Peptide molecules to specifically bind targets such as aptamer, avimer and kunitz domain have been intensively studied and developed as alternatives to antibodies.

□Unique Structural Scaffold , □High Affinity to Target Moleuces, □Small Molecular Weight , □Economic Production , □Versatile Application

l  Technology Platform

The core technology of Gwangju Institute of Science and Technology (GIST) is to provide novel peptide molecules namned as bipodal peptide binder (BPB). The BPB molecule having unique structural scaffold exhibits high affinity and specificity to target molecules.

Background and unmet needs: Peptide molecules to spcifically bind targets such as aptamer, avimer and kunitz domain have been intensively studied and developed as alternatives to antibodies. The peptides with high affinity to targets can be used as drugs or diagnositic agents, particulary where whole antibodies may be unsuitable. Given applibility and market potential of peptide molecules as drugs or diagnositic agents, a multitue of companies and laboratories are researching to seek peptide molecules with a novel structure.

Discovery and Achievements:  The bipodal peptide binder (BPB) of the GIST has a novel and unique structure comprising one structure stabilizing region and two target binding regions. The structure stabilizing region plays a crucial role in forming the structure of the BPB and two target binding regions cooperatively bind to two different regions of a target molecule. The biding affintiy of the BPB is determined by two target binding regions as well as the structure stabilizing region and the specificity by two target binding regions. The amino acid sequence of the target binding region can be randomly changed by a phage display technology to increase the affinity.

Key Features and Advantages:

                     (a) Unique structural scaffold

The bipodal peptide binder (BPB) has a novel and unique structural scaffold with one structure stabilizing region and two target binding regions to provide high affinity and specificity to target molecules.

 

(b) High Affinity to Target Moleuces

The BPB molecule has nM affinity to target molecules, even though its molecular weight is much smaller than whole antibody molecules. This high affinity highlights applications of the BPB molecule to drugs and diagnostic agents.

                     (c) Small Molecular Weight

The BPB molecules can be constructed using only 20-30 amino acids (2.2-4 kDa). Such small molecular weights permit to overcome shortcomings of antibodies having large molecular weights.

(d)   Economic Production

The BPB molecules having smaller molecular weights can be produced in cost-effective manners. For example, they can be chemically synthesized in conventional peptide synthesis processes.

(e)   Versatile Application

The BPB molecules can be developed as drugs and diagnostic agents (in vivo and ex vivo imaging) because they can bind to target molecules with high affinity and specificity.

 

 

Early Stage

1. Bagolkot V, Farokhzad OC, Langer R and Jon S. “Aptamer-Drug Physical Conjugate as A Novel Targeted Drug Delivery Platform”, Angew. Chem. Int. Ed., 2006; in revision.(IF: 9.60)

            2. Suh KY, Khademhosseini A, Jon S and Langer R*. “Direct Confinement of Individual Viruses within Polyethylene Glycol (PEG) Nanowells”, Nano Letter, 2006; 6, 1196-1201.(IF: 9.85)

           3. Lee H, Lee E, Kim DK, Jang NK, Jeong YY* and Jon S*. “Antibiofouling Polymer-Coated Superparamagnetic Iron Oxide Nanoparticles as Potential Magnetic Resonance Contrast Agents for In Vivo Cancer Imaging”, J. Am. Chem. Soc, 2006; 128, 7383-7389.(IF: 7.42)

           4. Farokhzad OC, Cheng J, Teply BA, Sherifi I, Jon S, Kantoff PW, Richie J and Langer R*. “Targeted nanoparticle-aptamer bioconjugates result in total tumor reduction in vivo”, PNAS, 2006; 103(16), 6315-6320.(IF: 10.45)

           5. ParkS, Chi YS, Choi IS, Seong J* and Jon S*. “A Facile Method for the Construction of Antifouling Surfaces by Self-Assembled Polymeric Monolayers of PEG-Silane Copolymers formed in Aqueous Medium”, Journal of Nanoscience and Nanotechnology, 2006; in press. (IF: 2.1)

           6. Cheng J, Teply BA, Yim CH, Jeong SY, Sherifi I, Jon S, Farokhzad OC, Khademhosseini A and Langer R*. “Magnetically Responsive Polymeric Microparticles for Oral Delivery of Protein Drugs”, Pharmaceutical Research, 2006; in press. (IF: 2.33)

            7. Kim D, Jon S, Lee HK, Baek K, Oh NK, Zin WC and Kim K*. “Anion-directed self-organization of thermotropic liquid crystalline materials containing a guanidinium moiety” Chem. Commun. 2005; 5509-5511. (IF: 4.0)

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