Direct and allosteric inhibition of the FGF2/HSPGs/FGFR1 ternary complex formation by an antiangiogenic, thrombospondin-1-mimic small molecule

K Pagano, R Torella, C Foglieni, A Bugatti… - PLoS …, 2012 - journals.plos.org
Fibroblast growth factors (FGFs) are recognized targets for the development of therapies
against angiogenesis-driven diseases, including cancer. The formation of a ternary complex …

Integrating computational and chemical biology tools in the discovery of antiangiogenic small molecule ligands of FGF2 derived from endogenous inhibitors

C Foglieni, K Pagano, M Lessi, A Bugatti, E Moroni… - Scientific Reports, 2016 - nature.com
Abstract The FGFs/FGFRs system is a recognized actionable target for therapeutic
approaches aimed at inhibiting tumor growth, angiogenesis, metastasis, and resistance to …

[HTML][HTML] Targeting tumor angiogenesis with TSP-1-based compounds: rational design of antiangiogenic mimetics of endogenous inhibitors

G Taraboletti, M Rusnati, L Ragona, G Colombo - Oncotarget, 2010 - ncbi.nlm.nih.gov
Inhibitors of angiogenesis are an important addition to conventional chemotherapy. Among
different “druggable” angiogenic factors, fibroblast growth factor-2 (FGF-2) is an attractive …

[HTML][HTML] Molecular mechanism of SSR128129E, an extracellularly acting, small-molecule, allosteric inhibitor of FGF receptor signaling

C Herbert, U Schieborr, K Saxena, J Juraszek… - Cancer cell, 2013 - cell.com
The fibroblast growth factor (FGF)/fibroblast growth factor receptor (FGFR) signaling network
plays an important role in cell growth, survival, differentiation, and angiogenesis …

Tumor vasculature is regulated by FGF/FGFR signaling‐mediated angiogenesis and bone marrow‐derived cell recruitment: this mechanism is inhibited by …

P Fons, G Gueguen‐Dorbes, JP Herault… - Journal of Cellular …, 2015 - Wiley Online Library
Tumor angiogenesis is accompanied by vasculogenesis, which is involved in the
differentiation and mobilization of human bone marrow cells. In order to further characterize …

Modulation of fibroblast growth factor-2 receptor binding, signaling, and mitogenic activity by heparin-mimicking polysulfonated compounds

S Liekens, D Leali, J Neyts, R Esnouf, M Rusnati… - Molecular …, 1999 - ASPET
Basic fibroblast growth factor (FGF-2) interacts with high-affinity tyrosine-kinase fibroblast
growth factor receptors (FGFRs) and low-affinity heparan sulfate proteoglycans (HSPGs) in …

Targeting drugs against fibroblast growth factor (s)-induced cell signaling

S Agrawal, S Maity, Z AlRaawi, M Al-Ameer… - Current drug …, 2021 - ingentaconnect.com
Background: The fibroblast growth factor (FGF) family is comprised of 23 highly regulated
monomeric proteins that regulate a plethora of developmental and pathophysiological …

Non-peptidic thrombospondin-1 mimics as fibroblast growth factor-2 inhibitors: an integrated strategy for the development of new antiangiogenic compounds

G Colombo, B Margosio, L Ragona, M Neves… - Journal of Biological …, 2010 - ASBMB
Endogenous inhibitors of angiogenesis, such as thrombospondin-1 (TSP-1), are promising
sources of therapeutic agents to treat angiogenesis-driven diseases, including cancer. TSP …

Fibroblast growth factor receptors 1 and 2 interact differently with heparin/heparan sulfate: implications for dynamic assembly of a ternary signaling complex

AK Powell, DG Fernig, JE Turnbull - Journal of Biological Chemistry, 2002 - ASBMB
Heparan sulfate (HS) regulates the kinetics of fibroblast growth factor 2 (FGF2)-stimulated
intracellular signaling and differentially activates cell proliferation of cells expressing …

Influence of heparin mimetics on assembly of the FGF· FGFR4 signaling complex

K Saxena, U Schieborr, O Anderka… - Journal of Biological …, 2010 - ASBMB
Fibroblast growth factor (FGF) signaling regulates mammalian development and
metabolism, and its dysregulation is implicated in many inherited and acquired diseases …