Fibroblast growth factors, old kids on the new block

Developing Predictive Approaches to Characterize Adaptive Responses of the Reproductive Endocrine Axis to Aromatase Inhibition: I. Data Generation in a Small Fish Model

Fibroblast growth factors (FGFs) are pleiotropic molecules exerting autocrine, intracrine and paracrine functions via activating four tyrosine kinase FGF receptors (FGFR), which further trigger a variety of cellular processes including angiogenesis, evasion from apoptosis, bone formation, embryogenesis, wound repair and homeostasis. Four major mechanisms including angiogenesis, inflammation, cell proliferation, and metastasis are active in FGF/FGFR-driven tumors. Furthermore, gain-of-function or loss-of-function in FGFRs1-4 which is due to amplification, fusions, mutations, and changes in tumor-stromal cells interactions, is associated with the development and progression of cancer. Although, the developed small molecule or antibodies targeting FGFR signaling offer immense potential for cancer therapy, emergence of drug resistance, activation of compensatory pathways and systemic toxicity of modulators are bottlenecks in clinical application of anti-FGFRs. In this review, we present FGF/FGFR structure and the mechanisms of its function, as well as cross-talks with other nodes and/or signaling pathways. We describe deregulation of FGF/FGFR-related mechanisms in human disease and tumor progression leading to the presentation of emerging therapeutic approaches, resistance to FGFR targeting, and clinical potentials of individual FGF family in several human cancers. Additionally, the underlying biological mechanisms of FGF/FGFR signaling, besides several attempts to develop predictive biomarkers and combination therapies for different cancers have been explored.

Implications of Fibroblast Growth Factors (FGFs) in Cancer: From Prognostic to Therapeutic Applications

Fibroblast growth factor 2 (FGF2) plays a critical role in tumorigenesis and progression of solid tumor and is upregulated in gastric carcinoma serum. Therefore, it is regarded as a potential therapeutic target of human gastric cancer. Suppression of bioactivities of FGF2 may contribute to human gastric cancer therapy. Herein, we obtained a novel FGF2-binding peptide derivative (named P32), which originated from a previously isolated P7 peptide with poor stability. We proved that P32, which had a half-life in human plasma up to 12 h, enhanced stability and exerted strong inhibitory effect on FGF2-induced cell proliferation and invasion in human gastric cancer cell lines. Further investigations revealed that the underlying anti-proliferation mechanisms of P32 in vitro included arresting FGF2-stimulated cells at the G0/G1 phase and reducing the activation of AKT and Erk1/2 cascades. The FGF2-binding peptide derivative P32 has improved stability, is relatively safe, and may have therapeutic potential in FGF2-driven gastric cancer.

A peptide derivative serves as a fibroblast growth factor 2 antagonist in human gastric cancer.

In the mol­ecule of the title compound, C17H14BrFO3, the aromatic rings are tilted with respect to the enone bridge by 13.63 (14) and 4.27 (15)°, and form a dihedral angle 17.91 (17)°. In the crystal, centrosymmetrically related mol­ecules are linked by pairs of C—H⋯O hydrogen bonds into dimeric units, forming rings of R22(14) graph-set motif. The dimers are further connected by weak C—H⋯O hydrogen inter­actions, forming layers parallel to (10\overline{1}). Hirshfeld surface analysis shows that van der Waals inter­actions constitute the major contribution to the inter­molecular inter­actions, with H⋯H contacts accounting for 29.7% of the surface.

https://journals.iucr.org/e/issues/2019/07/00/is5515/is5515.pdf

Crystal structure and Hirshfeld surface analysis of (2E)-3-(3-bromo-4-fluoro­phen­yl)-1-(3,4-di­meth­oxy­phen­yl)prop-2-en-1-one

Some fibroblast growth factors (FGFs) play a critical role in tumorigenesis and progression. Among them, FGF2 was highly expressed in some tumors, and antagonists binding to FGF2 can suppress the growth of tumor cells. Therefore, FGF2 has been considered as an important target in cancer therapy. In this study, we identified a novel FGF2-binding short peptide (P8, PLLQATAGGGS-NH2) using phage display technology and alanine scanning. The P8 peptide suppressed FGF2-induced proliferation with no cytotoxic effect on cells, arrested the cycle at the G0/G1 phase in B16-F10 cells, and downregulated the activation of fibroblast growth factor receptor substrate 2α (FRS2α)/ERK cascade in B16-F10, NIH-H460, and SGC-7901 cells. Besides, P8 peptide can also inhibit the phosphorylation of FRS2α stimulated by FGF1 and KGF2. These implied that P8 peptide may develop as a multi-target antagonist peptide contributing to tumor treatment.

A novel FGF2 antagonist peptide P8 with potent antiproliferation activity.

The crystal structure of the title compound, C17H15BrO3, a chalcone derivative, exhibits two crystallographically independent mol­ecules per asymmetric unit showing an E conformation about the ethyl­ene double bond. In each mol­ecule, the two phenyl rings are almost coplanar: the mean planes make dihedral angles of 9.3 (2) and 19.4 (2)°. In the crystal, mol­ecules are linked through weak inter­molecular C—H⋯O hydrogen bonds.

https://journals.iucr.org/e/issues/2012/03/00/zq2148/zq2148.pdf

(E)-3-(2-Bromo­phen­yl)-1-(3,4-dimeth­oxy­phen­yl)prop-2-en-1-one

The title compound, C22H21Cl2NO, is a derivative of mono-carbonyl analogues of curcumin (MACs). The mol­ecule has an E conformation for each of the olefinic bonds. The 1-propyl­piperidin-4-one ring has a distorted chair conformation with the ring N and the C and O atoms of the carbonyl group deviating from the mean plane of the remaining four ring C atoms by 0.682 (2), −0.134 (3) and −0.340 (4) A, respectively. The dihedral angle between the benzene rings is 26.5 (1)°. In the crystal, mol­ecules are connected by weak C—H⋯O and C—H⋯π inter­actions.

https://journals.iucr.org/e/issues/2013/01/00/zq2188/zq2188.pdf

(3E,5E)-3,5-Bis(2-chloro-benzyl-idene)-1-propyl-piperidin-4-one.

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A novel FGF2 antagonist peptide P8 with potent antiproliferation activity.

(E)-3-(2-Bromophenyl)-1-(3,4-dimethoxyphenyl)prop-2-en-1-one

(3E,5E)-3,5-Bis(2-chloro-benzyl-idene)-1-propyl-piperidin-4-one.

Lingzi Chen

Author Tools

Chat about Author

Papers

A novel FGF2 antagonist peptide P8 with potent antiproliferation activity.

(E)-3-(2-Bromo­phen­yl)-1-(3,4-dimeth­oxy­phen­yl)prop-2-en-1-one

(3E,5E)-3,5-Bis(2-chloro-benzyl-idene)-1-propyl-piperidin-4-one.

(E)-3-(2-Bromophenyl)-1-(3,4-dimethoxyphenyl)prop-2-en-1-one