Synthesis and biological activity of conjugates between paclitaxel and the cell delivery vector penetratin

CT and MR arthrograms demonstrate a consistent communication between the tibiofemoral and superior tibiofibular joints

“…Caveolae are novel cellular organizing centers for receptors, signaling machinery, integrins, and actin scaffolding complexes. Caveolin expression has been shown to inhibit TGF‐β1‐induced collagen type I, fibronectin, and alpha‐smooth muscle actin, phospho‐SMAD2 expression 54. Similarly, administration of a bipartite synthetic peptide composed of the AntP PTD fused to a scaffolding domain of caveolin 1‐inhibited bleomycin‐induced expression of tenascin C, α‐SMA, and collagen III 55…”

Internalization and Intracellular Trafficking of a PTD-Conjugated Anti-Fibrotic Peptide, AZX100, in Human Dermal Keloid Fibroblasts

“…Caveolin expression has been shown to inhibit TGF-b1-induced collagen type I, fibronectin, and alpha-smooth muscle actin, phospho-SMAD2 expression. 54 Similarly, administration of a bipartite synthetic peptide composed of the AntP PTD fused to a scaffolding domain of caveolin 1-inhibited bleomycin-induced expression of tenascin C, a-SMA, and collagen III. 55 The functional activity of phospho-caveolin-1 is poorly understood, but its localization near FA and associated microfilaments suggests a role in the regulation of actin and FA dynamics and the modulation of fibroblast-myofibroblast transformation.…”

Synthesis and biological evaluation of a peptide–paclitaxel conjugate which targets the integrin αvβ6

“…By comparison, 70% of paclitaxel is released from the peptide-paclitaxel conjugate after 48 h incubation in rat serum, with a half-life of approximately 20 h. The half-life of the conjugate in serum is similar to that observed for other paclitaxel ester linkers. 41 The increased release is likely due to participation of other proteases or esterases present in rat serum. This also raises some concern about the stability of the conjugate while in circulation; however, 86% of the conjugate remains intact in rat serum at 1 h. As the overall size of the complex is below the renal filtration cutoff, we believe most of the conjugate that does not reach the tumor will be cleared by the kidney within this time frame.…”

“…Other peptide-paclitaxel conjugates have shown reduced efficacy under short incubation times but the reason for the observation has not been determined. 16,41 However, improved biodistribution of the targeted drug conjugates in vivo can often overcome the loss of activity.…”