Imaging of Platelet-Derived Growth Factor Receptor β Expression in Glioblastoma Xenografts Using Affibody Molecule¹¹¹In-DOTA-Z09591

Imaging of HER3-expressing xenografts in mice using a 99mTc(CO)3-HEHEHE-ZHER3:08699 affibody molecule

“…The high renal re-absorption of the radioactivity was similar to re-absorption of affibody molecules to other tyrosine kinase receptors (e.g. HER2 [38], HER1 [18], IGF-1R [19], PDGFRβ [39]), and is, probably, a property of this scaffold. Radioactivity accumulation in kidneys was not reduced with time, which reflected residualising properties of the label and was in agreement with previous observations for small proteins labeled using 99m Tc(CO) 3 [37,40].…”

Role of the anti-glioma drug AT13148 in the inhibition of Notch signaling pathway

“…PDGFRB is a Notch signaling target in human, encoding a cell surface tyrosine kinase receptor for genes in the platelet-derived growth factor family (Jin et al, 2008). Abnormal signaling mediated through high expression of PDGFRB has been proposed as a possible mechanism for initiation and progression of spinal cord glioma (Haberler et al, 2006;Liu et al, 2011;Tolmachev et al, 2014). Thus, several studies have attempted to inhibit PDGFRB accumulation to avoid the PDGFB-induced glioma growth (Holdhoff et al, 2005;Camorani et al, 2014).…”

How receptor diffusion influences gradient sensing

“…Diffusion constants of relevant receptors such as epidermal growth factor receptor (EGFR) and platelet-derived factor receptors are of order 10 22 mm 2 , whereas the dissociation constants are of order 10 21 s, suggesting that this approximation is valid at K d and higher concentrations [24][25][26][27][28].…”