Entry of a cationic lytic-type peptide into the cytoplasm via endocytosis-dependent and -independent pathways in human glioma U251 cells

Endocytotic Routes of Cobra Cardiotoxins Depend on Spatial Distribution of Positively Charged and Hydrophobic Domains to Target Distinct Types of Sulfated Glycoconjugates on Cell Surface

“…Multiple mechanisms have been proposed for the internalization and/or penetration of cationic peptide into living cells, such as temperature/energy dependence (47), the involvement of proteoglycans (48,49), hydrophobicity (50), amphiphilicity (51), and distinct endocytotic pathways (52)(53)(54). The CTX homologues in the cobra venom are cationic polypeptide with different ligand-binding specificities and cellular targets.…”

CD147 monoclonal antibody mediated by chitosan nanoparticles loaded with α-hederin enhances antineoplastic activity and cellular uptake in liver cancer cells

“…The effects of endocytosis inhibitors on cellular uptake were evaluated with FACS. Briefly, 5 × 10 5 HepG2 cells per well were plated onto six-well plates pretreated with sodium azide 38 (NaN 3 , 200 μg/mL), sucrose 39 (0.45 M), chlorpromazine 40 (7 μg/mL), methyl-β-cyclodextrin 41 (MβCD, 3 nM), and wortmannin (500 nM) for 1 h. After rapid washing twice, the cells were incubated with FITC-labeled NPs for 2 h. The samples were resuspended for FACS analysis. The effects of endocytosis inhibitors were evaluated as the relative cell uptake rate with non-treated cells as background and NP-treated cells as positive control.…”

Multidimensional Design of Anticancer Peptides

“…Decoralin itself displayed pronounced cell-penetrating activity in MCF7 and A549 cells ( Figure 2B,C), thus corroborating previous observations that ACPs could show mixed membrane-lytic and cell-penetrating activities. [22] Our machine-learning models were apparently capable of identifying key features of CPPs and allowed us to transfer these to the Decoralin derivatives.M oreover,t he designed peptides retained anticancer activity.W e successfully tuned the Decoralin sequence according to these objectives and confirmed the additional cell-penetrating ability in MCF7 cells.I nA C1, AC2, and AC5, two serine residues of the Decoralin sequence are replaced by arginine, which is in line with previous work by Nakase et al,w ho showed that introducing an arginine residue into an ACPc ould improve membrane permeation. [23] However,their arginine-substituted peptides lost cytotoxicity against HeLa cells, thus suggesting ad elicately balanced structure-activity relationship between ACPs and CPPs.O ur peptide design strategy adequately addressed this issue through the SVM models.…”