The Experts below are selected from a list of 108 Experts worldwide ranked by ideXlab platform
Nicholas J Lawrence - One of the best experts on this subject based on the ideXlab platform.
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abstract 3239 shp2 inhibitor activity of estramustine phosphate and its triterpenoid analogues
Cancer Research, 2011Co-Authors: Latanya M Scott, Liwei Chen, Kenyon G Daniel, Wesley H Brooks, Wayne C Guida, Harshani R Lawrence, Said M Sebti, Murali K Urlam, Nicholas J LawrenceAbstract:Shp2 is a non-receptor protein tyrosine phosphatase (PTP) encoded by the PTPN11 gene. Shp2 mediates proliferative signaling induced by growth factors. Gain-of-function PTPN11 mutations that encode constitutively active Shp2 are leukemic oncogenes. In a continuing effort to identify new Shp2 PTP inhibitors, we screened a small molecule library comprising the National Cancer Institute (NCI) Approved Oncology Drug set and the NIH Clinical Collection. After evaluation of initial hits, estramustine phosphate was verified as a Shp2 PTP inhibitor. A focused structure-activity relationship study indicated that the 17-phosphate group is required for the Shp2 PTP inhibitor activity of estramustine phosphate. A search for estramustine phosphate analogs led to identification of two triperpenoids, Enoxolone and celastrol, having Shp2 PTP inhibitor activity. With the previously reported PTP1B inhibitor trodusquemine, our study reveals steroids and triterpenoids with negatively charged phosphate, carboxylate, or sulfonate groups as novel pharmacophores of selective PTP inhibitors. These findings point to a rich natural source for discovery of lead compounds of novel PTP inhibitors. Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 102nd Annual Meeting of the American Association for Cancer Research; 2011 Apr 2-6; Orlando, FL. Philadelphia (PA): AACR; Cancer Res 2011;71(8 Suppl):Abstract nr 3239. doi:10.1158/1538-7445.AM2011-3239
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shp2 protein tyrosine phosphatase inhibitor activity of estramustine phosphate and its triterpenoid analogs
Bioorganic & Medicinal Chemistry Letters, 2011Co-Authors: Latanya M Scott, Liwei Chen, Kenyon G Daniel, Wesley H Brooks, Wayne C Guida, Harshani R Lawrence, Said M Sebti, Nicholas J LawrenceAbstract:Shp2 protein tyrosine phosphate (PTP) is a novel target for anticancer drug discovery. We identified estramustine phosphate as a Shp2 PTP inhibitor from the National Cancer Institute Approved Oncology Drug set. A focused structure-activity relationship study indicated that the 17-phosphate group is required for the Shp2 PTP inhibitor activity of estramustine phosphate. A search for estramustine phosphate analogs led to identification of two triterpenoids, Enoxolone, and celastrol, having Shp2 PTP inhibitor activity. With the previously reported PTP1B inhibitor trodusquemine, our study reveals steroids and triterpenoids with negatively charged phosphate, carboxylate, or sulfonate groups as novel pharmacophores of selective PTP inhibitors.
Latanya M Scott - One of the best experts on this subject based on the ideXlab platform.
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abstract 3239 shp2 inhibitor activity of estramustine phosphate and its triterpenoid analogues
Cancer Research, 2011Co-Authors: Latanya M Scott, Liwei Chen, Kenyon G Daniel, Wesley H Brooks, Wayne C Guida, Harshani R Lawrence, Said M Sebti, Murali K Urlam, Nicholas J LawrenceAbstract:Shp2 is a non-receptor protein tyrosine phosphatase (PTP) encoded by the PTPN11 gene. Shp2 mediates proliferative signaling induced by growth factors. Gain-of-function PTPN11 mutations that encode constitutively active Shp2 are leukemic oncogenes. In a continuing effort to identify new Shp2 PTP inhibitors, we screened a small molecule library comprising the National Cancer Institute (NCI) Approved Oncology Drug set and the NIH Clinical Collection. After evaluation of initial hits, estramustine phosphate was verified as a Shp2 PTP inhibitor. A focused structure-activity relationship study indicated that the 17-phosphate group is required for the Shp2 PTP inhibitor activity of estramustine phosphate. A search for estramustine phosphate analogs led to identification of two triperpenoids, Enoxolone and celastrol, having Shp2 PTP inhibitor activity. With the previously reported PTP1B inhibitor trodusquemine, our study reveals steroids and triterpenoids with negatively charged phosphate, carboxylate, or sulfonate groups as novel pharmacophores of selective PTP inhibitors. These findings point to a rich natural source for discovery of lead compounds of novel PTP inhibitors. Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 102nd Annual Meeting of the American Association for Cancer Research; 2011 Apr 2-6; Orlando, FL. Philadelphia (PA): AACR; Cancer Res 2011;71(8 Suppl):Abstract nr 3239. doi:10.1158/1538-7445.AM2011-3239
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shp2 protein tyrosine phosphatase inhibitor activity of estramustine phosphate and its triterpenoid analogs
Bioorganic & Medicinal Chemistry Letters, 2011Co-Authors: Latanya M Scott, Liwei Chen, Kenyon G Daniel, Wesley H Brooks, Wayne C Guida, Harshani R Lawrence, Said M Sebti, Nicholas J LawrenceAbstract:Shp2 protein tyrosine phosphate (PTP) is a novel target for anticancer drug discovery. We identified estramustine phosphate as a Shp2 PTP inhibitor from the National Cancer Institute Approved Oncology Drug set. A focused structure-activity relationship study indicated that the 17-phosphate group is required for the Shp2 PTP inhibitor activity of estramustine phosphate. A search for estramustine phosphate analogs led to identification of two triterpenoids, Enoxolone, and celastrol, having Shp2 PTP inhibitor activity. With the previously reported PTP1B inhibitor trodusquemine, our study reveals steroids and triterpenoids with negatively charged phosphate, carboxylate, or sulfonate groups as novel pharmacophores of selective PTP inhibitors.
Jian Jiang - One of the best experts on this subject based on the ideXlab platform.
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Simultaneous determination of multiple bioactive components of Bu-zhong-yi-qi-tang in rat tissues by LC-MS/MS: Application to a tissue distribution study.
Journal of chromatography. B Analytical technologies in the biomedical and life sciences, 2017Co-Authors: Wenwen Chen, Mengmeng Wang, Jin Zeng, Zhirong Zhang, Shujiao Shen, Jian JiangAbstract:A liquid chromatography coupled with electrospray ionization mass spectrometry method was developed and validated for simultaneous determination of seven bioactive constituents including astragaloside IV, calycosin, glycyrrhizic acid, Enoxolone, saikosaponin D, ferulic acid and hesperiden in rats' various tissues using diclofenac as the internal standard (IS). Biological samples were pretreated by protein precipitation with acetonitrile. The chromatographic separation was carried out on a C18 column with a gradient mobile phase consisting of acetonitrile and water (containing 0.1% formic acid and 4mM ammonium acetate). All analytes and IS were quantitated through electrospray ionization in negative ion multiple reaction monitoring mode. The mass transitions were as follows: m/z 829.7→783.3 for astragaloside IV, m/z 283.3→267.7 for calycosin, m/z 821.6→350.0 for glycyrrhizic acid, m/z 469.9→425.2 for Enoxolone, m/z 825.7→779.6 for saikosaponin D, m/z 192.5→133.9 for ferulic acid, m/z 609.1→301.0 for hesperiden and m/z 293.6→249.9 for the IS, respectively. The lower limits of quantification for the seven analytes in different rat tissues were 0.2-20ng/mL. Bu-zhong-yi-qi-tang (Hochuekkito in Japan, Bojungikki-tang in Korea) is one of the most frequently prescribed traditional herbal formulas used in Korea, Japan, and China to treat gastrointestinal diseases, cancer and chronic fatigue syndrome. The validated method was successfully applied to a tissue distribution study of the seven components in rat tissue after oral administration of Bu-zhong-yi-qi-tang concentrated granule. The results of the tissue distribution study showed that the high concentration of seven components were mainly in the gastrointestinal tract.
Wayne C Guida - One of the best experts on this subject based on the ideXlab platform.
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abstract 3239 shp2 inhibitor activity of estramustine phosphate and its triterpenoid analogues
Cancer Research, 2011Co-Authors: Latanya M Scott, Liwei Chen, Kenyon G Daniel, Wesley H Brooks, Wayne C Guida, Harshani R Lawrence, Said M Sebti, Murali K Urlam, Nicholas J LawrenceAbstract:Shp2 is a non-receptor protein tyrosine phosphatase (PTP) encoded by the PTPN11 gene. Shp2 mediates proliferative signaling induced by growth factors. Gain-of-function PTPN11 mutations that encode constitutively active Shp2 are leukemic oncogenes. In a continuing effort to identify new Shp2 PTP inhibitors, we screened a small molecule library comprising the National Cancer Institute (NCI) Approved Oncology Drug set and the NIH Clinical Collection. After evaluation of initial hits, estramustine phosphate was verified as a Shp2 PTP inhibitor. A focused structure-activity relationship study indicated that the 17-phosphate group is required for the Shp2 PTP inhibitor activity of estramustine phosphate. A search for estramustine phosphate analogs led to identification of two triperpenoids, Enoxolone and celastrol, having Shp2 PTP inhibitor activity. With the previously reported PTP1B inhibitor trodusquemine, our study reveals steroids and triterpenoids with negatively charged phosphate, carboxylate, or sulfonate groups as novel pharmacophores of selective PTP inhibitors. These findings point to a rich natural source for discovery of lead compounds of novel PTP inhibitors. Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 102nd Annual Meeting of the American Association for Cancer Research; 2011 Apr 2-6; Orlando, FL. Philadelphia (PA): AACR; Cancer Res 2011;71(8 Suppl):Abstract nr 3239. doi:10.1158/1538-7445.AM2011-3239
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shp2 protein tyrosine phosphatase inhibitor activity of estramustine phosphate and its triterpenoid analogs
Bioorganic & Medicinal Chemistry Letters, 2011Co-Authors: Latanya M Scott, Liwei Chen, Kenyon G Daniel, Wesley H Brooks, Wayne C Guida, Harshani R Lawrence, Said M Sebti, Nicholas J LawrenceAbstract:Shp2 protein tyrosine phosphate (PTP) is a novel target for anticancer drug discovery. We identified estramustine phosphate as a Shp2 PTP inhibitor from the National Cancer Institute Approved Oncology Drug set. A focused structure-activity relationship study indicated that the 17-phosphate group is required for the Shp2 PTP inhibitor activity of estramustine phosphate. A search for estramustine phosphate analogs led to identification of two triterpenoids, Enoxolone, and celastrol, having Shp2 PTP inhibitor activity. With the previously reported PTP1B inhibitor trodusquemine, our study reveals steroids and triterpenoids with negatively charged phosphate, carboxylate, or sulfonate groups as novel pharmacophores of selective PTP inhibitors.
Said M Sebti - One of the best experts on this subject based on the ideXlab platform.
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abstract 3239 shp2 inhibitor activity of estramustine phosphate and its triterpenoid analogues
Cancer Research, 2011Co-Authors: Latanya M Scott, Liwei Chen, Kenyon G Daniel, Wesley H Brooks, Wayne C Guida, Harshani R Lawrence, Said M Sebti, Murali K Urlam, Nicholas J LawrenceAbstract:Shp2 is a non-receptor protein tyrosine phosphatase (PTP) encoded by the PTPN11 gene. Shp2 mediates proliferative signaling induced by growth factors. Gain-of-function PTPN11 mutations that encode constitutively active Shp2 are leukemic oncogenes. In a continuing effort to identify new Shp2 PTP inhibitors, we screened a small molecule library comprising the National Cancer Institute (NCI) Approved Oncology Drug set and the NIH Clinical Collection. After evaluation of initial hits, estramustine phosphate was verified as a Shp2 PTP inhibitor. A focused structure-activity relationship study indicated that the 17-phosphate group is required for the Shp2 PTP inhibitor activity of estramustine phosphate. A search for estramustine phosphate analogs led to identification of two triperpenoids, Enoxolone and celastrol, having Shp2 PTP inhibitor activity. With the previously reported PTP1B inhibitor trodusquemine, our study reveals steroids and triterpenoids with negatively charged phosphate, carboxylate, or sulfonate groups as novel pharmacophores of selective PTP inhibitors. These findings point to a rich natural source for discovery of lead compounds of novel PTP inhibitors. Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 102nd Annual Meeting of the American Association for Cancer Research; 2011 Apr 2-6; Orlando, FL. Philadelphia (PA): AACR; Cancer Res 2011;71(8 Suppl):Abstract nr 3239. doi:10.1158/1538-7445.AM2011-3239
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shp2 protein tyrosine phosphatase inhibitor activity of estramustine phosphate and its triterpenoid analogs
Bioorganic & Medicinal Chemistry Letters, 2011Co-Authors: Latanya M Scott, Liwei Chen, Kenyon G Daniel, Wesley H Brooks, Wayne C Guida, Harshani R Lawrence, Said M Sebti, Nicholas J LawrenceAbstract:Shp2 protein tyrosine phosphate (PTP) is a novel target for anticancer drug discovery. We identified estramustine phosphate as a Shp2 PTP inhibitor from the National Cancer Institute Approved Oncology Drug set. A focused structure-activity relationship study indicated that the 17-phosphate group is required for the Shp2 PTP inhibitor activity of estramustine phosphate. A search for estramustine phosphate analogs led to identification of two triterpenoids, Enoxolone, and celastrol, having Shp2 PTP inhibitor activity. With the previously reported PTP1B inhibitor trodusquemine, our study reveals steroids and triterpenoids with negatively charged phosphate, carboxylate, or sulfonate groups as novel pharmacophores of selective PTP inhibitors.