دورية أكاديمية
Discovery of Novel Receptor Tyrosine Kinase-like Orphan Receptor 1 (ROR1) Inhibitors for Cancer Treatment.
| العنوان: | Discovery of Novel Receptor Tyrosine Kinase-like Orphan Receptor 1 (ROR1) Inhibitors for Cancer Treatment. |
|---|---|
| المؤلفون: | Luo D; Laboratory of Molecular Oncology, Frontiers Science Center for Disease-related Molecular Network, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu 610064, China., Qiu X; Laboratory of Molecular Oncology, Frontiers Science Center for Disease-related Molecular Network, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu 610064, China., Zheng Q; Laboratory of Molecular Oncology, Frontiers Science Center for Disease-related Molecular Network, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu 610064, China., Ming Y; Laboratory of Molecular Oncology, Frontiers Science Center for Disease-related Molecular Network, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu 610064, China., Pu W; Laboratory of Molecular Oncology, Frontiers Science Center for Disease-related Molecular Network, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu 610064, China., Ai M; Laboratory of Molecular Oncology, Frontiers Science Center for Disease-related Molecular Network, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu 610064, China., He J; Laboratory of Molecular Oncology, Frontiers Science Center for Disease-related Molecular Network, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu 610064, China., Peng Y; Laboratory of Molecular Oncology, Frontiers Science Center for Disease-related Molecular Network, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu 610064, China.; Frontier Medical Center, Tianfu Jincheng Laboratory, Chengdu 610212, China. |
| المصدر: | Journal of medicinal chemistry [J Med Chem] 2024 Jul 11; Vol. 67 (13), pp. 10655-10686. Date of Electronic Publication: 2024 Jun 24. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Washington Dc : American Chemical Society Original Publication: [Easton, Pa.] : American Chemical Society, [c1963- |
| مواضيع طبية MeSH: | Receptor Tyrosine Kinase-like Orphan Receptors*/antagonists & inhibitors , Receptor Tyrosine Kinase-like Orphan Receptors*/metabolism , Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/chemistry , Antineoplastic Agents*/chemical synthesis , Antineoplastic Agents*/therapeutic use, Humans ; Animals ; Structure-Activity Relationship ; Mice ; Cell Line, Tumor ; Protein Kinase Inhibitors/pharmacology ; Protein Kinase Inhibitors/chemistry ; Protein Kinase Inhibitors/chemical synthesis ; Protein Kinase Inhibitors/therapeutic use ; Apoptosis/drug effects ; Female ; Cell Proliferation/drug effects ; Drug Discovery ; Drug Screening Assays, Antitumor ; Molecular Docking Simulation ; Mice, Nude ; Lung Neoplasms/drug therapy ; Lung Neoplasms/pathology ; Lung Neoplasms/metabolism ; Mice, Inbred BALB C ; Molecular Structure ; Xenograft Model Antitumor Assays |
| مستخلص: | Receptor tyrosine kinase-like orphan receptor 1 (ROR1) is an oncogenic membrane protein in several malignancies and has been considered an attractive target for the treatment of human cancers. In this study, structure-based virtual screening and structure optimization were conducted to identify novel ROR1 inhibitors. Based on hit compound 2 , 45 novel ROR1 inhibitors were designed and synthesized, and the detailed structure-activity relationship was investigated. Representative compound 19h potently binds ROR1 with a K |
| المشرفين على المادة: | EC 2.7.10.1 (Receptor Tyrosine Kinase-like Orphan Receptors) EC 2.7.10.1 (ROR1 protein, human) 0 (Antineoplastic Agents) 0 (Protein Kinase Inhibitors) |
| تواريخ الأحداث: | Date Created: 20240624 Date Completed: 20240711 Latest Revision: 20240715 |
| رمز التحديث: | 20240715 |
| DOI: | 10.1021/acs.jmedchem.4c00175 |
| PMID: | 38913699 |
| قاعدة البيانات: | MEDLINE |
Find this issue from the American Chemical Society | تدمد: | 1520-4804 |
|---|---|
| DOI: | 10.1021/acs.jmedchem.4c00175 |