成纤维细胞生长因子受体

成纤维细胞生长因子受体（英语：fibroblast growth factor receptors，FGFR）是一类与成纤维细胞生长因子结合的受体蛋白质家族，参与了多种生理与发育过程，包括胚胎发育、血管生成、创伤愈合、以及器官形成等。当 FGFR 透过与其配体 FGF结合时，便能启动多种细胞内讯号传递路径^[1]。这类受体涉及了一些病理条件。例如，FGFR3上的一个位点突变可导致软骨发育不全症。

结构

成纤维细胞生长因子受体的结构包括在细胞外与配体结合的三个免疫球蛋白样结构域，一个单跨膜的螺旋结构域，和带有酪氨酸激酶活性的细胞内结构域。这些受体的配体是成纤维细胞生长因子，有22个成员^[2]^[3]，是最大的生长因子家族。

致癌原因

不正常的 FGF 讯号传递与多种疾病相关，尤其是在癌症中。大多数是基因扩增，其次是突变和重排/融合，当 FGFR 发生异常时，可能会导致讯号持续活化，进而促进肿瘤的形成与恶化。^[4]

FGFR 的异常表现不仅包含上述，还能在无配体情况下自发活化讯号，并根据不同配体触发不同构型与活性，依各类肿瘤类型呈现多样化，进一步凸显其作为治疗标靶的潜力。^[5]

参考文献

^ Desai, Arpita; Adjei, Alex A. FGFR Signaling as a Target for Lung Cancer Therapy. Journal of Thoracic Oncology. 2016-01, 11 (1) [2025-05-14]. doi:10.1016/j.jtho.2015.08.003. （原始内容存档于2024-04-13）（英语）.
^ Ornitz DM. and Itoh, N. Fibroblast growth factors. Genome Biol. 2001, 2 (3): REVIEWS 3005. PMC 138918 . PMID 11276432. doi:10.1186/gb-2001-2-3-reviews3005.
^ Belov AA, Mohammadi M. Molecular mechanisms of fibroblast growth factor signaling in physiology and pathology. Cold Spring Harbor Perspectives in Biology. June 2013, 5 (6). PMID 23732477. doi:10.1101/cshperspect.a015958.
^ Zhang, Pei; Yue, Lin; Leng, QingQing; Chang, Chen; Gan, Cailing; Ye, Tinghong; Cao, Dan. Targeting FGFR for cancer therapy. Journal of Hematology & Oncology. 2024-06-03, 17 (1) [2025-05-14]. ISSN 1756-8722. PMC 11149307 . PMID 38831455. doi:10.1186/s13045-024-01558-1. （原始内容存档于2024-06-06）（英语）.
^ Sobhani, Navid; Ianza, Anna; D’Angelo, Alberto; Roviello, Giandomenico; Giudici, Fabiola; Bortul, Marina; Zanconati, Fabrizio; Bottin, Cristina; Generali, Daniele. Current Status of Fibroblast Growth Factor Receptor-Targeted Therapies in Breast Cancer. Cells. 2018-07-15, 7 (7) [2025-05-14]. ISSN 2073-4409. PMC 6071019 . PMID 30011957. doi:10.3390/cells7070076. （原始内容存档于2025-03-22）（英语）.

外部链接

[1] Desai, Arpita; Adjei, Alex A. FGFR Signaling as a Target for Lung Cancer Therapy. Journal of Thoracic Oncology. 2016-01, 11 (1) [2025-05-14]. doi:10.1016/j.jtho.2015.08.003. （原始内容存档于2024-04-13）（英语）.

[ornitz-2] Ornitz DM. and Itoh, N. Fibroblast growth factors. Genome Biol. 2001, 2 (3): REVIEWS 3005. PMC 138918 . PMID 11276432. doi:10.1186/gb-2001-2-3-reviews3005.

[3] Belov AA, Mohammadi M. Molecular mechanisms of fibroblast growth factor signaling in physiology and pathology. Cold Spring Harbor Perspectives in Biology. June 2013, 5 (6). PMID 23732477. doi:10.1101/cshperspect.a015958.

[4] Zhang, Pei; Yue, Lin; Leng, QingQing; Chang, Chen; Gan, Cailing; Ye, Tinghong; Cao, Dan. Targeting FGFR for cancer therapy. Journal of Hematology & Oncology. 2024-06-03, 17 (1) [2025-05-14]. ISSN 1756-8722. PMC 11149307 . PMID 38831455. doi:10.1186/s13045-024-01558-1. （原始内容存档于2024-06-06）（英语）.

[5] Sobhani, Navid; Ianza, Anna; D’Angelo, Alberto; Roviello, Giandomenico; Giudici, Fabiola; Bortul, Marina; Zanconati, Fabrizio; Bottin, Cristina; Generali, Daniele. Current Status of Fibroblast Growth Factor Receptor-Targeted Therapies in Breast Cancer. Cells. 2018-07-15, 7 (7) [2025-05-14]. ISSN 2073-4409. PMC 6071019 . PMID 30011957. doi:10.3390/cells7070076. （原始内容存档于2025-03-22）（英语）.

[1]

[2]

[3]

[4]

[5]