Screening a novel FGF3 antagonist peptide with anti-tumor effects on breast cancer from a phage display library.
Accumulating evidence has suggested that fibroblast growth factor 3 (FGF3) is expressed in breast cancer and correlates with the stage and grade of the disease. In the present study, a specific FGF3‑binding peptide (VLWLKNR, termed FP16) was isolated from a phage display heptapeptide library with FGF3. The peptide FP16 contained four identical (WLKN) amino acids and demonstrated high homology to the peptides of the 188‑194 (TMRWLKN) site of the high‑affinity FGF3 receptor fibroblast growth factor receptor 2. Functional analyses indicated that FP16 mediated significant inhibition of FGF3‑induced cell proliferation, arrested the cell cycle at the G0/G1 phase by increasing proliferation‑associated protein 2G4, suppressing cyclin D1 and proliferating cell nuclear antigen, and inhibited the FGF3‑induced activation of extracellular signal‑regulated kinase 1/2 and Akt kinase. Taken together, these results demonstrated that the peptide FP16, acting as an FGF3 antagonist, is a promising therapeutic agent for the treatment of breast cancer.
Department of Clinical Laboratory and Disease Control, Foshan Fourth People's Hospital, Foshan, Guangdong 528000, P.R. China.
Wei
W
Wang
Department of Provincial Reference Laboratory and Disease Control, Center for Tuberculosis Control of Guangdong, Guangzhou, Guangdong 510630, P.R. China.
Tao
T
Chen
Department of Provincial Reference Laboratory and Disease Control, Center for Tuberculosis Control of Guangdong, Guangzhou, Guangdong 510630, P.R. China.
Haicheng
H
Li
Department of Provincial Reference Laboratory and Disease Control, Center for Tuberculosis Control of Guangdong, Guangzhou, Guangdong 510630, P.R. China.
Yuhui
Y
Chen
Department of Clinical Laboratory and Disease Control, Foshan Fourth People's Hospital, Foshan, Guangdong 528000, P.R. China.
Zhilong
Z
Wu
Department of Clinical Laboratory and Disease Control, Foshan Fourth People's Hospital, Foshan, Guangdong 528000, P.R. China.
Tongming
T
Feng
Department of Clinical Laboratory and Disease Control, Foshan Fourth People's Hospital, Foshan, Guangdong 528000, P.R. China.
Xilin
X
Zhang
Department of Provincial Reference Laboratory and Disease Control, Center for Tuberculosis Control of Guangdong, Guangzhou, Guangdong 510630, P.R. China.
Qiu
Q
Zhong
Department of Clinical Laboratory and Disease Control, Foshan Fourth People's Hospital, Foshan, Guangdong 528000, P.R. China.
Qianhong
Q
Zhong
Department of Clinical Laboratory, Chronic Disease Control and Prevention Station of Dongguan, Dongguan, Guangdong 523008, P.R. China.
Guozhou
G
Li
Department of Nutrition, Guangdong Provincial Hospital of Chinese Traditional Medicine, Guangzhou, Guangdong 510120, P.R. China.
Lina
L
Guo
Department of Provincial Reference Laboratory and Disease Control, Center for Tuberculosis Control of Guangdong, Guangzhou, Guangdong 510630, P.R. China.
Lin
L
Zhou
Department of Clinical Laboratory and Disease Control, Foshan Fourth People's Hospital, Foshan, Guangdong 528000, P.R. China.
Jie
J
Zhou
D000595:Amino Acid Sequence; D000970:Antineoplastic Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D001943:Breast Neoplasms / Q000378:metabolism / Q000473:pathology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D019938:Cyclin D1 / Q000378:metabolism; D004353:Drug Evaluation, Preclinical; D005260:Female; D051518:Fibroblast Growth Factor 3 / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D059585:G1 Phase Cell Cycle Checkpoints / Q000187:drug effects; D006801:Humans; D019151:Peptide Library; D010455:Peptides / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D010766:Phosphorylation / Q000187:drug effects; D011485:Protein Binding / Q000187:drug effects; D051057:Proto-Oncogene Proteins c-akt / Q000378:metabolism; D017468:Receptors, Fibroblast Growth Factor / Q000737:chemistry / Q000378:metabolism; D011994:Recombinant Proteins / Q000096:biosynthesis / Q000302:isolation & purification / Q000494:pharmacology; D015398:Signal Transduction / Q000187:drug effects
D000970:Antineoplastic Agents; D051518:Fibroblast Growth Factor 3; D019151:Peptide Library; D010455:Peptides; D017468:Receptors, Fibroblast Growth Factor; D011994:Recombinant Proteins; D019938:Cyclin D1; D051057:Proto-Oncogene Proteins c-akt