068-9290 aut Mohan, Arun Kumar verfasserin (orcid)0009-0009-2058-8386 aut Pandey, Vijay verfasserin (orcid)0000-0001-8704-0694 aut Lobie, Peter E. verfasserin aut Basappa, Shreeja verfasserin aut Basappa, Basappa verfasserin aut Ahn, Kwang Seok verfasserin (orcid)0000-0002-2882-0612 aut Enthalten in Chemico-biological interactions Amsterdam [u.a.] : Elsevier Science, 1969 386 Online-Ressource (DE-627)306353911 (DE-600)1496834-4 (DE-576)255530633 1872-7786 nnns volume:386 GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-BIODIV FID-PHARM SSG-OLC-PHA SSG-OPC-PHA GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_370 GBV_ILN_602 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2034 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2088 GBV_ILN_2106 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2470 GBV_ILN_2507 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4242 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 35.70 Biochemie: Allgemeines VZ 44.39 Toxikologie VZ AR 386 |
spelling |
10.1016/j.cbi.2023.110780 doi (DE-627)ELV065595084 (ELSEVIER)S0009-2797(23)00447-7 DE-627 ger DE-627 rda eng 570 540 VZ BIODIV DE-30 fid PHARM DE-84 fid 35.70 bkl 44.39 bkl Yang, Min Hee verfasserin aut Discovery of imidazopyridine-pyrazoline-hybrid structure as SHP-1 agonist that suppresses phospho-STAT3 signaling in human breast cancer cells 2023 nicht spezifiziert zzz rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Signal transducer and activator of transcription 3 (STAT3) promotes breast cancer malignancy and controls key processes including proliferation, differentiation, and survival in breast cancer cells. Although many methods for treating breast cancer have been improved, there is still a need to discover and develop new methods for breast cancer treatment. Therefore, we synthesized a new compound 2-(4-(2,3-dichlorophenyl)piperazin-1-yl)-1-(3-(2,6-dimethylimidazo[1,2-a]pyridin-3-yl)-5-(3-nitrophenyl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone (DIP). We aimed to evaluate the anti-cancer effect of DIP in breast cancer cells and clarify its mode of action. We noted that DIP abrogated STAT3 activation and STAT3 upstream kinases janus-activated kinase (JAK) and Src kinases. In addition, DIP promoted the levels of SHP-1 protein and acts as SHP-1 agonist. Further, silencing of SHP-1 gene reversed the DIP-induced attenuation of STAT3 activation and apoptosis. DIP also induced apoptosis through modulating PARP cleavage and oncogenic proteins. Moreover, DIP also significantly enhanced the apoptotic effects of docetaxel through the suppression of STAT3 activation in breast cancer cells. DIP STAT3 Apoptosis Breast cancer Docetaxel Sethi, Gautam verfasserin aut Ravish, Akshay verfasserin (orcid)0000-0001-6068-9290 aut Mohan, Arun Kumar verfasserin (orcid)0009-0009-2058-8386 aut Pandey, Vijay verfasserin (orcid)0000-0001-8704-0694 aut Lobie, Peter E. verfasserin aut Basappa, Shreeja verfasserin aut Basappa, Basappa verfasserin aut Ahn, Kwang Seok verfasserin (orcid)0000-0002-2882-0612 aut Enthalten in Chemico-biological interactions Amsterdam [u.a.] : Elsevier Science, 1969 386 Online-Ressource (DE-627)306353911 (DE-600)1496834-4 (DE-576)255530633 1872-7786 nnns volume:386 GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-BIODIV FID-PHARM SSG-OLC-PHA SSG-OPC-PHA GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_370 GBV_ILN_602 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2034 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2088 GBV_ILN_2106 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2470 GBV_ILN_2507 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4242 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 35.70 Biochemie: Allgemeines VZ 44.39 Toxikologie VZ AR 386 |
allfields_unstemmed |
10.1016/j.cbi.2023.110780 doi (DE-627)ELV065595084 (ELSEVIER)S0009-2797(23)00447-7 DE-627 ger DE-627 rda eng 570 540 VZ BIODIV DE-30 fid PHARM DE-84 fid 35.70 bkl 44.39 bkl Yang, Min Hee verfasserin aut Discovery of imidazopyridine-pyrazoline-hybrid structure as SHP-1 agonist that suppresses phospho-STAT3 signaling in human breast cancer cells 2023 nicht spezifiziert zzz rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Signal transducer and activator of transcription 3 (STAT3) promotes breast cancer malignancy and controls key processes including proliferation, differentiation, and survival in breast cancer cells. Although many methods for treating breast cancer have been improved, there is still a need to discover and develop new methods for breast cancer treatment. Therefore, we synthesized a new compound 2-(4-(2,3-dichlorophenyl)piperazin-1-yl)-1-(3-(2,6-dimethylimidazo[1,2-a]pyridin-3-yl)-5-(3-nitrophenyl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone (DIP). We aimed to evaluate the anti-cancer effect of DIP in breast cancer cells and clarify its mode of action. We noted that DIP abrogated STAT3 activation and STAT3 upstream kinases janus-activated kinase (JAK) and Src kinases. In addition, DIP promoted the levels of SHP-1 protein and acts as SHP-1 agonist. Further, silencing of SHP-1 gene reversed the DIP-induced attenuation of STAT3 activation and apoptosis. DIP also induced apoptosis through modulating PARP cleavage and oncogenic proteins. Moreover, DIP also significantly enhanced the apoptotic effects of docetaxel through the suppression of STAT3 activation in breast cancer cells. DIP STAT3 Apoptosis Breast cancer Docetaxel Sethi, Gautam verfasserin aut Ravish, Akshay verfasserin (orcid)0000-0001-6068-9290 aut Mohan, Arun Kumar verfasserin (orcid)0009-0009-2058-8386 aut Pandey, Vijay verfasserin (orcid)0000-0001-8704-0694 aut Lobie, Peter E. verfasserin aut Basappa, Shreeja verfasserin aut Basappa, Basappa verfasserin aut Ahn, Kwang Seok verfasserin (orcid)0000-0002-2882-0612 aut Enthalten in Chemico-biological interactions Amsterdam [u.a.] : Elsevier Science, 1969 386 Online-Ressource (DE-627)306353911 (DE-600)1496834-4 (DE-576)255530633 1872-7786 nnns volume:386 GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-BIODIV FID-PHARM SSG-OLC-PHA SSG-OPC-PHA GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_370 GBV_ILN_602 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2034 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2088 GBV_ILN_2106 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2470 GBV_ILN_2507 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4242 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 35.70 Biochemie: Allgemeines VZ 44.39 Toxikologie VZ AR 386 |
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10.1016/j.cbi.2023.110780 doi (DE-627)ELV065595084 (ELSEVIER)S0009-2797(23)00447-7 DE-627 ger DE-627 rda eng 570 540 VZ BIODIV DE-30 fid PHARM DE-84 fid 35.70 bkl 44.39 bkl Yang, Min Hee verfasserin aut Discovery of imidazopyridine-pyrazoline-hybrid structure as SHP-1 agonist that suppresses phospho-STAT3 signaling in human breast cancer cells 2023 nicht spezifiziert zzz rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Signal transducer and activator of transcription 3 (STAT3) promotes breast cancer malignancy and controls key processes including proliferation, differentiation, and survival in breast cancer cells. Although many methods for treating breast cancer have been improved, there is still a need to discover and develop new methods for breast cancer treatment. Therefore, we synthesized a new compound 2-(4-(2,3-dichlorophenyl)piperazin-1-yl)-1-(3-(2,6-dimethylimidazo[1,2-a]pyridin-3-yl)-5-(3-nitrophenyl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone (DIP). We aimed to evaluate the anti-cancer effect of DIP in breast cancer cells and clarify its mode of action. We noted that DIP abrogated STAT3 activation and STAT3 upstream kinases janus-activated kinase (JAK) and Src kinases. In addition, DIP promoted the levels of SHP-1 protein and acts as SHP-1 agonist. Further, silencing of SHP-1 gene reversed the DIP-induced attenuation of STAT3 activation and apoptosis. DIP also induced apoptosis through modulating PARP cleavage and oncogenic proteins. Moreover, DIP also significantly enhanced the apoptotic effects of docetaxel through the suppression of STAT3 activation in breast cancer cells. DIP STAT3 Apoptosis Breast cancer Docetaxel Sethi, Gautam verfasserin aut Ravish, Akshay verfasserin (orcid)0000-0001-6068-9290 aut Mohan, Arun Kumar verfasserin (orcid)0009-0009-2058-8386 aut Pandey, Vijay verfasserin (orcid)0000-0001-8704-0694 aut Lobie, Peter E. verfasserin aut Basappa, Shreeja verfasserin aut Basappa, Basappa verfasserin aut Ahn, Kwang Seok verfasserin (orcid)0000-0002-2882-0612 aut Enthalten in Chemico-biological interactions Amsterdam [u.a.] : Elsevier Science, 1969 386 Online-Ressource (DE-627)306353911 (DE-600)1496834-4 (DE-576)255530633 1872-7786 nnns volume:386 GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-BIODIV FID-PHARM SSG-OLC-PHA SSG-OPC-PHA GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_370 GBV_ILN_602 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2034 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2088 GBV_ILN_2106 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2470 GBV_ILN_2507 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4242 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 35.70 Biochemie: Allgemeines VZ 44.39 Toxikologie VZ AR 386 |
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10.1016/j.cbi.2023.110780 doi (DE-627)ELV065595084 (ELSEVIER)S0009-2797(23)00447-7 DE-627 ger DE-627 rda eng 570 540 VZ BIODIV DE-30 fid PHARM DE-84 fid 35.70 bkl 44.39 bkl Yang, Min Hee verfasserin aut Discovery of imidazopyridine-pyrazoline-hybrid structure as SHP-1 agonist that suppresses phospho-STAT3 signaling in human breast cancer cells 2023 nicht spezifiziert zzz rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Signal transducer and activator of transcription 3 (STAT3) promotes breast cancer malignancy and controls key processes including proliferation, differentiation, and survival in breast cancer cells. Although many methods for treating breast cancer have been improved, there is still a need to discover and develop new methods for breast cancer treatment. Therefore, we synthesized a new compound 2-(4-(2,3-dichlorophenyl)piperazin-1-yl)-1-(3-(2,6-dimethylimidazo[1,2-a]pyridin-3-yl)-5-(3-nitrophenyl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone (DIP). We aimed to evaluate the anti-cancer effect of DIP in breast cancer cells and clarify its mode of action. We noted that DIP abrogated STAT3 activation and STAT3 upstream kinases janus-activated kinase (JAK) and Src kinases. In addition, DIP promoted the levels of SHP-1 protein and acts as SHP-1 agonist. Further, silencing of SHP-1 gene reversed the DIP-induced attenuation of STAT3 activation and apoptosis. DIP also induced apoptosis through modulating PARP cleavage and oncogenic proteins. Moreover, DIP also significantly enhanced the apoptotic effects of docetaxel through the suppression of STAT3 activation in breast cancer cells. DIP STAT3 Apoptosis Breast cancer Docetaxel Sethi, Gautam verfasserin aut Ravish, Akshay verfasserin (orcid)0000-0001-6068-9290 aut Mohan, Arun Kumar verfasserin (orcid)0009-0009-2058-8386 aut Pandey, Vijay verfasserin (orcid)0000-0001-8704-0694 aut Lobie, Peter E. verfasserin aut Basappa, Shreeja verfasserin aut Basappa, Basappa verfasserin aut Ahn, Kwang Seok verfasserin (orcid)0000-0002-2882-0612 aut Enthalten in Chemico-biological interactions Amsterdam [u.a.] : Elsevier Science, 1969 386 Online-Ressource (DE-627)306353911 (DE-600)1496834-4 (DE-576)255530633 1872-7786 nnns volume:386 GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-BIODIV FID-PHARM SSG-OLC-PHA SSG-OPC-PHA GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_187 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_370 GBV_ILN_602 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2034 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2088 GBV_ILN_2106 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2470 GBV_ILN_2507 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4242 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 35.70 Biochemie: Allgemeines VZ 44.39 Toxikologie VZ AR 386 |
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DIP STAT3 Apoptosis Breast cancer Docetaxel |
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Yang, Min Hee @@aut@@ Sethi, Gautam @@aut@@ Ravish, Akshay @@aut@@ Mohan, Arun Kumar @@aut@@ Pandey, Vijay @@aut@@ Lobie, Peter E. @@aut@@ Basappa, Shreeja @@aut@@ Basappa, Basappa @@aut@@ Ahn, Kwang Seok @@aut@@ |
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Yang, Min Hee |
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Yang, Min Hee ddc 570 fid BIODIV fid PHARM bkl 35.70 bkl 44.39 misc DIP misc STAT3 misc Apoptosis misc Breast cancer misc Docetaxel Discovery of imidazopyridine-pyrazoline-hybrid structure as SHP-1 agonist that suppresses phospho-STAT3 signaling in human breast cancer cells |
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570 540 VZ BIODIV DE-30 fid PHARM DE-84 fid 35.70 bkl 44.39 bkl Discovery of imidazopyridine-pyrazoline-hybrid structure as SHP-1 agonist that suppresses phospho-STAT3 signaling in human breast cancer cells DIP STAT3 Apoptosis Breast cancer Docetaxel |
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Discovery of imidazopyridine-pyrazoline-hybrid structure as SHP-1 agonist that suppresses phospho-STAT3 signaling in human breast cancer cells |
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Discovery of imidazopyridine-pyrazoline-hybrid structure as SHP-1 agonist that suppresses phospho-STAT3 signaling in human breast cancer cells |
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discovery of imidazopyridine-pyrazoline-hybrid structure as shp-1 agonist that suppresses phospho-stat3 signaling in human breast cancer cells |
title_auth |
Discovery of imidazopyridine-pyrazoline-hybrid structure as SHP-1 agonist that suppresses phospho-STAT3 signaling in human breast cancer cells |
abstract |
Signal transducer and activator of transcription 3 (STAT3) promotes breast cancer malignancy and controls key processes including proliferation, differentiation, and survival in breast cancer cells. Although many methods for treating breast cancer have been improved, there is still a need to discover and develop new methods for breast cancer treatment. Therefore, we synthesized a new compound 2-(4-(2,3-dichlorophenyl)piperazin-1-yl)-1-(3-(2,6-dimethylimidazo[1,2-a]pyridin-3-yl)-5-(3-nitrophenyl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone (DIP). We aimed to evaluate the anti-cancer effect of DIP in breast cancer cells and clarify its mode of action. We noted that DIP abrogated STAT3 activation and STAT3 upstream kinases janus-activated kinase (JAK) and Src kinases. In addition, DIP promoted the levels of SHP-1 protein and acts as SHP-1 agonist. Further, silencing of SHP-1 gene reversed the DIP-induced attenuation of STAT3 activation and apoptosis. DIP also induced apoptosis through modulating PARP cleavage and oncogenic proteins. Moreover, DIP also significantly enhanced the apoptotic effects of docetaxel through the suppression of STAT3 activation in breast cancer cells. |
abstractGer |
Signal transducer and activator of transcription 3 (STAT3) promotes breast cancer malignancy and controls key processes including proliferation, differentiation, and survival in breast cancer cells. Although many methods for treating breast cancer have been improved, there is still a need to discover and develop new methods for breast cancer treatment. Therefore, we synthesized a new compound 2-(4-(2,3-dichlorophenyl)piperazin-1-yl)-1-(3-(2,6-dimethylimidazo[1,2-a]pyridin-3-yl)-5-(3-nitrophenyl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone (DIP). We aimed to evaluate the anti-cancer effect of DIP in breast cancer cells and clarify its mode of action. We noted that DIP abrogated STAT3 activation and STAT3 upstream kinases janus-activated kinase (JAK) and Src kinases. In addition, DIP promoted the levels of SHP-1 protein and acts as SHP-1 agonist. Further, silencing of SHP-1 gene reversed the DIP-induced attenuation of STAT3 activation and apoptosis. DIP also induced apoptosis through modulating PARP cleavage and oncogenic proteins. Moreover, DIP also significantly enhanced the apoptotic effects of docetaxel through the suppression of STAT3 activation in breast cancer cells. |
abstract_unstemmed |
Signal transducer and activator of transcription 3 (STAT3) promotes breast cancer malignancy and controls key processes including proliferation, differentiation, and survival in breast cancer cells. Although many methods for treating breast cancer have been improved, there is still a need to discover and develop new methods for breast cancer treatment. Therefore, we synthesized a new compound 2-(4-(2,3-dichlorophenyl)piperazin-1-yl)-1-(3-(2,6-dimethylimidazo[1,2-a]pyridin-3-yl)-5-(3-nitrophenyl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone (DIP). We aimed to evaluate the anti-cancer effect of DIP in breast cancer cells and clarify its mode of action. We noted that DIP abrogated STAT3 activation and STAT3 upstream kinases janus-activated kinase (JAK) and Src kinases. In addition, DIP promoted the levels of SHP-1 protein and acts as SHP-1 agonist. Further, silencing of SHP-1 gene reversed the DIP-induced attenuation of STAT3 activation and apoptosis. DIP also induced apoptosis through modulating PARP cleavage and oncogenic proteins. Moreover, DIP also significantly enhanced the apoptotic effects of docetaxel through the suppression of STAT3 activation in breast cancer cells. |
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title_short |
Discovery of imidazopyridine-pyrazoline-hybrid structure as SHP-1 agonist that suppresses phospho-STAT3 signaling in human breast cancer cells |
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Although many methods for treating breast cancer have been improved, there is still a need to discover and develop new methods for breast cancer treatment. Therefore, we synthesized a new compound 2-(4-(2,3-dichlorophenyl)piperazin-1-yl)-1-(3-(2,6-dimethylimidazo[1,2-a]pyridin-3-yl)-5-(3-nitrophenyl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone (DIP). We aimed to evaluate the anti-cancer effect of DIP in breast cancer cells and clarify its mode of action. We noted that DIP abrogated STAT3 activation and STAT3 upstream kinases janus-activated kinase (JAK) and Src kinases. In addition, DIP promoted the levels of SHP-1 protein and acts as SHP-1 agonist. Further, silencing of SHP-1 gene reversed the DIP-induced attenuation of STAT3 activation and apoptosis. DIP also induced apoptosis through modulating PARP cleavage and oncogenic proteins. 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