WANG HANLU2015 9 6

Advance in research of aptamers and related drugs

Aptamer

Aptamers are oligonucleotides such as RNA and single-strand deoxyribonucleic acid (ssDNA) or peptide molecules that can bind to their targets with high affinity and specificity due to their specific three-dimensional structures

Advantages of aptamers

Aptamers are produced chemically in a readily scalable process Chemical production process is not prone to viral or bacterial

contamination Non-immunogenic Smaller size allows more efficient entry into biological

compartments

The annual trends in the number of publications of aptamers-related research The term ldquoaptamerrdquo has been utilized for literature search on Thomson Reuters Web of Science

Aptamers in research

ELLINGTON AD SZOSTAK JW In vitro selection of RNA molecules that bind specific ligands［ J] Nature 1990 346（ 6287） 818－ 822TUERK CGOLD L Systematic evolution of ligands by exponential enrichment RNA ligands to bacteriophage-T4 DNA polymerase［ J] Science1990 249（ 4968） 505－ 510

SELEX (Systematic evolution of ligands by exponential enrichment)bull First reported by both Goldrsquos group and Szostakrsquos group in 1990

bull SELEX experiment a random sequence oligonucleotide library is synthesized that spans 20ndash100 residues in length and each nucleotide is flanked by constant sequences

bull The pool will frequently contain between 1 times 1013 to 1 times1015

members

Aptamer discovery process

Song K M Aptamers and their biological applications Sensors (Basel)12 612-31(2012)

Various application fields of aptamers

Aptamers in the Clinical Pipeline

JELLINEK DGREEN LSBELL Cet al Inhibition of receptor-binding by high-affinity RNA ligands to vascular endothelial growth-factor[J] Biochemistry199433 ( 34 ) 10450 - 10456 RUCKMAN JGREEN LSBEESON Jet al 2-fluoropyrimi- dine RNA-based aptamers to the 165-amino acid form of vascular endothelial growth factor ( VEGF ( 165 ) ) -inhibition of receptor binding and VEGF-induced vascular permeability through interac- tions requiring the exon 7-encoded domain[J] J Biol Chem 1998273( 32) 20556 - 20567DlsquoAMICO DJMASONSON HNPATEL Met al Pegaptanib sodium for neovascular age-related macular degeneration-Two-year safety results of the two prospective multicenter controlled clinical trials[J] Ophthalmology2006113( 6) 992 - 1001

Pegaptanibmdashmdashanti-VEGF aptamer

Schematic representation of the design of the activatable aptamers probe (AAP)

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Aptamer-mediated drug delivery

Omid C Farokhzad Jianjun Cheng1113142 Benjamin A Teply et al Targeted nanoparticle-aptamer bioconjugates for cancer chemotherapy in vivo Proc Natl Acad Sci USA 2006103

Aptamer-mediated drug delivery

Problems

bull Time-consuming in selection

CE-SELEX automated screening technologybull Easy to degrade in vivo

Modified nucleoside Capping PEGlyationhellipbull How to illustrate the binding structure

NMRhellipbull Not mature for application

• Advance in research of aptamers and related drugs
• Aptamer
• Slide 3
• Slide 4
• Slide 5
• Slide 6
• Slide 7
• Slide 8
• Slide 9
• Slide 10
• Slide 11
• Slide 12
• Slide 13
• Slide 14
• Slide 15

Aptamer

Aptamers are oligonucleotides such as RNA and single-strand deoxyribonucleic acid (ssDNA) or peptide molecules that can bind to their targets with high affinity and specificity due to their specific three-dimensional structures

Advantages of aptamers

Aptamers are produced chemically in a readily scalable process Chemical production process is not prone to viral or bacterial

contamination Non-immunogenic Smaller size allows more efficient entry into biological

compartments

The annual trends in the number of publications of aptamers-related research The term ldquoaptamerrdquo has been utilized for literature search on Thomson Reuters Web of Science

Aptamers in research

ELLINGTON AD SZOSTAK JW In vitro selection of RNA molecules that bind specific ligands［ J] Nature 1990 346（ 6287） 818－ 822TUERK CGOLD L Systematic evolution of ligands by exponential enrichment RNA ligands to bacteriophage-T4 DNA polymerase［ J] Science1990 249（ 4968） 505－ 510

SELEX (Systematic evolution of ligands by exponential enrichment)bull First reported by both Goldrsquos group and Szostakrsquos group in 1990

bull SELEX experiment a random sequence oligonucleotide library is synthesized that spans 20ndash100 residues in length and each nucleotide is flanked by constant sequences

bull The pool will frequently contain between 1 times 1013 to 1 times1015

members

Aptamer discovery process

Song K M Aptamers and their biological applications Sensors (Basel)12 612-31(2012)

Various application fields of aptamers

Aptamers in the Clinical Pipeline

JELLINEK DGREEN LSBELL Cet al Inhibition of receptor-binding by high-affinity RNA ligands to vascular endothelial growth-factor[J] Biochemistry199433 ( 34 ) 10450 - 10456 RUCKMAN JGREEN LSBEESON Jet al 2-fluoropyrimi- dine RNA-based aptamers to the 165-amino acid form of vascular endothelial growth factor ( VEGF ( 165 ) ) -inhibition of receptor binding and VEGF-induced vascular permeability through interac- tions requiring the exon 7-encoded domain[J] J Biol Chem 1998273( 32) 20556 - 20567DlsquoAMICO DJMASONSON HNPATEL Met al Pegaptanib sodium for neovascular age-related macular degeneration-Two-year safety results of the two prospective multicenter controlled clinical trials[J] Ophthalmology2006113( 6) 992 - 1001

Pegaptanibmdashmdashanti-VEGF aptamer

Schematic representation of the design of the activatable aptamers probe (AAP)

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Aptamer-mediated drug delivery

Omid C Farokhzad Jianjun Cheng1113142 Benjamin A Teply et al Targeted nanoparticle-aptamer bioconjugates for cancer chemotherapy in vivo Proc Natl Acad Sci USA 2006103

Aptamer-mediated drug delivery

Problems

bull Time-consuming in selection

CE-SELEX automated screening technologybull Easy to degrade in vivo

Modified nucleoside Capping PEGlyationhellipbull How to illustrate the binding structure

NMRhellipbull Not mature for application

• Advance in research of aptamers and related drugs
• Aptamer
• Slide 3
• Slide 4
• Slide 5
• Slide 6
• Slide 7
• Slide 8
• Slide 9
• Slide 10
• Slide 11
• Slide 12
• Slide 13
• Slide 14
• Slide 15

The annual trends in the number of publications of aptamers-related research The term ldquoaptamerrdquo has been utilized for literature search on Thomson Reuters Web of Science

Aptamers in research

ELLINGTON AD SZOSTAK JW In vitro selection of RNA molecules that bind specific ligands［ J] Nature 1990 346（ 6287） 818－ 822TUERK CGOLD L Systematic evolution of ligands by exponential enrichment RNA ligands to bacteriophage-T4 DNA polymerase［ J] Science1990 249（ 4968） 505－ 510

SELEX (Systematic evolution of ligands by exponential enrichment)bull First reported by both Goldrsquos group and Szostakrsquos group in 1990

bull SELEX experiment a random sequence oligonucleotide library is synthesized that spans 20ndash100 residues in length and each nucleotide is flanked by constant sequences

bull The pool will frequently contain between 1 times 1013 to 1 times1015

members

Aptamer discovery process

Song K M Aptamers and their biological applications Sensors (Basel)12 612-31(2012)

Various application fields of aptamers

Aptamers in the Clinical Pipeline

JELLINEK DGREEN LSBELL Cet al Inhibition of receptor-binding by high-affinity RNA ligands to vascular endothelial growth-factor[J] Biochemistry199433 ( 34 ) 10450 - 10456 RUCKMAN JGREEN LSBEESON Jet al 2-fluoropyrimi- dine RNA-based aptamers to the 165-amino acid form of vascular endothelial growth factor ( VEGF ( 165 ) ) -inhibition of receptor binding and VEGF-induced vascular permeability through interac- tions requiring the exon 7-encoded domain[J] J Biol Chem 1998273( 32) 20556 - 20567DlsquoAMICO DJMASONSON HNPATEL Met al Pegaptanib sodium for neovascular age-related macular degeneration-Two-year safety results of the two prospective multicenter controlled clinical trials[J] Ophthalmology2006113( 6) 992 - 1001

Pegaptanibmdashmdashanti-VEGF aptamer

Schematic representation of the design of the activatable aptamers probe (AAP)

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Aptamer-mediated drug delivery

Omid C Farokhzad Jianjun Cheng1113142 Benjamin A Teply et al Targeted nanoparticle-aptamer bioconjugates for cancer chemotherapy in vivo Proc Natl Acad Sci USA 2006103

Aptamer-mediated drug delivery

Problems

bull Time-consuming in selection

CE-SELEX automated screening technologybull Easy to degrade in vivo

Modified nucleoside Capping PEGlyationhellipbull How to illustrate the binding structure

NMRhellipbull Not mature for application

• Advance in research of aptamers and related drugs
• Aptamer
• Slide 3
• Slide 4
• Slide 5
• Slide 6
• Slide 7
• Slide 8
• Slide 9
• Slide 10
• Slide 11
• Slide 12
• Slide 13
• Slide 14
• Slide 15

ELLINGTON AD SZOSTAK JW In vitro selection of RNA molecules that bind specific ligands［ J] Nature 1990 346（ 6287） 818－ 822TUERK CGOLD L Systematic evolution of ligands by exponential enrichment RNA ligands to bacteriophage-T4 DNA polymerase［ J] Science1990 249（ 4968） 505－ 510

SELEX (Systematic evolution of ligands by exponential enrichment)bull First reported by both Goldrsquos group and Szostakrsquos group in 1990

bull SELEX experiment a random sequence oligonucleotide library is synthesized that spans 20ndash100 residues in length and each nucleotide is flanked by constant sequences

bull The pool will frequently contain between 1 times 1013 to 1 times1015

members

Aptamer discovery process

Song K M Aptamers and their biological applications Sensors (Basel)12 612-31(2012)

Various application fields of aptamers

Aptamers in the Clinical Pipeline

JELLINEK DGREEN LSBELL Cet al Inhibition of receptor-binding by high-affinity RNA ligands to vascular endothelial growth-factor[J] Biochemistry199433 ( 34 ) 10450 - 10456 RUCKMAN JGREEN LSBEESON Jet al 2-fluoropyrimi- dine RNA-based aptamers to the 165-amino acid form of vascular endothelial growth factor ( VEGF ( 165 ) ) -inhibition of receptor binding and VEGF-induced vascular permeability through interac- tions requiring the exon 7-encoded domain[J] J Biol Chem 1998273( 32) 20556 - 20567DlsquoAMICO DJMASONSON HNPATEL Met al Pegaptanib sodium for neovascular age-related macular degeneration-Two-year safety results of the two prospective multicenter controlled clinical trials[J] Ophthalmology2006113( 6) 992 - 1001

Pegaptanibmdashmdashanti-VEGF aptamer

Schematic representation of the design of the activatable aptamers probe (AAP)

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Aptamer-mediated drug delivery

Omid C Farokhzad Jianjun Cheng1113142 Benjamin A Teply et al Targeted nanoparticle-aptamer bioconjugates for cancer chemotherapy in vivo Proc Natl Acad Sci USA 2006103

Aptamer-mediated drug delivery

Problems

bull Time-consuming in selection

CE-SELEX automated screening technologybull Easy to degrade in vivo

Modified nucleoside Capping PEGlyationhellipbull How to illustrate the binding structure

NMRhellipbull Not mature for application

• Advance in research of aptamers and related drugs
• Aptamer
• Slide 3
• Slide 4
• Slide 5
• Slide 6
• Slide 7
• Slide 8
• Slide 9
• Slide 10
• Slide 11
• Slide 12
• Slide 13
• Slide 14
• Slide 15

Aptamer discovery process

Song K M Aptamers and their biological applications Sensors (Basel)12 612-31(2012)

Various application fields of aptamers

Aptamers in the Clinical Pipeline

JELLINEK DGREEN LSBELL Cet al Inhibition of receptor-binding by high-affinity RNA ligands to vascular endothelial growth-factor[J] Biochemistry199433 ( 34 ) 10450 - 10456 RUCKMAN JGREEN LSBEESON Jet al 2-fluoropyrimi- dine RNA-based aptamers to the 165-amino acid form of vascular endothelial growth factor ( VEGF ( 165 ) ) -inhibition of receptor binding and VEGF-induced vascular permeability through interac- tions requiring the exon 7-encoded domain[J] J Biol Chem 1998273( 32) 20556 - 20567DlsquoAMICO DJMASONSON HNPATEL Met al Pegaptanib sodium for neovascular age-related macular degeneration-Two-year safety results of the two prospective multicenter controlled clinical trials[J] Ophthalmology2006113( 6) 992 - 1001

Pegaptanibmdashmdashanti-VEGF aptamer

Schematic representation of the design of the activatable aptamers probe (AAP)

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Aptamer-mediated drug delivery

Omid C Farokhzad Jianjun Cheng1113142 Benjamin A Teply et al Targeted nanoparticle-aptamer bioconjugates for cancer chemotherapy in vivo Proc Natl Acad Sci USA 2006103

Aptamer-mediated drug delivery

Problems

bull Time-consuming in selection

CE-SELEX automated screening technologybull Easy to degrade in vivo

Modified nucleoside Capping PEGlyationhellipbull How to illustrate the binding structure

NMRhellipbull Not mature for application

• Advance in research of aptamers and related drugs
• Aptamer
• Slide 3
• Slide 4
• Slide 5
• Slide 6
• Slide 7
• Slide 8
• Slide 9
• Slide 10
• Slide 11
• Slide 12
• Slide 13
• Slide 14
• Slide 15

Song K M Aptamers and their biological applications Sensors (Basel)12 612-31(2012)

Various application fields of aptamers

Aptamers in the Clinical Pipeline

JELLINEK DGREEN LSBELL Cet al Inhibition of receptor-binding by high-affinity RNA ligands to vascular endothelial growth-factor[J] Biochemistry199433 ( 34 ) 10450 - 10456 RUCKMAN JGREEN LSBEESON Jet al 2-fluoropyrimi- dine RNA-based aptamers to the 165-amino acid form of vascular endothelial growth factor ( VEGF ( 165 ) ) -inhibition of receptor binding and VEGF-induced vascular permeability through interac- tions requiring the exon 7-encoded domain[J] J Biol Chem 1998273( 32) 20556 - 20567DlsquoAMICO DJMASONSON HNPATEL Met al Pegaptanib sodium for neovascular age-related macular degeneration-Two-year safety results of the two prospective multicenter controlled clinical trials[J] Ophthalmology2006113( 6) 992 - 1001

Pegaptanibmdashmdashanti-VEGF aptamer

Schematic representation of the design of the activatable aptamers probe (AAP)

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Aptamer-mediated drug delivery

Omid C Farokhzad Jianjun Cheng1113142 Benjamin A Teply et al Targeted nanoparticle-aptamer bioconjugates for cancer chemotherapy in vivo Proc Natl Acad Sci USA 2006103

Aptamer-mediated drug delivery

Problems

bull Time-consuming in selection

CE-SELEX automated screening technologybull Easy to degrade in vivo

Modified nucleoside Capping PEGlyationhellipbull How to illustrate the binding structure

NMRhellipbull Not mature for application

• Advance in research of aptamers and related drugs
• Aptamer
• Slide 3
• Slide 4
• Slide 5
• Slide 6
• Slide 7
• Slide 8
• Slide 9
• Slide 10
• Slide 11
• Slide 12
• Slide 13
• Slide 14
• Slide 15

Aptamers in the Clinical Pipeline

JELLINEK DGREEN LSBELL Cet al Inhibition of receptor-binding by high-affinity RNA ligands to vascular endothelial growth-factor[J] Biochemistry199433 ( 34 ) 10450 - 10456 RUCKMAN JGREEN LSBEESON Jet al 2-fluoropyrimi- dine RNA-based aptamers to the 165-amino acid form of vascular endothelial growth factor ( VEGF ( 165 ) ) -inhibition of receptor binding and VEGF-induced vascular permeability through interac- tions requiring the exon 7-encoded domain[J] J Biol Chem 1998273( 32) 20556 - 20567DlsquoAMICO DJMASONSON HNPATEL Met al Pegaptanib sodium for neovascular age-related macular degeneration-Two-year safety results of the two prospective multicenter controlled clinical trials[J] Ophthalmology2006113( 6) 992 - 1001

Pegaptanibmdashmdashanti-VEGF aptamer

Schematic representation of the design of the activatable aptamers probe (AAP)

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Aptamer-mediated drug delivery

Omid C Farokhzad Jianjun Cheng1113142 Benjamin A Teply et al Targeted nanoparticle-aptamer bioconjugates for cancer chemotherapy in vivo Proc Natl Acad Sci USA 2006103

Aptamer-mediated drug delivery

Problems

bull Time-consuming in selection

CE-SELEX automated screening technologybull Easy to degrade in vivo

Modified nucleoside Capping PEGlyationhellipbull How to illustrate the binding structure

NMRhellipbull Not mature for application

• Advance in research of aptamers and related drugs
• Aptamer
• Slide 3
• Slide 4
• Slide 5
• Slide 6
• Slide 7
• Slide 8
• Slide 9
• Slide 10
• Slide 11
• Slide 12
• Slide 13
• Slide 14
• Slide 15

JELLINEK DGREEN LSBELL Cet al Inhibition of receptor-binding by high-affinity RNA ligands to vascular endothelial growth-factor[J] Biochemistry199433 ( 34 ) 10450 - 10456 RUCKMAN JGREEN LSBEESON Jet al 2-fluoropyrimi- dine RNA-based aptamers to the 165-amino acid form of vascular endothelial growth factor ( VEGF ( 165 ) ) -inhibition of receptor binding and VEGF-induced vascular permeability through interac- tions requiring the exon 7-encoded domain[J] J Biol Chem 1998273( 32) 20556 - 20567DlsquoAMICO DJMASONSON HNPATEL Met al Pegaptanib sodium for neovascular age-related macular degeneration-Two-year safety results of the two prospective multicenter controlled clinical trials[J] Ophthalmology2006113( 6) 992 - 1001

Pegaptanibmdashmdashanti-VEGF aptamer

Schematic representation of the design of the activatable aptamers probe (AAP)

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Aptamer-mediated drug delivery

Omid C Farokhzad Jianjun Cheng1113142 Benjamin A Teply et al Targeted nanoparticle-aptamer bioconjugates for cancer chemotherapy in vivo Proc Natl Acad Sci USA 2006103

Aptamer-mediated drug delivery

Problems

bull Time-consuming in selection

CE-SELEX automated screening technologybull Easy to degrade in vivo

Modified nucleoside Capping PEGlyationhellipbull How to illustrate the binding structure

NMRhellipbull Not mature for application

• Advance in research of aptamers and related drugs
• Aptamer
• Slide 3
• Slide 4
• Slide 5
• Slide 6
• Slide 7
• Slide 8
• Slide 9
• Slide 10
• Slide 11
• Slide 12
• Slide 13
• Slide 14
• Slide 15

Schematic representation of the design of the activatable aptamers probe (AAP)

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Aptamer-mediated drug delivery

Omid C Farokhzad Jianjun Cheng1113142 Benjamin A Teply et al Targeted nanoparticle-aptamer bioconjugates for cancer chemotherapy in vivo Proc Natl Acad Sci USA 2006103

Aptamer-mediated drug delivery

Problems

bull Time-consuming in selection

CE-SELEX automated screening technologybull Easy to degrade in vivo

Modified nucleoside Capping PEGlyationhellipbull How to illustrate the binding structure

NMRhellipbull Not mature for application

• Advance in research of aptamers and related drugs
• Aptamer
• Slide 3
• Slide 4
• Slide 5
• Slide 6
• Slide 7
• Slide 8
• Slide 9
• Slide 10
• Slide 11
• Slide 12
• Slide 13
• Slide 14
• Slide 15

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Aptamer-mediated drug delivery

Omid C Farokhzad Jianjun Cheng1113142 Benjamin A Teply et al Targeted nanoparticle-aptamer bioconjugates for cancer chemotherapy in vivo Proc Natl Acad Sci USA 2006103

Aptamer-mediated drug delivery

Problems

bull Time-consuming in selection

CE-SELEX automated screening technologybull Easy to degrade in vivo

Modified nucleoside Capping PEGlyationhellipbull How to illustrate the binding structure

NMRhellipbull Not mature for application

• Advance in research of aptamers and related drugs
• Aptamer
• Slide 3
• Slide 4
• Slide 5
• Slide 6
• Slide 7
• Slide 8
• Slide 9
• Slide 10
• Slide 11
• Slide 12
• Slide 13
• Slide 14
• Slide 15

Optical Molecular Imaging with Aptamer-Based Probes

Shi H He X Wang K Wu X Ye X Guo Q Tan W Qing Z Yang X Zhou B Activatable aptamer probe for contrast-enhanced in vivo cancer imaging based on cell membrane protein-triggered conformation alteration Proc Natl Acad Sci USA 2011108

Aptamer-mediated drug delivery

Omid C Farokhzad Jianjun Cheng1113142 Benjamin A Teply et al Targeted nanoparticle-aptamer bioconjugates for cancer chemotherapy in vivo Proc Natl Acad Sci USA 2006103

Aptamer-mediated drug delivery

Problems

bull Time-consuming in selection

CE-SELEX automated screening technologybull Easy to degrade in vivo

Modified nucleoside Capping PEGlyationhellipbull How to illustrate the binding structure

NMRhellipbull Not mature for application

• Advance in research of aptamers and related drugs
• Aptamer
• Slide 3
• Slide 4
• Slide 5
• Slide 6
• Slide 7
• Slide 8
• Slide 9
• Slide 10
• Slide 11
• Slide 12
• Slide 13
• Slide 14
• Slide 15

Aptamer-mediated drug delivery

Omid C Farokhzad Jianjun Cheng1113142 Benjamin A Teply et al Targeted nanoparticle-aptamer bioconjugates for cancer chemotherapy in vivo Proc Natl Acad Sci USA 2006103

Aptamer-mediated drug delivery

Problems

bull Time-consuming in selection

CE-SELEX automated screening technologybull Easy to degrade in vivo

Modified nucleoside Capping PEGlyationhellipbull How to illustrate the binding structure

NMRhellipbull Not mature for application

• Advance in research of aptamers and related drugs
• Aptamer
• Slide 3
• Slide 4
• Slide 5
• Slide 6
• Slide 7
• Slide 8
• Slide 9
• Slide 10
• Slide 11
• Slide 12
• Slide 13
• Slide 14
• Slide 15

Aptamer-mediated drug delivery

Problems

bull Time-consuming in selection

CE-SELEX automated screening technologybull Easy to degrade in vivo

Modified nucleoside Capping PEGlyationhellipbull How to illustrate the binding structure

NMRhellipbull Not mature for application

• Advance in research of aptamers and related drugs
• Aptamer
• Slide 3
• Slide 4
• Slide 5
• Slide 6
• Slide 7
• Slide 8
• Slide 9
• Slide 10
• Slide 11
• Slide 12
• Slide 13
• Slide 14
• Slide 15

Problems

bull Time-consuming in selection

CE-SELEX automated screening technologybull Easy to degrade in vivo

Modified nucleoside Capping PEGlyationhellipbull How to illustrate the binding structure

NMRhellipbull Not mature for application

• Advance in research of aptamers and related drugs
• Aptamer
• Slide 3
• Slide 4
• Slide 5
• Slide 6
• Slide 7
• Slide 8
• Slide 9
• Slide 10
• Slide 11
• Slide 12
• Slide 13
• Slide 14
• Slide 15

• Advance in research of aptamers and related drugs
• Aptamer
• Slide 3
• Slide 4
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