The Experts below are selected from a list of 259044 Experts worldwide ranked by ideXlab platform
Hiroshi Miki - One of the best experts on this subject based on the ideXlab platform.
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design and synthesis of novel human epidermal Growth Factor Receptor 2 her2 epidermal Growth Factor Receptor egfr dual inhibitors bearing a pyrrolo 3 2 d pyrimidine scaffold
Journal of Medicinal Chemistry, 2011Co-Authors: Tomoyasu Ishikawa, Masaki Seto, Hiroshi Banno, Youichi Kawakita, Mami Oorui, Takahiko Taniguchi, Yoshikazu Ohta, Toshiya Tamura, Akiko Nakayama, Hiroshi MikiAbstract:Dual inhibitors of human epidermal Growth Factor Receptor 2 (HER2) and epidermal Growth Factor Receptor (EGFR) have been investigated for breast, lung, gastric, prostate, and other cancers; one, lapatinib, is currently approved for breast cancer. To develop novel HER2/EGFR dual kinase inhibitors, we designed and synthesized pyrrolo[3,2-d]pyrimidine derivatives capable of fitting into the Receptors’ ATP binding site. Among the prepared compounds, 34e showed potent HER2 and EGFR (HER1) inhibitory activities as well as tumor Growth inhibitory activity. The X-ray cocrystal structures of 34e with both HER2 and EGFR demonstrated that 34e interacts with the expected residues in their respective ATP pockets. Furthermore, reflecting its good oral bioavailability, 34e exhibited potent in vivo efficacy in HER2-overexpressing tumor xenograft models. On the basis of these findings, we report 34e (TAK-285) as a promising candidate for clinical development as a novel HER2/EGFR dual kinase inhibitor.
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design and synthesis of novel human epidermal Growth Factor Receptor 2 her2 epidermal Growth Factor Receptor egfr dual inhibitors bearing a pyrrolo 3 2 d pyrimidine scaffold
Journal of Medicinal Chemistry, 2011Co-Authors: Tomoyasu Ishikawa, Masaki Seto, Hiroshi Banno, Youichi Kawakita, Mami Oorui, Takahiko Taniguchi, Yoshikazu Ohta, Toshiya Tamura, Akiko Nakayama, Hiroshi MikiAbstract:Dual inhibitors of human epidermal Growth Factor Receptor 2 (HER2) and epidermal Growth Factor Receptor (EGFR) have been investigated for breast, lung, gastric, prostate, and other cancers; one, lapatinib, is currently approved for breast cancer. To develop novel HER2/EGFR dual kinase inhibitors, we designed and synthesized pyrrolo[3,2-d]pyrimidine derivatives capable of fitting into the Receptors’ ATP binding site. Among the prepared compounds, 34e showed potent HER2 and EGFR (HER1) inhibitory activities as well as tumor Growth inhibitory activity. The X-ray cocrystal structures of 34e with both HER2 and EGFR demonstrated that 34e interacts with the expected residues in their respective ATP pockets. Furthermore, reflecting its good oral bioavailability, 34e exhibited potent in vivo efficacy in HER2-overexpressing tumor xenograft models. On the basis of these findings, we report 34e (TAK-285) as a promising candidate for clinical development as a novel HER2/EGFR dual kinase inhibitor.
Tomoyasu Ishikawa - One of the best experts on this subject based on the ideXlab platform.
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design and synthesis of novel human epidermal Growth Factor Receptor 2 her2 epidermal Growth Factor Receptor egfr dual inhibitors bearing a pyrrolo 3 2 d pyrimidine scaffold
Journal of Medicinal Chemistry, 2011Co-Authors: Tomoyasu Ishikawa, Masaki Seto, Hiroshi Banno, Youichi Kawakita, Mami Oorui, Takahiko Taniguchi, Yoshikazu Ohta, Toshiya Tamura, Akiko Nakayama, Hiroshi MikiAbstract:Dual inhibitors of human epidermal Growth Factor Receptor 2 (HER2) and epidermal Growth Factor Receptor (EGFR) have been investigated for breast, lung, gastric, prostate, and other cancers; one, lapatinib, is currently approved for breast cancer. To develop novel HER2/EGFR dual kinase inhibitors, we designed and synthesized pyrrolo[3,2-d]pyrimidine derivatives capable of fitting into the Receptors’ ATP binding site. Among the prepared compounds, 34e showed potent HER2 and EGFR (HER1) inhibitory activities as well as tumor Growth inhibitory activity. The X-ray cocrystal structures of 34e with both HER2 and EGFR demonstrated that 34e interacts with the expected residues in their respective ATP pockets. Furthermore, reflecting its good oral bioavailability, 34e exhibited potent in vivo efficacy in HER2-overexpressing tumor xenograft models. On the basis of these findings, we report 34e (TAK-285) as a promising candidate for clinical development as a novel HER2/EGFR dual kinase inhibitor.
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design and synthesis of novel human epidermal Growth Factor Receptor 2 her2 epidermal Growth Factor Receptor egfr dual inhibitors bearing a pyrrolo 3 2 d pyrimidine scaffold
Journal of Medicinal Chemistry, 2011Co-Authors: Tomoyasu Ishikawa, Masaki Seto, Hiroshi Banno, Youichi Kawakita, Mami Oorui, Takahiko Taniguchi, Yoshikazu Ohta, Toshiya Tamura, Akiko Nakayama, Hiroshi MikiAbstract:Dual inhibitors of human epidermal Growth Factor Receptor 2 (HER2) and epidermal Growth Factor Receptor (EGFR) have been investigated for breast, lung, gastric, prostate, and other cancers; one, lapatinib, is currently approved for breast cancer. To develop novel HER2/EGFR dual kinase inhibitors, we designed and synthesized pyrrolo[3,2-d]pyrimidine derivatives capable of fitting into the Receptors’ ATP binding site. Among the prepared compounds, 34e showed potent HER2 and EGFR (HER1) inhibitory activities as well as tumor Growth inhibitory activity. The X-ray cocrystal structures of 34e with both HER2 and EGFR demonstrated that 34e interacts with the expected residues in their respective ATP pockets. Furthermore, reflecting its good oral bioavailability, 34e exhibited potent in vivo efficacy in HER2-overexpressing tumor xenograft models. On the basis of these findings, we report 34e (TAK-285) as a promising candidate for clinical development as a novel HER2/EGFR dual kinase inhibitor.
Masaki Seto - One of the best experts on this subject based on the ideXlab platform.
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design and synthesis of novel human epidermal Growth Factor Receptor 2 her2 epidermal Growth Factor Receptor egfr dual inhibitors bearing a pyrrolo 3 2 d pyrimidine scaffold
Journal of Medicinal Chemistry, 2011Co-Authors: Tomoyasu Ishikawa, Masaki Seto, Hiroshi Banno, Youichi Kawakita, Mami Oorui, Takahiko Taniguchi, Yoshikazu Ohta, Toshiya Tamura, Akiko Nakayama, Hiroshi MikiAbstract:Dual inhibitors of human epidermal Growth Factor Receptor 2 (HER2) and epidermal Growth Factor Receptor (EGFR) have been investigated for breast, lung, gastric, prostate, and other cancers; one, lapatinib, is currently approved for breast cancer. To develop novel HER2/EGFR dual kinase inhibitors, we designed and synthesized pyrrolo[3,2-d]pyrimidine derivatives capable of fitting into the Receptors’ ATP binding site. Among the prepared compounds, 34e showed potent HER2 and EGFR (HER1) inhibitory activities as well as tumor Growth inhibitory activity. The X-ray cocrystal structures of 34e with both HER2 and EGFR demonstrated that 34e interacts with the expected residues in their respective ATP pockets. Furthermore, reflecting its good oral bioavailability, 34e exhibited potent in vivo efficacy in HER2-overexpressing tumor xenograft models. On the basis of these findings, we report 34e (TAK-285) as a promising candidate for clinical development as a novel HER2/EGFR dual kinase inhibitor.
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design and synthesis of novel human epidermal Growth Factor Receptor 2 her2 epidermal Growth Factor Receptor egfr dual inhibitors bearing a pyrrolo 3 2 d pyrimidine scaffold
Journal of Medicinal Chemistry, 2011Co-Authors: Tomoyasu Ishikawa, Masaki Seto, Hiroshi Banno, Youichi Kawakita, Mami Oorui, Takahiko Taniguchi, Yoshikazu Ohta, Toshiya Tamura, Akiko Nakayama, Hiroshi MikiAbstract:Dual inhibitors of human epidermal Growth Factor Receptor 2 (HER2) and epidermal Growth Factor Receptor (EGFR) have been investigated for breast, lung, gastric, prostate, and other cancers; one, lapatinib, is currently approved for breast cancer. To develop novel HER2/EGFR dual kinase inhibitors, we designed and synthesized pyrrolo[3,2-d]pyrimidine derivatives capable of fitting into the Receptors’ ATP binding site. Among the prepared compounds, 34e showed potent HER2 and EGFR (HER1) inhibitory activities as well as tumor Growth inhibitory activity. The X-ray cocrystal structures of 34e with both HER2 and EGFR demonstrated that 34e interacts with the expected residues in their respective ATP pockets. Furthermore, reflecting its good oral bioavailability, 34e exhibited potent in vivo efficacy in HER2-overexpressing tumor xenograft models. On the basis of these findings, we report 34e (TAK-285) as a promising candidate for clinical development as a novel HER2/EGFR dual kinase inhibitor.
Akiko Nakayama - One of the best experts on this subject based on the ideXlab platform.
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design and synthesis of novel human epidermal Growth Factor Receptor 2 her2 epidermal Growth Factor Receptor egfr dual inhibitors bearing a pyrrolo 3 2 d pyrimidine scaffold
Journal of Medicinal Chemistry, 2011Co-Authors: Tomoyasu Ishikawa, Masaki Seto, Hiroshi Banno, Youichi Kawakita, Mami Oorui, Takahiko Taniguchi, Yoshikazu Ohta, Toshiya Tamura, Akiko Nakayama, Hiroshi MikiAbstract:Dual inhibitors of human epidermal Growth Factor Receptor 2 (HER2) and epidermal Growth Factor Receptor (EGFR) have been investigated for breast, lung, gastric, prostate, and other cancers; one, lapatinib, is currently approved for breast cancer. To develop novel HER2/EGFR dual kinase inhibitors, we designed and synthesized pyrrolo[3,2-d]pyrimidine derivatives capable of fitting into the Receptors’ ATP binding site. Among the prepared compounds, 34e showed potent HER2 and EGFR (HER1) inhibitory activities as well as tumor Growth inhibitory activity. The X-ray cocrystal structures of 34e with both HER2 and EGFR demonstrated that 34e interacts with the expected residues in their respective ATP pockets. Furthermore, reflecting its good oral bioavailability, 34e exhibited potent in vivo efficacy in HER2-overexpressing tumor xenograft models. On the basis of these findings, we report 34e (TAK-285) as a promising candidate for clinical development as a novel HER2/EGFR dual kinase inhibitor.
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design and synthesis of novel human epidermal Growth Factor Receptor 2 her2 epidermal Growth Factor Receptor egfr dual inhibitors bearing a pyrrolo 3 2 d pyrimidine scaffold
Journal of Medicinal Chemistry, 2011Co-Authors: Tomoyasu Ishikawa, Masaki Seto, Hiroshi Banno, Youichi Kawakita, Mami Oorui, Takahiko Taniguchi, Yoshikazu Ohta, Toshiya Tamura, Akiko Nakayama, Hiroshi MikiAbstract:Dual inhibitors of human epidermal Growth Factor Receptor 2 (HER2) and epidermal Growth Factor Receptor (EGFR) have been investigated for breast, lung, gastric, prostate, and other cancers; one, lapatinib, is currently approved for breast cancer. To develop novel HER2/EGFR dual kinase inhibitors, we designed and synthesized pyrrolo[3,2-d]pyrimidine derivatives capable of fitting into the Receptors’ ATP binding site. Among the prepared compounds, 34e showed potent HER2 and EGFR (HER1) inhibitory activities as well as tumor Growth inhibitory activity. The X-ray cocrystal structures of 34e with both HER2 and EGFR demonstrated that 34e interacts with the expected residues in their respective ATP pockets. Furthermore, reflecting its good oral bioavailability, 34e exhibited potent in vivo efficacy in HER2-overexpressing tumor xenograft models. On the basis of these findings, we report 34e (TAK-285) as a promising candidate for clinical development as a novel HER2/EGFR dual kinase inhibitor.
Toshiya Tamura - One of the best experts on this subject based on the ideXlab platform.
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design and synthesis of novel human epidermal Growth Factor Receptor 2 her2 epidermal Growth Factor Receptor egfr dual inhibitors bearing a pyrrolo 3 2 d pyrimidine scaffold
Journal of Medicinal Chemistry, 2011Co-Authors: Tomoyasu Ishikawa, Masaki Seto, Hiroshi Banno, Youichi Kawakita, Mami Oorui, Takahiko Taniguchi, Yoshikazu Ohta, Toshiya Tamura, Akiko Nakayama, Hiroshi MikiAbstract:Dual inhibitors of human epidermal Growth Factor Receptor 2 (HER2) and epidermal Growth Factor Receptor (EGFR) have been investigated for breast, lung, gastric, prostate, and other cancers; one, lapatinib, is currently approved for breast cancer. To develop novel HER2/EGFR dual kinase inhibitors, we designed and synthesized pyrrolo[3,2-d]pyrimidine derivatives capable of fitting into the Receptors’ ATP binding site. Among the prepared compounds, 34e showed potent HER2 and EGFR (HER1) inhibitory activities as well as tumor Growth inhibitory activity. The X-ray cocrystal structures of 34e with both HER2 and EGFR demonstrated that 34e interacts with the expected residues in their respective ATP pockets. Furthermore, reflecting its good oral bioavailability, 34e exhibited potent in vivo efficacy in HER2-overexpressing tumor xenograft models. On the basis of these findings, we report 34e (TAK-285) as a promising candidate for clinical development as a novel HER2/EGFR dual kinase inhibitor.
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design and synthesis of novel human epidermal Growth Factor Receptor 2 her2 epidermal Growth Factor Receptor egfr dual inhibitors bearing a pyrrolo 3 2 d pyrimidine scaffold
Journal of Medicinal Chemistry, 2011Co-Authors: Tomoyasu Ishikawa, Masaki Seto, Hiroshi Banno, Youichi Kawakita, Mami Oorui, Takahiko Taniguchi, Yoshikazu Ohta, Toshiya Tamura, Akiko Nakayama, Hiroshi MikiAbstract:Dual inhibitors of human epidermal Growth Factor Receptor 2 (HER2) and epidermal Growth Factor Receptor (EGFR) have been investigated for breast, lung, gastric, prostate, and other cancers; one, lapatinib, is currently approved for breast cancer. To develop novel HER2/EGFR dual kinase inhibitors, we designed and synthesized pyrrolo[3,2-d]pyrimidine derivatives capable of fitting into the Receptors’ ATP binding site. Among the prepared compounds, 34e showed potent HER2 and EGFR (HER1) inhibitory activities as well as tumor Growth inhibitory activity. The X-ray cocrystal structures of 34e with both HER2 and EGFR demonstrated that 34e interacts with the expected residues in their respective ATP pockets. Furthermore, reflecting its good oral bioavailability, 34e exhibited potent in vivo efficacy in HER2-overexpressing tumor xenograft models. On the basis of these findings, we report 34e (TAK-285) as a promising candidate for clinical development as a novel HER2/EGFR dual kinase inhibitor.
