Outline. Market & Technology Trends. LifeTein Technology Portfolio. LifeTein Services

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2 Outline Market & Technology Trends LifeTein Technology Portfolio LifeTein Services 2

3 Synthetic Therapeutic Peptides More than 60 synthetic therapeutic peptides under 50 amino acids in size have reached the pharmaceutical market as APIs or generics. 3

4 Chemical Optimization Drug Discovery Today Volume 15, Numbers 1/2 January 2010 Strategies for Lead Peptide Optimization 4

5 Technology Trends Microwave Synthesis Using Nitroalkanes as Acyl Anion Equivalents Green Chemistry for Synthesis 5

6 LifeTein Technology Portfolio PeptideSyn TM Platform Provides high-yield peptide synthesis Combines SPPS and LPPS for the highest synthesis success rate possible Ensures shorter turnaround 6

7 LifeTein Technology Portfolio PeptideSyn TM Ligation Synthesizes long peptides (up to 120 amino acids) Ensures high yield and short turnaround 7

8 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 8

9 LifeTein Services Custom Peptide Synthesis Service Custom Peptide Library Synthesis Service Custom Polyclonal Antibody Service Custom Monoclonal Antibody Service 9

10 LifeTein Services Advantages of PeptideSyn TM 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 10

11 Peptide Synthesis Service Peptide Length Peptide Scale amino acids From mg to kg Peptide Purity Crude, desalted, >75%, >85%, >90%, >95%, 98%, and >99% Peptide Modifications Peptide Labels Carrier Proteins Cyclic Peptides Analysis Peptide Libraries Others 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 11

12 Free Aliquot Service 12

13 Case Studies Cell Penetrating Peptides Name Origin Sequence Tat family Tat (48-60) HIV-1 protein GRKKRRQRRRPPQQ Oligoarginine Tat derivative Rn Penetralia family p-antp Antermapedia homeodomain RQIKIWFQNRRMKWKK plsl Igl-1 homeodomain RVIRVWFQNKRCKDKK Chimeric CPPs Transportan Galanin-mastoparan GWTLNSAGYLLGKINLKALAA LAKKIL 13

14 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. 14

15 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. 15

16 Peptide Antigen Design Continuous versus Discontinuous Epitopes? 16

17 Peptide Antigen Design Sequence Length Peptide Purity Peptide Solubility Difficult Amino Acids Carrier Proteins 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 Cys and Met can undergo rapid oxidation Avoid multiple Ser or Pro Avoid multiple or adjacent β-sheet forming amino acids: Glu, Iso, Leu, Phe, Thr, Tyr, Val KLH, BSA, OVA Multiple Antigenic Peptides (MAPs) 17

18 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 AdjuBooster TM Adjuvant Technology 18

19 More information, please visit 19

20 Contact Information LifeTein LLC 150 Maple Ave South Plainfield, NJ USA (Toll Free) (Fax) Let us be a partner to your growth! 20