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815 Development of Non Integrating Foamy Vectors for Gene Therapy Molecular Therapy Volume 17, Supplement 1, May 2009 Copyright © The American Society of Gene Therapy S312 RNA VIRUS VECTORS III the ge[.]

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Molecular Therapy Volume 17, Supplement 1, May 2009 Copyright © The American Society of Gene Therapy S312

RNA VIRUS VECTORS III

the gene transfer effi ciency to actively dividing cells, in particular

when vectors were applied, and 2) Overall gene delivery effi ciency

could be highly over-estimated, depending on post-transfection (or

transduction) time periods These are crucial questions needed to be

addressed for in vitro and in vivo gene delivery, but to quantitatively

understand and compare various vector systems cannot be achieved by

experiments alone In this study, cells were cultured to form colonies

where only the cells in periphery actively spread and proliferate A

computer-simulated stochastic cell growth model was utilized in order

to fi t to the gene expression rates collected at various post-tranfection

(or transduction) time points, and then the specifi c gene transfer rates

to actively dividing and non-dividing cells at the time of transfection

(or transduction) were determined The results indicated: 1) There

was a signifi cant difference in the apparent gene transfer effi ciency,

(e.g., 82, 56 and 40% using HEK 293 cells and VSV-G pseudotyped

MoMLV vectors) 24h after transduction, depending on the ratio of

actively-dividing vs non-dividing cells and time of transduction, 2)

The true values of viral transduction rates are relatively consistent

(e.g., approx 75 and 0% transduction rates to actively dividing and

non-dividing cells over the course of 2h exposure) This means that

gene transfer effi ciency based on the number of gene expressing cells

varies up to several folds with post-transfection (or transduction)

time as well as ratio of actively dividing vs non-dividing cells

More extended examples, including transfection rates to various

types of actively dividing and non-dividing cells by different kinds

of gene delivery vectors (e.g., lentiviral and non-viral gene delivery

to actively-dividing vs non-dividing cancer cells) will be presented

Implications of the fi ndings for in vivo gene delivery will also be

discussed

Therapy Vectors for the Treatment of Cystic

Fibrosis

Anna R Kwilas,1,3 Mark A Yednak,3 Liquin Zhang,4 Peter L

Collins,5 Raymond J Pickles,4 Mark E Peeples.2,3

1 Integrated Biomedical Science Graduate Program, The Ohio

State University, Columbus, OH; 2 Department of Pediatrics,

The Ohio State University, Columbus, OH; 3 Center for Vaccines

and Immunity, The Research Institute at Nationwide Children’s

Hospital, Columbus, OH; 4 Cystic Fibrosis/Pulmonary Research

and Treatment Center, University of North Carolina at Chapel Hill,

Chapel Hill, NC; 5 Laboratory of Infectious Diseases, NIAID, NIH,

Bethesda, MD.

Cystic fi brosis (CF) is the most common lethal recessive genetic

disease in the Caucasian population It is caused by any of a number

of mutations in the CF transmembrane conductance regulator (CFTR)

gene A mutation in the CFTR gene, leading to the production of a

partially or completely non-functional protein, results in dehydration

of mucosal surfaces and an inability to remove pathogens from

the respiratory tract leading to morbidity and mortality in the CF

population Since CFTR was fi rst cloned in 1989 a major goal of CF

research has been to develop an effective gene therapy for this disease

Respiratory syncytial virus (RSV) naturally infects the ciliated cells that line the respiratory tract, the same cells that express CFTR

In addition, although RSV does induce an immune response, this response does not prevent subsequent infection suggesting that an RSV-based vector might be effectively readministered, a requirement since the apical ciliated cells do not divide We have inserted the large (4.5 kb) CFTR gene into four sites in the recombinant, green

fl uorescent protein-expressing (rg)RSV genome to generate virus expressing increasing amounts of the CFTR protein Two of these rgRSV-CFTR viruses were capable of expressing CFTR The inclusion of the CFTR gene in the (rg)RSV genome did cause a delay

in the growth of the viruses, however this was overcome by 72 hours post infection The CFTR expressed by the rgRSV-CFTR viruses was functional in primary human airway epithelial cultures derived from

CF patients and infection with these viruses resulted in a minimum of 30% of the normal chloride channel function seen in non-CF primary human airway epithelial cultures Unfortunately, ciliated airway cells infected with RSV die within 5 days post infection To create an improved RSV-based vector we have generated an RSV “replicon”

by removing the three glycoprotein genes from a full-length RSV cDNA The replicon is able to replicate in cells without killing them

or producing infectious virus, allowing the isolation and expansion

of replicon-containing cells Providing the viral glycoproteins in trans enables the production of “one-step virus” (OSV) which is

capable of delivering a replicon to fresh cells where it produces its encoded proteins, but cannot spread to additional cells We inserted the CFTR gene into the RSV replicon genome in four positions, all four of which produced the CFTR protein When CFTR-expressing replicon OSV were used to infect primary human airway epithelial cultures, replicon containing cells remained within the cultures for 12-20 days, indicating that replicon containing cells have a survival advantage over those infected with the complete virus

Vectors for Gene Therapy

David R Deyle,1 Yi Li,1 David W Russell.1

1 Department of Medicine, Division of Hematology, University of Washington, Seattle, WA.

Foamy virus (FV) is a retrovirus that has been developed for gene therapy because it has not been associated with disease, is able to infect many different hosts and tissue types, and has the largest genome of all retroviruses After infection, FVs can stably integrate into the host DNA and facilitate effi cient transgene expression However, integration of exogenous DNA into the genome can cause insertional mutagenesis To avoid the issues of insertional mutagenesis, previous attempts have been made to create a functional non-integrating foamy virus (NIFV) vector similar to integrase-defi cient lentiviral vectors However, these efforts have been unsuccessful To further investigate this problem, we constructed NIFV vectors by introducing mutations in the highly conserved DD35E catalytic core motif of the

FV integrase gene Three independent vectors stocks containing the expression cassette MSCV-GFP were generated for two single mutant NIFV vectors packaged with point mutations D131V or D188A, a double mutant NIFV vector packaged with both D131V and D188A mutations, and an integrase-profi cient FV vector Genome titers were determined by Southern blot analysis and all titers ranged from 8 x 10^8 to 3 x 10^10 genomes/ml, showing that NIFV vector stocks were comparable to the integrase profi cient FV vector stocks All three NIFV vectors and the integrase-profi cient FV vector expressed GFP in human fi broblasts and HT1080 cells two days after infection Unlike integrase profi cient FV vectors that showed stable GFP expression,

fi broblasts and HT1080 cells transduced with NIFV vectors had a decreasing percent of GFP+ cells over a 10 day period, refl ecting

a lack of integration and dilution over time in the proliferating culture We also generated NIFV and integrase-profi cient FV vectors

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Molecular Therapy Volume 17, Supplement 1, May 2009

PRECLINICAL AND CLINICAL APPLICATIONS OF AAV

containing a CMV-nuclear localized lacZ-PGK-Neo-Ori (CnZPNO)

cassette and transduced fi broblasts Again, all three NIFV vectors and

the integrase-profi cient FV vector expressed the transgene, nuclear

localized lacZ, as evidenced by the presence of

beta-galactosidase-positive foci In addition, after selecting infected fi broblasts with

G418, we found that the NIFV vectors integrated at a frequency

several logs lower than integrase-profi cient FV vectors NIFV

vector-chromosome integration junctions from G418 resistant fi broblast

clones will be sequenced to determine the mechanism of

integrase-independent vector insertion Since non-integrating viral genomes

are known to exist in various forms, including linear, one-LTR or

two-LTR circles, we are currently utilizing Southern blot analysis to

identify the predominate DNA species Our NIFV vector would be

especially advantageous for those applications in which short-term

gene expression is required, such as expressing a factor to infl uence

development, inducing a cellular phenotype, or expressing a genomic

modifying protein (e.g Cre recombinase) Also, NIFV vectors may be

useful for targeted gene repair In summary, our novel NIFV system

expresses transgenes, infects different cell types, has applications

for gene therapy, and most importantly, does not integrate, greatly

reducing the risk of genotoxicity

Preclinical and Clinical Applications of AAV

Their Responsiveness to Hepatic AAV Gene

Transfer

Hua Li,1 Katherine High,2 Hildegund C J Ertl.1

1 Immunology Program, The Wistar Institute, Philadelphia, PA;

2 Children’s Hospital of Philadelphia, Philadelphia, PA.

Hepatic adeno-associated virus (AAV)-serotype 2-mediated

gene transfer results in sustained transgene product expression in

experimental animals but not in human subjects We hypothesized

that loss of transgene product expression in humans might be caused

by immune memory mechanisms that become reactivated upon

AAV vector transfer We tested the effect of hepatic AAV2-hF.IX or

AAV8-hF.IX gene transfer on AAV capsid-specifi c CD8+ T cells in

mice AAV capsid-specifi c CD8+ T cells were found to proliferate in

response to hepatic AAV gene transfer indicating that degradation of

the AAV particles triggered a recall response The kinetics of the recall

response analyzed by adoptive transfer of CD8+ T cells into mice that

had received AAV-2hF.IX or AAV-8hF.IX vectors previously showed

differences in the degradation rates of AAV-2 and AAV-8 vectors

Other functional properties of AAV capsid-specifi c CD8+ T cells

were analyzed and the most remarkable fi nding was that in mice AAV

capsid-specifi c CD8+ T cells require a rather high concentration of

their cognate antigen in order to exhibit lysis The implication of these

fi ndings on the potential role of AAV capsid-specifi c CD8+ T cells in

limiting hepatic AAV gene transfer in humans will be discussed

Mutant Alpha One Antitrypsin Using Recombinant

AAV Delivered shRNA

Christian Mueller,1 Qiushi Tang,1 Brian O’Sullivan Murphy,1 Sofi a

Braag,1 Terence R Flotte.1

1 UMass Gene Therapy Center, UMass Medical School, Worcester,

MA.

Alpha-1 antitrypsin (AAT) defi ciency is one of the most common

genetic diseases in North America, with a carrier frequency of

approximately 4% in the US population Homozygosity for the most

common mutation caused by a single base pair change (Glu342Lys,

PI*Z) leads to the synthesis of a mutant protein, which accumulates

and polymerizes within hepatocytes rather than being effi ciently

secreted This lack of secretion causes severe serum defi ciency

predisposing patients to chronic lung disease 12 to 15% of patients with PI*ZZ also develop liver disease, which can be severe, even in infancy This is thought to be due to toxic effects of the accumulated mutant Z-AAT within the hepatocyte Thus, an approach to reduce AAT-defi cient liver disease will likely require some mechanism to decrease the amount of Z-AAT within hepatocytes Here we describe studies of allele specifi c small interfering RNAs (siRNAs) designed to down regulate PI*Z specifi c AAT within hepatocytes Two different siRNA sequences were identifi ed and cloned into a recombinant adeno-associated virus (rAAV) backbone as U6 driven shRNA, one with the single base pair change at position 10 (p10) and one with the change at position 16 (p16) of the targeting siRNA molecule Each construct was able to reduce Z-AAT levels, but experiments

on wildtype PiM AAT expressing cell culture models showed the greatest PiZ specifi c reduction with p10, whereas the p16 construct also signifi cantly down regulated wildtype AAT The rAAV-U6p10 was then packaged into AAV8 capsids and used in vivo to transduce the livers of human Z-AAT over-expressing transgenic mice These studies show a decrease in total human AAT after 2 weeks, and a clearing of Z-AAT accumulation by immunohistochemistry in the livers The rAAV8-U6-p10 vector may hold promise as a potential therapy for patients with AAT liver disease

Delivery by Adeno-Associated Virus Vectors Carrying Large Genomes in Hemophilia Mouse and Dog Models

Junjiang Sun,1 Paul E Monahan,1 R Jude Samulski,1 Clinton D Lothrop, Jr 2

1 Gene Therapy Center, University of North Carolina at Chapel Hill, Chapel Hill, NC; 2 Biochemistry and Molecular Genetics, School of Medicine, University of Alabama, Birmingham, AL.

The use of adeno-associated virus (AAV) vectors for correction of many clinically relevant congenital defi ciencies has been hampered by the relatively small size of the AAV genome (4680 nt) and ineffi cient AAV vector delivery of genes that are larger than the wild type (wt) size We previously demonstrated in vitro that proteasome inhibitor (PI) treatment concurrent with AAV delivery improves transduction using larger than wt expression cassettes that exceed the size of the wtAAV genome We have extended these studies using AAV2 or 8 vectors carrying a 5.6 kb factor VIII cassette in hemophilia A mice treated with or without proteasome inhibitor PI enhancement of expression was observed that was increased on average 6-fold (AAV2) and 3-fold (AAV8); enhanced expression persisted throughout the

1 year of observation In addition, a limiting dose of 1 x 1013 vg/kg AAV8.canine FVIII was delivered via portal vein to two hemophilia

A dogs after receiving PI I.V.; two hemophilic dogs received vector without PI No toxicity was observed; specifi cally, there were no abnormalities of liver transaminases, blood platelet, white blood cell

or other cell counts, or development of FVIII inhibitory antibodies The Whole Blood Clotting Time (WBCT), which is normally prolonged to greater than 20 minutes in hemophilic dogs, corrected

to the normal range (6-10 minutes) by the fi rst timepoint at one week

in the dogs receiving PI Over one year after vector delivery dogs receiving AAV8cFVIII alone had a mean WBCT of 13.6 minutes, and experienced 9 bleeding episodes apiece, a bleeding rate not different from untreated hemophilic dogs followed in parallel Dogs receiving vector with PI had a mean WBCT of 9.0 minutes, and correction of the hemophilic phenotype was evidenced by zero bleeding episodes Because male gender may be associated with higher hepatic expression from AAV vectors, a second litter of dogs was subsequently treated with two females receiving AAV + PI and one male receiving vector alone After fi ve months follow-up, the PI-treated females show the same pattern of improved hemostatic correction The fi rst litter has now been followed for 27 months remaining asymptomatic with

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