Streptavidin-ZAP References

Cat #IT-27


Castiello MC, Bosticardo M, Sacchetti N, Calzoni E, Fontana E, Yamazaki Y, Draghici E, Corsino C, Bortolomai I, Sereni L, Yu HH, Uva P, Palchaudhuri R, Scadden DT, Villa A, Notarangelo LD. Efficacy and safety of anti-CD45-saporin as conditioning agent for RAG deficiency. (2021) J Allergy Clin Immunol 147(1):309-320.e6. doi: 10.1016/j.jaci.2020.04.033

Objective:  To improve multi-lineage engraftment using non-genotoxic conditioning with anti-CD45-Saporin.
Summary:  Conditioning with anti-CD45 antibody-drug conjugates may represent a novel and safe conditioning regimen for patients with RAG deficiency and other inborn errors of immunity.
Dose:  Intravenous injection of CD45-SAP (3 mg/kg).

Koeniger T, Bell L, Mifka A, Enders M, Hautmann V, Mekala SR, Kirchner P, Ekici AB, Schulz C, Wörsdörfer P, Mencl S, Kleinschnitz C, Ergün S, Kuerten S (2021) Bone marrow-derived myeloid progenitors in the leptomeninges of adult mice. Stem Cells 39(2):227-239. doi: 10.1002/stem.3311

Summary: This report confirms the presence of myeloid progenitors at the meningeal border of the brain and lays the foundation to unravel their possible functions in CNS surveillance and local immune cell production. Compared to bone marrow transfer after whole-body irradiation, chimerism developed more slowly in the CD45-SAP (biotinylated anti-CD45 mixed with Streptavidin-ZAP) model and only reached around 50% in the blood myeloid compartment 15 weeks after transplantation. Also see: Palchaudhuri et al. (2016) Non-genotoxic conditioning for hematopoietic stem cell transplantation using a hematopoietic-cell-specific internalizing immunotoxin. Nat Biotechnol 34:738-745. doi: 10.1038/nbt.3584

Penna S, Villa A, Capo V (2021) Autosomal recessive osteopetrosis: mechanisms and treatments. Dis Model Mech 14(5):dmm048940. doi: 10.1242/dmm.048940

Summary: Autosomal recessive osteopetrosis (ARO) is a severe inherited bone disease characterized by defective osteoclast resorption or differentiation. Novel therapeutic approaches are needed for ARO patients. The authors review preclinical and proof-of-concept studies, such as gene therapy, systematic administration of deficient protein, in utero Hematopoietic stem cell transplantation (HSCT) and gene editing.
Dose: Efficacy in HSCT conditioning was demonstrated with CD45.2-SAP (biotinylated Anti-CD45 mixed with Streptavidin-ZAP). In mice, CD45.2–SAP preserved normal bone marrow architecture compared to total body irradiation, which instead reduced vascular integrity and bone marrow cellularity. Mice conditioned with CD45.2–SAP rapidly recovered their peripheral myeloid cells and had a survival advantage when exposed to infections (3 mg/kg iv; Palchaudhuri et al., 2016). Additionally, conditioning with CD45.2–SAP resulted in significant chimerism after transplantation, even in a pathological mouse model (3 mg/kg iv; Castiello et al., 2021).

Wang D, Shao X, Wang Q, Pan X, Dai Y, Yao S, Yin T, Wang Z, Zhu J, Xi X, Chen Z, Chen S, Zhang G (2021) Activated factor X targeted stored in platelets as an effective gene therapy strategy for both hemophilia A and B. Clin Transl Med 11(3):e375. doi: 10.1002/ctm2.375

Summary: Treatment of hemophiliacs with inhibitors remains challenging, and new treatments are in urgent need. Coagulation factor X plays a critical role in downstream blood coagulation cascade, which could serve as a bypassing agent for hemophilia therapy. Target expression of the FXa precursor to platelets can generate a storage pool of FXa in platelet α-granules, the platelet-stored FXa is effective in treating HA and HB with inhibitors, suggesting that this could be a novel choice for hemophilia patients with inhibitors.
Dose: A single dose of CD45.2-SAP (biotinylated Anti-CD45 mixed with Streptavidin-ZAP) enabled efficient engraftment of donor cells (> 90%) and full correction of sickle-cell anemia. (3 mg/kg iv; Palchaudhuri et al., 2016).


Fischer A, Wolf I, Fuchs H, Masilamani AP, Wolf P (2020) Pseudomonas Exotoxin A Based Toxins Targeting Epidermal Growth Factor Receptor for the Treatment of Prostate Cancer. Toxins (Basel) 12(12):753. doi: 10.3390/toxins12120753

Summary: Refers to chimeric murine-human mAb cetuximab bound to Streptavidin-ZAP.  See: Yip WL, Weyergang A, Berg K, Tonnesen HH, Selbo PK (2007) Targeted Delivery and Enhanced Cytotoxicity of Cetuximab-Saporin by Photochemical Internalization in EGFR-Positive Cancer Cells. Mol Pharm 4(2):241-251.

Su Y, Zhang X, Bidlingmaier S, Behrens CR, Lee NK, Liu B (2020) ALPPL2 Is a Highly Specific and Targetable Tumor Cell Surface Antigen. Cancer Res 80(20):4552-4564. doi: 10.1101/2020.01.07.898122

Objective:  To evaluate therapeutic potential of ALPPL2 targeting.
Summary:  Exquisite tissue specificity and broad tumor type coverage suggest that ALPPL2 could be an excellent cell surface target for therapeutic development against mesothelioma.
Dose:  Biotinylated M25 IgG1 and Streptavidin-ZAP were mixed at a molar ratio of 1:1.


Abadir E, Bryant C, Larsen S, & Clark GJ. Targeting the niche: depleting haemopoietic stem cells with targeted therapy. (2019) Bone Marrow Transplant 54: 961–968. doi: 10.1038/s41409-019-0445-0

Review:  Anti-mouse CD45 ADC (clone 104-Saporin) Depletes mature lymphoid cells and HSPC, conditioning allows for high level sustained multilineage engraftment of congenic mice. Anti-mouse ADC (CD117-saporin) Combined with T cell depleting agents allowed for significant and durable engraftment in an immunocompetent mouse allo-HSCT model.

Berhani O, Glasner A, Kahlon S, Duev-Cohen A, Yamin R, Horwitz E, Enk J, Moshel O, Varvak A, Porgador A, Jonjic S, Mandelboim O.. Human anti-NKp46 antibody for studies of NKp46-dependent NK cell function and its applications for type 1 diabetes and cancer research. (2019) Eur J Immunol 49(2):228-241. doi: 10.1002/eji.201847611

Objective:  To investigate human NKp46 activity and its critical role in Natural Killer (NK) cell biology.
Summary:  A unique anti-human NKp46 monoclocal antibody was developed and conjugated to Saporin.  Targeted toxin inhibits growth of NKp46-positive cells; thus, exemplifying the potential as an immunotherapeutic drug to treat NKp46-dependent diseases, such as, type I diabetes and NK and T cell related malignancies.
Dose:  Conjugation of the antibodies to Saporin, treatment of cells, and cell viability assay Biotin-Z Kit instructions.

Czechowicz A, Palchaudhuri R, Scheck A, Hu Y, Hoggatt J, Saez B, Pang WW, Mansour MK, Tate TA, Chan YY, Walck E, Wernig G, Shizuru JA, Winau F, Scadden DT, & Rossi DJ. Selective hematopoietic stem cell ablation using CD117-antibody-drug-conjugates enables safe and effective transplantation with immunity preservation. (2019) Nat Commun 10:617. doi: 10.1038/s41467-018-08201-x

Objective:  To investigate a safe and effective method for hematopoietic stem cell transplantation.
Summary:  CD117-ADC selectively targets hematopoietic stem cells yet does not cause clinically significant side-effects.
Dose:  The CD117-ADC was prepared by combining biotinylated anti-CD117 (clone 2B8) with Streptavidin–ZAP.  A dose of 1.5 mg/kg of CD117-ADC (~12 µg Streptavidin-ZAP) optimally resulted in depletion of >99% of immunophenotypic and functional HSCs.

Gao C, Schroeder JA, Xue F, Jing W, Cai Y, Scheck A, Subramaniam S, Rao S, Weiler H, Czechowicz A, Shi Q. Nongenotoxic antibody-drug conjugate conditioning enables safe and effective platelet gene therapy of hemophilia A mice. (2019) Blood Adv 3(18):2700-2711. doi: 10.1182/bloodadvances.2019000516

Objective:  To determine whether hematopoietic cell–targeted ADC preconditioning is effective for engraftments that are genetically manipulated by 2bF8 lentivirus (2bF8LV) and whether sustained therapeutic platelet FVIII expression is attainable in platelet-specific gene therapy utilizing ADC-based preconditioning.
Summary:  The authors describe targeted nongenotoxic preconditioning for 2bF8 gene therapy utilizing  a hematopoietic cell–specific antibody-drug conjugate (ADC), which consists of saporin conjugated to CD45.2- and CD117-targeting antibodies.
Dose:  ADCs were prepared by combining biotinylated antibody with Streptavidin-ZAP.  The combination of CD45.2-ADC (3 mg/kg) plus CD117-ADC (0.5 mg/kg), with or without additional CD4-ADC (0.5 mg/kg) or CD8-ADC (0.5 mg/kg), was administered IV to 5- to 6-week-old FVIIInull/CD45.2 recipients 2 days before transplantation.

Li Z, Czechowicz A, Scheck A, Rossi DJ, & Murphy PM. Hematopoietic chimerism and donor-specific skin allograft tolerance after non-genotoxic CD117 antibody-drug-conjugate conditioning in MHC-mismatched allotransplantation. (2019) Nat Commun 10: 616. doi: 10.1038/s41467-018-08202-w

Objective:  To develop a conditioning protocol for fully MHC-mismatched bone marrow allotransplantation in mice involving transient immunosuppression and selective depletion of recipient hematopoietic stem cells.
Summary:  CD117-ADC conditioning promotes skin allograft tolerance.
Dose:  Biotinylated monoclonal antibodies directed against mouse CD117 were coupled to Streptavidin-ZAP.  Each mouse was injected with 1.5 mg/kg of ADC in a total volume of 300 mcl PBS.

Plum T. Identification of lineage-specific markers for therapeutic targeting of mast cells. (2019) PhD Dissertation, Ruperto-Carola University of Heidelberg, Germany. doi: 10.11588/heidok.00023555

Mice were injected i.v. with either 100 µg of 1:1 molar mixture of biotinylated CD63 antibody and Streptavidin-ZAP (60 µg mAb + 40 µg SAP) or with 40 µg SAP alone. All injections were performed in 200 µl PBS.

Wüstemann T, Haberkorn U, Babich J, Mier W. Targeting prostate cancer: Prostate-specific membrane antigen based diagnosis and therapy. (2019) Med Res Rev 39(1):40-69. doi: 10.1002/med.21508

Summary: Conjugation to the antibody was achieved by reacting the biotinylated antibody with Streptavidin-ZAP . Binding potency of the conjugate was comparable to that of the naked antibody and in vivo experiments proved potent and selective tumor growth inhibition in mice bearing LNCaP tumors.


Eng MS, Kaur J, Prasmickaite L, Engesaeter BO, Weyergang A, Skarpen E, Berg K, Rosenblum MG, Maelandsmo GM, Hogset A, Ferrone S, Selbo PK.  (2018) Enhanced targeting of triple-negative breast carcinoma and malignant melanoma by photochemical internalization of CSPG4-targeting immunotoxins. Photochem Photobiol Sci 17:539-551. doi: 10.1039/C7PP00358G

Summary: The combination of the drug delivery technology PCI and CSPG4-targeting immunotoxins is an efficient, specific and light-controlled strategy for the elimination of aggressive cells of TNBC and malignant melanoma origin. This study lays the foundation for further preclinical evaluation of PCI in combination with CSPG4-targeting.
Dose: To obtain the immunotoxin 225.28-saporin, Streptavidin-Saporin (Cat. #IT-27; Streptavidin-ZAP), with an average of 2.5 molecules of saporin per molecule of streptavidin, was combined with biotinylated 225.28, a CSPG4-specific mouse mAb, IgG2a.

Hoffmann RM, et al. Development and evaluation of T-Zap: a novel antibody-drug conjugate for the treatment of Her2 positive breast cancer (2018) AACR Ann Mtg 2018. 78: (13 Suppl):Abstract LB-001.

Objective:  Develop and Evaluate a novel ADC (T-Zap) for breast cancer.
Summary:  Binding to target cells of T-Zap was confirmed. Comparison of T-Zap efficacy in breast cancer cell lines with and without resistance against trastuzumab showed a trend for higher efficacy of cell killing by T-Zap in trastuzumab resistant cells compared to T-DM1. Toxicity assays revealed no impact of T-Zap on cell viability in immune cells.
Dose:  T-ZAP was made using Biotinylated monoclonal antibody tratuzumab mixed with Streptavidin-ZAP.

Kusano-Arai O, Iwanari H, Kudo S, Kikuchi C, Yui A, Akiba H, Matsusaka K, Kaneda A, Fukayama M, Tsumoto K, & Hamakubo T. Synergistic Cytotoxic Effect on Gastric Cancer Cells of an Immunotoxin Cocktail in Which Antibodies Recognize Different Epitopes on Cdh17. (2018). Monoclonal Antibodies in Immunodiagnosis and Immunotherapy, 37 (1):1-11.

Dose:  For immunotoxin preparation, Streptavidin-ZAP was mixed with biotinylated mAbs in equal molar concentrations for 30 min at room temp.
Objective:  To determine if an immunotoxin cocktail targeted to multiple epitopes has synergistic effects on low expression level cells, which would expand the applicable range of immunotoxin therapy for cancer.
Summary:  The combination of immunotoxins with different mechanisms of action in an antibody cocktail will increase cytotoxic activities and decrease side effects.  For immunotoxin preparation, Streptavidin-ZAP was mixed with biotinylated mAbs in equal molar concentrations for 30 minutes at room temperature.

Lelieveldt LPWM, Kristyanto H, Pruijn GJM, Scherer HU, Toes REM, & Bonger KM. Sequential Prodrug Strategy to Target and Eliminate ACPA-Selective Autoreactive B cells. (2018) Mol Pharm 15(12):5565-5573. doi: 10.1021/acs.molpharmaceut.8b00741

Objective: To develop a method to target and selectively eliminate autoreactive B cells using a sequential antigen prodrug targeting strategy.
Summary:  The selectivity of the antigen and the possibility to block binding toward circulation ACPA brings us a step closer to the specific elimination of autoreactive B cells for the treatment of patients with ACPA-positive RA.
Dose:  Biotinylated CCP1, CArgP1, and CCP1(CNBz) were conjugated with Streptavidin-ZAP in a 4:1 ratio to make peptide-drug conjugates.

Palchaudhuri R, Hyzy SL, Proctor JL, Adams HL, Pearse BR, Sarma G, Aslanian S, Gillard G, Lamothe TL, Burenkova O, Brooks ML, Gabros AD, McDonagh CF, Boitano AE, & Cooke MP. (2018). Antibody Drug Conjugates Targeted to CD45 or CD117 Enable Allogeneic Hematopoietic Stem Cell Transplantation in Animal Models. Paper presented at the ASH Annual Meeting, San Diego, CA.

Objective:  To further investigate and develop the utility of CD45-SAP and CD117-SAP, in combination with immunosuppression, in murine transplant models using i.v. administration in an allogeneic minor mismatch transplant model (Balb/c donor into DBA/2 recipients).
Summary:  CD45-SAP or CD117-SAP in combination with immunosuppressants (30Fll and post-transplant Cytoxan) enabled >85% peripheral donor chimerism at 12 weeks post-transplantation.  CD45-5AP and CD117-SAP were more effective at conditioning versus 2Gy TBI or pretransplant Cytoxan.
Dose:  CD45-SAP (1.9 mg/kg, iv) and CD117-SAP (1mg/kg, iv) in an allogeneic minor mismatch transplant model (Balb/c donor into DBA/2 recipients).

Su Y, Bidlingmaier S, Lee NK, Liu B (2018) Combine Phage Antibody Display Library Selection on Patient Tissue Specimens with Laser Capture Microdissection to Identify Novel Human Antibodies Targeting Clinically Relevant Tumor Antigens. Methods Mol Biol 1701:331-347. doi: 10.1007/978-1-4939-7447-4_18

Objective: To develop a technology that allows selection of phage antibody display libraries on tumor cells in situ residing in their natural tissue microenvironment.
Summary: Intracellular delivery of Immunotoxin was determined as follows: Immunotoxin was prepared by mixing biotinylated scFv with Streptavidin-ZAP (Cat. #IT-27) at a molar ratio of 1:1 and incubated on ice for 30 min. 50 μl of serially diluted immunotoxin was added to each well and incubated for 96 h at 37°C in 5% CO2. Cell growth medium were carefully removed from each well.
Dose: 100 μl of diluted CCK-8 was added to each well in the 96-well plates and incubated for 1–4 h at 37°C in 5% CO2. The absorbance was measured at 450 nm using a microtiter plate reader and the EC50 value determined using GraphPad Prism.

Tan HL, Yong C, Tan BZ, Fong WJ, Padmanabhan J, Chin A, Ding V, Lau A, Zheng L, Bi X, Yang Y, & Choo A. Conservation of Oncofetal Antigens on Human Embryonic Stem Cells Enables Discovery of Monoclonal Antibodies against Cancer. (2018). Scientific Reports, 8 (1):11608.

Objective:  To identify and characterize an antibody raised using human embryonic stem cells with potential as a cancer therapeutic.
Summary:  Antibody A19 not only binds to undifferentiated hESCs by flow cytometry, it also reacts with ovarian and breast cancer cell lines with low or no binding to normal cells.
DoseIn Vitro – Number of viable cells treated showed a decrease in cell number (Hum-ZAP mixed with A19; Streptavidin-ZAP mixed with biotinylated A19).  To determine if there were off-target effects, Hum-ZAP and chA19 were incubated with a non-binding cell line OVCAR10; no apparent cytotoxicity was observed.
In Vivo – 5 x 106 SKOV3 cells were implanted s.c. in NUDE mice and Biotinylated A19-Streptavidin-ZAP (ADC), administered ip.  The controls were free Saporin and naked A19.  By the end of 10 weeks, mice administered with the ADC saw a 60% reduction in tumor size compared to control groups.

Yuan X, Yang M, Chen X, Zhang X, Sukhadia S, Musolino N, Bao H, Chen T, Xu C, Wang Q, Santoro S, Ricklin D, Hu J, Lin R, Yang W, Li Z, Qin W, Zhao A, Scholler N, & Coukos G. Characterization of the first fully human anti-TEM1 scFv in models of solid tumor imaging and immunotoxin-based therapy. (2018). Cancer Immunol Immunother, 67 (2):329-339. 2018/01/10.

Objective: To evaluate potential applications of scFv78 as a tool for tumor molecular imaging, immunotoxin-based therapy and nanotherapy.
Summary: The data indicate that scFv78 has unique and favorable features that are advantageous for the development of imaging probes or antibody-toxin conjugates for a large spectrum of human TEM1-positive solid tumors.
Dose: Biotinylated ScFv78 was conjugated with Streptavidin-ZAP at a molar ratio of 4:1 (scFv78:ZAP).


Ha KD, Bidlingmaier SM, Su Y, Lee NK, & Liu B. Identification of Novel Macropinocytosing Human Antibodies by Phage Display and High-Content Analysis. (2017). Methods Enzymol, 585 91-110. 2017/01/23. PMID: 28109445

Streptavidin-ZAP is mixed with biotinylated IgG at a molar ratio of 1:1, vortexed, and incubated on ice for 30 min to form the immunotoxin. Serially-diluted immunotoxin (50 mcL in PBS) is added to each well and incubated for 96 h at 37°C with 5% CO2. For initial assessment, 1:10 serial dilutions are often used to find the range. For assessment of the half-maximal effective concentration (EC50), 1:3 serial dilution is used to improve accuracy.

Huang L, Yuan T, Tan M, Xi Y, Hu Y, Tao Q, Zhao Z, Zheng J, Han Y, Xu F, Luo M, Sollars PJ, Pu M, Pickard GE, So KF, & Ren C. A retinoraphe projection regulates serotonergic activity and looming-evoked defensive behaviour. (2017). Nat Commun, 8 14908. 2017/04/01. PMC5381010   

IT-27:  Streptavidin-ZAP; IT-44:  Melanopsin-SAPAB-N38:  Anti-Melanopsin
Objective:  To investigate how the dorsal raphe nucleus (DRN) and superior colliculus work in concert to extract and translate visual threats into defensive behavioural responses.
Summary:  A dedicated population of RGCs signals rapidly approaching visual threats and their input to the DRN controls a serotonergic self-gating mechanism that regulates innate defensive responses.
Dose:  Mice received bilateral intraocular injection (2 μg per eye) made between Streptavidin-Saporin and a biotinylated CTB antibody, or Anti-Melanopsin-SAP (2 μg per eye).  For detection of melanopsin, retinas were incubated for 3 days at 4 °C with anti-melanopsin (1:600).

Schiroli G, Ferrari S, Conway A, Jacob A, Capo V, Albano L, Plati T, Castiello MC, Sanvito F, Gennery AR, Bovolenta C, Palchaudhuri R, Scadden DT, Holmes MC, Villa A, Sitia G, Lombardo A, Genovese P, Naldini L. (2017) Preclinical Modeling Highlights the Therapeutic Potential of Hematopoietic Stem Cell Gene Editing for Correction of Scid-X1. Sci Transl Med 9(411)PMID: 29021165 (read summary)

Yuan X, Yang M, Chen X, Zhang X, Sukhadia S, Musolino N, Bao H, Chen T, Xu C, Wang Q, Santoro S, Ricklin D, Hu J, Lin R, Yang W, Li Z, Qin W, Zhao A. (2017) Characterization of the First Fully Human Anti-Tem1 Scfv in Models of Solid Tumor Imaging and Immunotoxin-Based Therapy. Cancer Immunol Immunother 66(3):367-378. PMID: 27933426 (Targeting Trends 17q1)


Dickey DD, Thomas GS, Dassie JP, Giangrande PH. (2016) Method for Confirming Cytoplasmic Delivery of RNA Aptamers. Methods Mol Biol 1364:209-217. PMID: 26472453 (Targeting Trends 16q1)

Palchaudhuri R, Saez B, Hoggatt J, Schajnovitz A, Sykes DB, Tate TA, Czechowicz A, Kfoury Y, Ruchika F, Rossi DJ, Verdine GL, Mansour MK, Scadden DT. (2016) Non-genotoxic conditioning for hematopoietic stem cell transplantation using a hematopoietic-cell-specific internalizing immunotoxin. Nat Biotechnol 34(7):738-745. PMID: 27272386 (Targeting Trends 16q3)

Palchaudhuri R. (2016) Targeted depletion of hematopoietic stem cells promises safer transplantation. Targeting Trends 17(3).


Damelin M, Bankovich A, Park A, Aguilar J, Anderson W, Santaguida M, Aujay M, Fong S, Khandke K, Pulito V, Ernstoff E, Escarpe P, Bernstein J, Pysz M, Zhong W, Upeslacis E, Lucas J, Lucas J, Nichols T, Loving K, Foord O, Hampl J, Stull R, Barletta F, Falahatpisheh H, Sapra P, Gerber HP, Dylla SJ. (2015) Anti-EFNA4 Calicheamicin Conjugates Effectively Target Triple-Negative Breast and Ovarian Tumor-Initiating Cells to Result in Sustained Tumor Regressions. Clin Cancer Res 21(18):4165-4173. PMID: 26015513 (Targeting Trends 15q4)

Sims S, Klenerman P. (2015) Increasing inflationary T-cell responses following transient depletion of MCMV-specific memory T cells. Eur J Immunol 45(1):113-118. (Targeting Trends 15q1)


Alonso MN, Gregorio JG, Davidson MG, Gonzalez JC, Engleman EG. (2014) Depletion of inflammatory dendritic cells with anti-CD209 conjugated to saporin toxin. Immunol Res 58(2-3):374-377. (Targeting Trends 14q3)

Bostad M, Kausberg M, Weyergang A, Olsen CE, Berg K, Hogset A, Selbo PK. (2014) Light-Triggered, Efficient Cytosolic Release of IM7-Saporin Targeting the Putative Cancer Stem Cell Marker CD44 by Photochemical Internalization. Mol Pharm 11(8):2764-2776. (Targeting Trends 14q4)

Ehrlich D, Wang B, Lu W, Dowling P, Yuan R. (2014) Intratumoral anti-HuD immunotoxin therapy for small cell lung cancer and neuroblastoma. J Hematol Oncol 7(1):91. (Targeting Trends 15q1)

Ha KD, Bidlingmaier SM, Zhang Y, Su Y, Liu B. (2014) High-content analysis of antibody phage-display library selection outputs identifies tumor selective macropinocytosis-dependent rapidly internalizing antibodies. Mol Cell Proteomics 13(12):3320-3331. (Targeting Trends 15q2)

Lund K, Bostad M, Skarpen E, Braunagel M, Krauss S, Duncan A, Hogset A, Selbo P. (2014) The novel EpCAM-targeting monoclonal antibody 3-17I linked to saporin is highly cytotoxic after photochemical internalization in breast, pancreas and colon cancer cell lines. MAbs 6(4):1038-50.(Targeting Trends 14q2)


Bostad M, Berg K, Hogset A, Skarpen E, Stenmark H, Selbo PK. (2013) Photochemical internalization (PCI) of immunotoxins targeting CD133 is specific and highly potent at femtomolar levels in cells with cancer stem cell properties. J Control Release 168(3):317-326. (Targeting Trends 13q3)

Burgos-Ojeda D, McLean K, Bai S, Pulaski H, Gong Y, Silva I, Skorecki K, Tzukerman M, Buckanovich RJ. (2013) A Novel Model for Evaluating Therapies Targeting Human Tumor Vasculature and Human Cancer Stem-like Cells. Cancer Res 73(12):3555-3565. (Targeting Trends 13q3)

Hernandez, LI, Flenker, KS, Hernandez, FJ, Klingelhutz, AJ, McNamara, JO, 2nd, & Giangrande, PH. (2013). Methods for Evaluating Cell-Specific, Cell-Internalizing Rna Aptamers. Pharmaceuticals (Basel), 6 (3):295-319. PMID: 23894227 (read summary)

Hess SM, Young EF, Miller KR, Vincent BG, Buntzman AS, Collins EJ, Frelinger JA, Hess PR. (2013) Deletion of naive T cells recognizing the minor histocompatibility antigen HY with toxin-coupled peptide-MHC class I tetramers inhibits cognate CTL responses and alters immunodominance. Transpl Immunol 29(1-4):138-145. (Targeting Trends 14q1)

Ren C, Luan L, Wui-Man Lau B, Huang X, Yang J, Zhou Y, Wu X, Gao J, Pickard GE, So KF, Pu M. (2013) Direct Retino-Raphe Projection Alters Serotonergic Tone and Affective Behavior. Neuropsychopharmacology 38(7):1163-1175. (Targeting Trends 13q2)

Stratford EW, Bostad M, Castro R, Skarpen E, Berg K, Hogset A, Myklebost O, Selbo PK. (2013) Photochemical internalization of CD133-targeting immunotoxins efficiently depletes sarcoma cells with stem-like properties and reduces tumorigenicity. Biochim Biophys Acta 1830(8):4235-4243. (Targeting Trends 13q3)


Berstad MB, Weyergang A, Berg K. (2012) Photochemical internalization (PCI) of HER2-targeted toxins: Synergy is dependent on the treatment sequence. Biochim Biophys Acta 1820(12):1849-1858. (Targeting Trends 13q1)

Rothenberg ME, Nusse Y, Kalisky T, Lee JJ, Dalerba P, Scheeren F, Lobo N, Kulkarni S, Sim S, Qian D, Beachy PA, Pasricha PJ, Quake SR, & Clarke MF. Identification of a cKit+ Colonic Crypt Base Secretory Cell That Supports Lgr5+ Stem Cells in Mice. (2012). Gastroenterology, 142 (5):1195-1205.e1196.

Summary:  cKit marks small intestinal Paneth cells and a subset of colonic goblet cells that are regulated by Notch signaling and support Lgr5 stem cells.
Dose:  For saporin experiments, small intestinal organoids with crypt buds and visible Paneth cells were passaged as single cells as described. Before embedding in Matrigel, dissociated cells were incubated for 30 minutes on ice with biotinylated-2B8 Biotinylated-2B8, 1 ug/mL, biotinylated-rat IgG 1 ug/mL, or a 1:4 molar mixture of biotinylated antibody and Streptavidin-ZAP.

Selbo PK, Weyergang A, Eng MS, Bostad M, Maelandsmo GM, Hogset A, Berg K ( 2012 ) Strongly amphiphilic photosensitizers are not substrates of the cancer stem cell marker ABCG2 and provides specific and efficient light-triggered drug delivery of an EGFR-targeted cytotoxic drug.. J Control Release  159(2):197-203 . doi: 10.1016/j.jconrel.2012.02.003

Summary: Many anti-cancer drugs are substrates of the ATP-binding cassette transporter ABCG2. Unfortunately ABCG2 is also thought to play an important role in multi-drug resistance and the protection of cancer stem cells against chemotherapeutics and photodynamic therapy. This paper examined whether photosensitizers used in photochemical internalization (PCI) are substrates for ABCG2. Streptavidin-ZAP (Cat. #IT-27) was combined with biotinylated EGF and applied to cells in culture; saporin (Cat. #PR-01) was used as a control. The data show that PCI with the EGF-saporin toxin did not utilize ABCG2 to enter cells.


Chung JS, Shiue LH, Duvic M, Pandya A, Cruz PDJ, Ariizumi K. (2011) Sezary syndrome cells overexpress syndecan-4 bearing distinct heparan sulfate moieties that suppress T-cell activation by binding DC-HIL and trapping TGF-{beta} on the cell surface. Blood 117(12):3382-3390. (Targeting Trends 11q2)

Facciabene A, Peng X, Hagemann IS, Balint K, Barchetti A, Wang L-P, Gimotty PA, Gilks CB, Lal P, Zhang L, & Coukos G. (2011) Tumour hypoxia promotes tolerance and angiogenesis via CCL28 and Treg cells. Nature, 475 226.

Yang MY, Chaudhary A, Seaman S, Dunty J, Stevens J, Elzarrad MK, Frankel AE, St Croix B (2011) The Cell Surface Structure of Tumor Endothelial Marker 8 (TEM8) is Regulated by the Actin Cytoskeleton. Biochim Biophys Acta 1813(1):39-49. (Targeting Trends 11q1)


Akiyoshi H, Chung JS, Tomihari M, Cruz PD, Jr., Ariizumi K (2010) Depleting Syndecan-4+ T Lymphocytes Using Toxin-Bearing Dendritic Cell-Associated Heparan Sulfate Proteoglycan-Dependent Integrin Ligand: A New Opportunity for Treating Activated T Cell-Driven Disease. J Immunol 184:3554-3561. (Targeting Trends 10q2)

Ariizumi K, Akiyoshi H, Chung J-S, Tomiharu M, Cruz Jr PD. (2010) Depletion of syndecan-4+ T lymphocytes by saporin-conjugated DC-HIL alleviates T cell-mediated imflammatory disease. Targeting Trends 11(2).

Berg K, Weyergang A, Prasmickaite L, Bonsted A, Hogset A, Strand MT, Wagner E, Selbo PK (2010) Photochemical internalization (PCI): a technology for drug delivery. Methods Mol Biol 635:133-145. (Targeting Trends 10q4)

Kuroda K, Liu H, Kim S, Guo M, Navarro V, Bander NH (2010) Saporin toxin-conjugated monoclonal antibody targeting prostate-specific membrane antigen has potent anticancer activity. Prostate 70(12):1286-1294. (Targeting Trends 10q4)

Vincent BG, Young EF, Buntzman AS, Stevens R, Kepler TB, Tisch RM, Frelinger JA, Hess PR (2010) Toxin-Coupled MHC Class I Tetramers Can Specifically Ablate Autoreactive CD8+ T Cells and Delay Diabetes in Nonobese Diabetic Mice. J Immunol 184(8):4196-4204. (Targeting Trends 10q2)


Hess PR, Buntzman AS, Murray SL, Young EF, Frelinger JA. (2009) Selective deletion of CD8+ T cells by saporin-coupled MHC class I tetramers. Targeting Trends 10(1).

Penaloza-MacMaster P, Masopust D, Ahmed R (2009) T-cell reconstitution without T-cell immunopathology in two models of T-cell-mediated tissue destruction. Immunology 128:164-171. (Targeting Trends 09q4)


Elson-Schwab L, Garner OB, Schuksz M, Esko JD, Tor Y (2007) Guanidinylated-Neomycin delivers large, bioactive cargo into cells through a heparan sulfate dependent pathway. J Biol Chem 282(18):13585-13591. (Targeting Trends 07q2)

Hess PR, Barnes C, Woolard MD, Johnson MD, Cullen JM, Collins EJ, Frelinger JA (2007) Selective deletion of antigen-specific CD8+ T cells by MHC class I tetramers coupled to the type I ribosome-inactivating protein saporin. Blood 109:3300-3307. (Targeting Trends 07q3)

Yip WL, Weyergang A, Berg K, Tonnesen HH, Selbo PK (2007) Targeted Delivery and Enhanced Cytotoxicity of Cetuximab-Saporin by Photochemical Internalization in EGFR-Positive Cancer Cells. Mol Pharm 4(2):241-251. (Targeting Trends 07q2)


Collins BE, Blixt O, Han S, Duong B, Li H, Nathan JK, Bovin N, Paulson JC (2006) High-affinity ligand probes of CD22 overcome the threshold set by cis ligands to allow for binding, endocytosis, and killing of B cells. J Immunol 177(5):2994-3003. (Targeting Trends 06q4)

Kohls M (2006) Evaluate Potential Targeting Molecules. Nature Methods. Published online 30 May 2006 (article).

Weyergang A, Selbo PK, Berg K (2006) Photochemically stimulated drug delivery increases the cytotoxicity and specificity of EGF-saporin. J Control Release 111(1-2):165-173. (Targeting Trends 06q2)


Blasius A, Vermi W, Krug A, Facchetti F, Cella M, Colonna M (2004) A cell-surface molecule selectively expressed on murine natural interferon-producing cells that blocks secretion of interferon-alpha. Blood 103(11):4201-4206.

Duxbury MS, Ito H, Ashley SW, Whang EE (2004) CEACAM6 as a novel target for indirect type 1 immunotoxin-based therapy in pancreatic adenocarcinoma. Biochem Biophys Res Commun 317(3):837-843. (Targeting Trends 05q3)


Sheriff ST, Xiao C, Chance WT, Kasckow JW, Balasubramaniam A (2002) Selective lesion of neuropeptide Y (NPY)-receptor neurons in hypothalamus inhibit food intake and reduces body weight in rats. Soc Neurosci Mtg, Orlando FL, Abstract #384.1.