LifeTein Peptide Synthesis Service Overview

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    Outline

    Market & Technology Trends

    LifeTein Technology Portfolio

    LifeTein Services

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    Synthetic Therapeutic Peptides

    More than 60 synthetic therapeutic peptides under 50 amino acids in

    size have reached the pharmaceutical market as APIs or generics.

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    Chemical Optimization

    Strategies for Lead Peptide Optimization

    Drug Discovery Today Volume 15, Numbers 1/2 January 2010

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    Technology Trends

    Using Nitroalkanes as Acyl AnionEquivalents

    Microwave Synthesis

    Green Chemistry for Synthesis

    www.nature.com/doifinder/10.1038/nature09125

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    LifeTein Technology Portfolio

    PeptideSynTM Platform

    Provides high-yieldpeptide synthesis

    Combines SPPS andLPPS for the highestsynthesis success ratepossible

    Ensures shorterturnaround

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    LifeTein Technology Portfolio

    PeptideSynTM Ligation

    Synthesizes longpeptides (up to 120amino acids)

    Ensures high yield andshort turnaround

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    LifeTein Technology Portfolio

    A: H-MEDSTYYKASKGC-NH2

    B: H-MEDST(PTyr)YKASKGC-NH2

    C: H-PKYLQNTLKLATGMRNVPEKQTT-OH

    D: H-MEDSTYYKASKGC-NH2E: H-MEDST(PTyr)YKASKGC-NH2

    F: H-PKYLQNTLKLATGMRNVPEKQTT-OH

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    LifeTein Services

    Custom Peptide Synthesis Service

    Custom Peptide Library Synthesis Service

    Custom Polyclonal Antibody Service

    Custom Monoclonal Antibody Service

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    LifeTein Services

    Increases yields and reduces costs

    Shortens production cycle

    Combines the advantages of both solid and solution phase methods

    Can scale up projects rapidly to over 100 kg

    Avoids solubility problems for long segments in solution phase

    Advantages of PeptideSynTM Technology

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    Peptide Synthesis Service

    Peptide Length 5-120 amino acids

    Peptide Scale From mg to kg

    Peptide Purity Crude, desalted, >75%, >85%, >90%, >95%, 98%, and >99%

    Peptide

    Modifications 2-5 phosphorylation sites, methylation, acetylation, amidation, MAPs(2, 4 or 8 chains), more

    Peptide Labels FITC, Biotin, 5-FAM, Rhodamine, Dansyl, TAMRA, more

    Carrier Proteins KLH, BSA, OVA

    Cyclic Peptides Amide cyclic peptide (head to tail, side chain), 1, 2, or 3 disulfide bond bridges

    Analysis HPLC, MS, Amino Acid Analysis (AAA), solubility testing, microbial analysis, more

    Peptide Libraries Peptide sequence length of 5-20 amino acids, 48, 96 peptides

    Others Free aliquots, spacers and linkers (Ahx, mini-PEG), more

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    Free Aliquot Service

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    Case Studies

    Cell Penetrating Peptides

    Name Origin SequenceTat family

    Tat (48-60) HIV-1 protein GRKKRRQRRRPPQQOligoarginine Tat derivative Rn

    Penetralia familyp-Antp Antermapedia homeodomain RQIKIWFQNRRMKWKK

    plsl Igl-1 homeodomain RVIRVWFQNKRCKDKKChimeric CPPs

    Transportan Galanin-mastoparan GWTLNSAGYLLGKINLKALAALAKKIL

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    Case Studies

    Cell Penetrating Peptides

    Attached to a CPP, therapeutic cargo is delivered to an intracellular target,

    thus overcoming the entry restrictions set by the plasma membrane.

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    Case Studies

    Chemically synthesized peptides have free amino and carboxyl termini.

    N-terminal acetylation and C-terminal amidation reduce the overall charge of the peptide. This canincrease the stability of the peptide and its resemblance to the native protein.

    N-Terminal Acetylation and C-Terminal AmidationBoth modifications are free of charge

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    Peptide Antigen Design

    Continuous versus Discontinuous Epitopes?

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    Peptide Antigen Design

    Sequence Length 8-20 amino acids

    Peptide Purity >75% for antibody generation, >90% for phosphorylated peptide antibody (recommended)

    Peptide Solubility Keep the hydrophobic amino acid content below 50% At least one charged residue for every five amino acids

    Difficult Amino Acids Cys and Met can undergo rapid oxidation Avoid multiple Ser or Pro Avoid multiple or adjacent -sheet forming amino acids: Glu, Iso, Leu, Phe, Thr, Tyr, Val

    Carrier Proteins KLH, BSA, OVA

    Multiple Antigenic Peptides (MAPs)

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    Custom Antibody Service

    Peptide Antigen Antibody Services Polyclonal Antibodies Monoclonal Antibodies

    Phosphorylated-Peptide Antibody Services Polyclonal Antibodies Monoclonal Antibodies

    Methylated-Peptide Antibody Services Polyclonal Antibodies Monoclonal Antibodies

    AdjuBoosterTM Adjuvant Technology

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    19More information, please visit www.lifetein.com

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    Contact Information

    Let us be a partner to your growth!

    LifeTein LLC150 Maple AveSouth Plainfield, NJ 07080USA

    [email protected]

    1-732-312-5852

    1-800-655-5405 (Toll Free)

    1-732-626-6074 (Fax)