saporin

Guo S, Xu H, Cheng Z, Wang L, Yang P, Wang R (2025) Efficient cytosolic delivery of protein by preorganized amidiniums on pillar[5]arene. CCL 111022. doi: 10.1016/j.cclet.2025.111022

Objective: To use amidinium functionalized pillar[5]arene (AP5) as a small molecular carrier to facilitate intracellular delivery of proteins with different sizes and isoelectric points.

Summary: The densely preorganized amidinium groups on pillar[5]arene skeleton could not only glue proteins together to form AP5@protein complex through multiple salt-bridges, but also promote cellular internalization AP5@protein complex. The bioactivities of the internalized proteins were well-maintained. This study provides a novel, versatile and macrocyclic-molecule based intracellular protein delivery carrier through the preorganization of amidiniums onpillar[5]arene.

Usage: The AP5@saporin complexes showed significant toxicity toward HeLa cells with an IC50 of 102 nmol/L. However, saporin alone showed minimal toxicity on HeLa cells due to membrane-impermeability of saporin.

Related Products: Saporin (Cat. #PR-01)

Rahhal N, Rentzsch M, Seiser S, Freystätter C, Elbe-Bürger A, Rademacher C (2025) Targeted delivery of cytotoxic proteins via lipid-based nanoparticles to primary Langerhans cells. Nanoscale 17(7):4038-4046. doi: 10.1039/d4nr03638g PMID: 39775685

Summary: Saporin was used as a model protein to showcase the potential of delivering intact proteins to Langerhans cells. Authors observed specific killing of cells expressing langerin in vitro, and in primary Langerhans cells isolated from mouse and human skin ex vivo with minimal off target effects.

Related Products: Saporin (Cat. #PR-01)

Zhao Z, Zhang H, Li W, Wang Y, Wang Y, Yang H, Yin L, Liu X (2025) Guanidyl-rich α-helical polypeptide enables efficient cytosolic pro-protein delivery and CRISPR-Cas9 genome editing. J Mater Chem B 13(6):1991-2002. doi: 10.1039/d4tb02009j PMID: 39760520

Objective: To develop an efficient strategy via cationic alpha-helical polypeptide-mediated anionic proprotein delivery.

Summary: The protein was reversibly modified with adenosine triphosphateviadynamic covalent chemistry to prepare an anionic proprotein (A-protein) with abundant phosphate groups. A guanidyl-decorated a-helical polypeptide (LPP) was employed not only to encapsulate A-protein through electrostatic attraction and hydrogen bonding, forming stable nanocomplexes, but also to enhance cell membrane penetration due to its rigid alpha-helical conformation. Consequently, this strategy mediated the effective delivery of various proteins with different isoelectric points and molecular weights, including a-chymotrypsin, bovine serum albumin, ribonuclease A, cytochromeC, saporin, horseradish peroxidase, b-galactosidase, and anti-phospho-Akt, into cancer cells.

Usage: Cytosolic delivery: Saporin, was employed to evaluate LPP-mediated cytosolic delivery and its cancer cell-killing efficacy. The LPP/A-saporin nocomplexes (NCs) caused significant toxicity, with an IC50 value of 0.4ug/mL. In vivo antitumor efficiency of LPP/A-saporin NCs: LPP/A-saporin NCs were administrated by intratumoral injection in HeLa xenograft tumor-bearing mice and their antitumor efficacy was evaluated. When the tumor volume reached B50 mm3, the mice were randomly divided into three groups (6 mice per group) and intratumorally injected with PBS, free saporin, or LPP/A-saporin NCs at 0.1 mg saporin per kg on days 0 and 2.

Related Products: Saporin (Cat. #PR-01)

Nakano T, Okita K, Okazaki S, Yoshimoto S, Masuko S, Yagi H, Kato K, Tomioka Y, Imai K, Hamada Y, Masuko K, Shimada-Takaura K, Nagai N, Saya H, Arai T, Ishiwata T, Masuko T (2025) CD44v, S1PR1, HER3, MET and cancer-associated amino acid transporters are promising targets for the pancreatic cancers characterized using mAb. FEBS Open Bio 15(5):867-884. doi: 10.1002/2211-5463.13963 PMID: 39757718

Objective: To analyze pancreatic ductal adenocarcinomas (PDAC) using novel rat mAbs against membrane proteins in conjunction with flow cytometry and immunohistochemistry

Summary: Internalization of membrane proteins by mAbs and growth inhibition by toxin-linked mAbs were demonstrated in many PDAC cell lines, and mAbs against S1PR1, ASCT2, HER3 and CD44v inhibited the growth of xenografted MIA PaCa-2PDAC cells. Furthermore, CD44v-high PDAC showed high mRNA expression of HER1–3, MET and CD44v, and was correlated with poor prognosis. Taken together, the results suggest that CD44v, S1PR1, HER3, MET and the above-mentioned cancer-associated amino acid transporters might be promising targets for the diagnosis and treatment of PDAC.

Usage: Growth inhibition by rat mAbs against PDAC cell lines with secondary antibodies conjugated to saporin (PR-01). Rat mAb solution (4 ug/mL), a PDAC cell suspension and Saporin-conjugated goat anti-rat IgG pAb (Rat-ZAP, IT-26 at 4 ug/mL) were added to each well of 96-well plates.

Related Products: Saporin (Cat. #PR-01), Rat-ZAP (Cat. #IT-26)

Yin S, Tao Y, Li T, Li C, Cui Y, Zhang Y, Yin S, Zhao L, Hu P, Cui L, Wu Y, He Y, Yu S, Chen J, Lu S, Qiu G, Song M, Hou Q, Qian C, Zou Z, Xu S, Yu Y (2024) Itaconate facilitates viral infection via alkylating GDI2 and retaining Rab GTPase on the membrane. Signal Transduct Target Ther 9(1):371. doi: 10.1038/s41392-024-02077-8 PMID: 39730330

Objective: To demonstrate that the IRG1-itaconate axis facilitates the infections of vesicular stomatitis virus (VSV) and influenza A virus (IAV) in macrophages and epithelial cells via Rab GTPases redistribution.

Summary: The study reveals that neutrophils-derived itaconate facilitates viral infection via redistribution of Rab GTPases, suggesting potential targets for antiviral therapy.

Usage: Immunofluorescence: cells were fixed in PBS solution containing 4% formaldehyde, permeabilized with 0.2% saporin (PR-01) along with a mixture of 5% BSA and 10% FCS

Related Products: Saporin (Cat. #PR-01)

Sun Y, Wu X, Li J, Radiom M, Mezzenga R, Verma CS, Yu J, Miserez A (2024) Phase-separating peptide coacervates with programmable material properties for universal intracellular delivery of macromolecules. Nat Commun 15(1):10094. doi: 10.1038/s41467-024-54463-z PMID: 39572548

Objective: To systematically manipulate the sequence of Phase-separating peptides (PSPs) to unravel the relationships between their molecular structure, the physical properties of the resulting coacervate microdroplets (CMs), and their delivery efficacy.

Summary: A few amino acid alterations are sufficient to modulate the viscoelastic properties of CMs towards either a gel-like or a liquid-like state as well as their binding interaction with cellular membranes, collectively enabling to tune the kinetics of intracellular cargo release. The authors also demonstrated that the optimized PSPs CMs display excellent transfection efficiency in hard-to-transfect cells such as primary fibroblasts and immune cells.

Usage: The cytotoxicity of the saporin-loaded (at various concentrations) or pristine CMs were evaluated using the Cell Counting Kit-8 (CCK-8).

Related Products: Saporin (Cat. #PR-01)

Kuroda M, Komatsu N, Kosai A, Hamakubo T, Abe T (2025) Anti-EGFR antibody immunotoxins improve cytotoxic effects in the salivary gland cancer A253 cell line. 37(3):450-454. doi: 10.1016/j.ajoms.2024.11.003

Objective: To confirm the antitumor effects of IT-Cetuximab (IT-Cmab= saporin-conjugated anti-EGFR antibody), which is cetuximab conjugated with a toxin, targeting salivary gland cancers—a type of cancer with limited effective treatment options aside from surgery.

Summary: Cmab alone exhibited no cytotoxic effects, but IT-Cmab demonstrated concentration-dependent cytotoxic effects in A253 cells.

Usage: Cytotoxicity assay (@1.34pM to 4.2nM)

Related Products: Saporin (Cat. #PR-01)

Mohammadi F, Zahraee H, Zibadi F, Khoshbin Z, Ramezani M, Alibolandi M, Abnous K, Taghdisi SM (2024) Progressive cancer targeting by programmable aptamer-tethered nanostructures. MedComm (2020) 5(11):e775. doi: 10.1002/mco2.775 PMID: 39434968

Objective: This review focuses on the significance of different aptamer-assembled nanoconstructs as multifunctional nucleic acid oligomeric nanoskeletons in efficient drug delivery.

Summary: Saporin was attached to a βCD-conjugated aptamer. After treating HeLa cells with the circular bivalent aptamer (Cb-Apt)‒saporin complex, cell viability decreased by 20%, whereas mono-apt‒saporin showed no significant toxicity. The Cb-Apt‒βCD complex effectively improved the intracellular delivery of saporin.

Usage: 1:50 molar ratio (nanostructure:saporin).

Related Products: Saporin (Cat. #PR-01)

Morrison G, Henry N, Kopytynski M, Chen R (2024) A bioinspired pseudopeptide-based intracellular delivery platform enhances the cytotoxicity of a ribosome-inactivating protein through multiple death pathways. Biomater Sci 12(19):5010-5022. doi: 10.1039/d4bm00600c PMID: 39177215

Objective: To overcome Saporin’s poor plasma membrane permeability.

Summary: To overcome this barrier, authors used a bioinspired intracellular delivery platform based on the pH-responsive pseudo peptide, poly (L-lysine isophthalamide) grafted with L-phenylalanine at a stoichiometric molar percentage of 50% (PP50). PP50 was co-incubated with saporin (PP50/saporin) in a mildly acidic pH environment to aid intracellular delivery and increase saporin’s therapeutic potential. It was shown that PP50 is a potential intracellular delivery platform for the internalization of protein therapeutic.

Usage: PP50/saporin formulations were prepared with D-PBS solutions at pH 6.5 containing PP50 at a specific concentration of 0.025, 0.1, 0.2, 0.5 or 5 mg mL−1 and Saporin (PR-01) at varying concentrations.

Related Products: Saporin (Cat. #PR-01)

Rosado M, Mahamed I, Garcia-Sampedro A, MacRoberts S, Selbo P, Pereira S, Acedo P (2024) Enhancing pancreatic cancer chemotherapy through photochemical internalisation. Cancer Res 84 (17_Supplement_2):A027. doi: 10.1158/1538-7445.PANCREATIC24-A027

Objective: The aim is to use the technique called Photochemical Internalisation (PCI), a light-triggered intracellular drug delivery method which combines low dose PhotodynamicTherapy (PDT) with chemotherapy, to induce efficient cytosolic delivery of therapeutic compounds to their specific subcellular targets.

Summary: Observation of minimal cytotoxicity induced by saporin, gemcitabine or TPPS2a+ light monotherapies. However, PCI synergistically enhanced saporin and gemcitabine cytotoxicity (p<0.001) using very low concentrations in all tumor models. Findings demonstrate the potential of PCI to enhance the efficacy of cancer chemotherapy for pancreatic cancer using lower doses than in monotherapy and open a new window for future translational studies.

Usage: Saporin was used as monotherapy or in combination with a light-activated photosensitizer.

Related Products: Saporin (Cat. #PR-01)