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Outline

Market & Technology Trends LifeTein Technology Portfolio LifeTein Services

Synthetic Therapeutic Peptides

More than 60 synthetic therapeutic peptides under 50 amino acids in size have reached the pharmaceutical market as APIs or generics.

Chemical Optimization

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

Strategies for Lead Peptide Optimization

Technology Trends

Microwave Synthesis

Using Nitroalkanes as Acyl Anion Equivalents

www.nature.com/doifinder/10.1038/nature09125

Green Chemistry for Synthesis

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LifeTein Technology Portfolio

PeptideSynTM Platform Provides high-yield peptide synthesis Combines SPPS and LPPS for the highest synthesis success rate possible Ensures shorter turnaround

LifeTein Technology Portfolio

PeptideSynTM Ligation Synthesizes long peptides (up to 120 amino acids) Ensures high yield and short turnaround

LifeTein Technology Portfolio

A: H-MEDSTYYKASKGC-NH2 B: H-MEDST(PTyr)YKASKGC-NH2 C: H-PKYLQNTLKLATGMRNVPEKQTT-OH D: H-MEDSTYYKASKGC-NH2 E: H-MEDST(PTyr)YKASKGC-NH2 F: H-PKYLQNTLKLATGMRNVPEKQTT-OH

LifeTein Services

Custom Peptide Synthesis Service Custom Peptide Library Synthesis Service Custom Polyclonal Antibody Service Custom Monoclonal Antibody Service

LifeTein Services
Advantages of PeptideSynTM Technology
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

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Peptide Synthesis Service

Peptide Length Peptide Scale Peptide Purity Peptide Modifications Peptide Labels Carrier Proteins Cyclic Peptides Analysis Peptide Libraries Others 5-120 amino acids From mg to kg Crude, desalted, >75%, >85%, >90%, >95%, 98%, and >99% 2-5 phosphorylation sites, methylation, acetylation, amidation, MAPs(2, 4 or 8 chains), more FITC, Biotin, 5-FAM, Rhodamine, Dansyl, TAMRA, more KLH, BSA, OVA Amide cyclic peptide (head to tail, side chain), 1, 2, or 3 disulfide bond bridges HPLC, MS, Amino Acid Analysis (AAA), solubility testing, microbial analysis, more Peptide sequence length of 5-20 amino acids, 48, 96 peptides 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
Tat family Tat (48-60) Oligoarginine Penetralia family p-Antp Antermapedia homeodomain RQIKIWFQNRRMKWKK HIV-1 protein Tat derivative GRKKRRQRRRPPQQ Rn

Origin

Sequence

plsl
Chimeric CPPs Transportan

Igl-1 homeodomain

RVIRVWFQNKRCKDKK

Galanin-mastoparan

GWTLNSAGYLLGKINLKALAA LAKKIL

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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
N-Terminal Acetylation and C-Terminal Amidation
Both modifications are free of charge

Chemically synthesized peptides have free amino and carboxyl termini.

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

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Peptide Antigen Design

Continuous versus Discontinuous Epitopes?

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Peptide Antigen Design

Sequence Length Peptide Purity Peptide Solubility 8-20 amino acids

>75% for antibody generation, >90% for phosphorylated peptide antibody (recommended)
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 KLH, BSA, OVA

Carrier Proteins

Multiple Antigenic Peptides (MAPs) 17

Custom Antibody Service

Polyclonal Antibodies Monoclonal Antibodies

Peptide Antigen Antibody Services

Phosphorylated-Peptide Antibody Services

Polyclonal Antibodies Monoclonal Antibodies

Methylated-Peptide Antibody Services

Polyclonal Antibodies Monoclonal Antibodies

AdjuBoosterTM Adjuvant Technology 18

More information, please visit www.lifetein.com

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Contact Information

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info@lifetein.com 1-732-312-5852 1-800-655-5405 (Toll Free) 1-732-626-6074 (Fax)

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