Peptide combinatorial library libraries

MA Gallop, RW Baii et, WJ Dower, SPA Fodor, EM Gordon. Applications of combinatorial technologies to drug discovery. 1. Background and peptide combinatorial libraries. J Med Chem 37 1233-1251, 1994. 

To study the role of lysine residues in susceptibility to formalin fixation, the amino acid composition of immunoreactive peptides (to various monoclonal antibodies) was studied. Each peptide was evaluated to determine if immu-noreactivity was lost after formalin fixation. Formalin sensitivity was correlated with the peptides amino acid composition. The first step in the method is biopanning from a peptide combinatorial library with a monoclonal antibody. The peptides that bind to the antibody were tested for their sensitivity to formalin fixation. Some peptides remain immunoreactive whereas others do not. The peptides were then sequenced to look for differences between those that were sensitive to formaldehyde versus those that were not. The goal was to find whether there is a particular amino acid that is present in formalin-sensitive epitopes but absent in formalin-resistant epitopes, or vice versa. An advantage of this approach is that it is open-ended, without excluding any amino acids. 

Medynski, D. (1994). Synthetic peptide combinatorial libraries. BiojTechnology 12, 709-710. 

Dooley, C., Houghten, R. (1993) The use of positional scanning synthetic peptide combinatorial libraries for the rapid determination of opioid receptor ligands. Life Sci 52, 1509-1517. 

Bartsevich W, Juliano RL. Regulation of the MDR1 gene by transcriptional repressors selected using peptide combinatorial libraries. Mol Pharmacol 2000 58 1-10. 

Houghten, R.A., Pinilla, C Blondelle, S.E., Appel, J.R., Dooley, C.T., and Cuervo, J.H. (1991) Generation and use of synthetic peptide combinatorial libraries for basic research and drug discovery. Nature 354, 84-86. 

The repetitive nature of oligomeric synthesis has enabled the rapid implementation of solid-phase and automated methods for DNA [20,21,85,86] and peptide combinatorial libraries. Using these systems for the synthesis of single compounds or mixtures of compounds, multiple reaction vessels numbering 8 [45], 15 [80], 20 [59], 24 [50], 25 [57,58], 36 [53-55,77-79], 48 [26,39-41], or 96 [42-44] can be manipulated. Only a few of these systems enable automated resin mixing and splitting within the instrument to generate mixtures of compounds [53,59,78,87,88],... 

Applications of Combinatorial Technologies to Drug Discovery. 1. Background and Peptide Combinatorial Libraries. 

Pinilla C, Appel JR, Houghten RA, Positional scanning synthetic peptide combinatorial libraries, In Schneider CH, Eberle AN eds., Peptides 1992, ESCOM, Leiden, 1993, p. 65-66. 

Lam KS, Lake D, Salmon SE, Smith J, Chen ML, Wade S, Abdul-Latif F, Leblova Z, Ferguson RD, Krchnak Y, Sepetov NF, Lebl M, A one-bead one-peptide combinatorial library method for B-cell epitope mapping, Methods Meth. Enzymol., 9 482 -93, 1996. 

Eichler J, Houghten RA, Identification of substrate-analog trypsin inhibitors through the screening of synthetic peptide combinatorial libraries, Biochemistry, 32(41) 11035—41, 1993. 

Pinilla C, Appel J, Blondelle S, Dooley C, Domer B, Eichler J, Ostresh J, Houghten RA, A review of the utility of soluble peptide combinatorial libraries, Biopolymers, 37(3) 221-240, 1995. 

Stevenson CL, Augustijns PF, Hendren RW (1995) Peremabil-ity screen for synthetic peptide combinatorial libraries using CACO-2 cell monolayers and LC-MS/MS. Pharm Res 12 94... 

Use of Synthetic Peptide Combinatorial Libraries to Produce Glutathione Analogs... 

It is important to further develop the concept of structure-activity relationships to precisely define the structural requirements of glutathione action. Thus, this section introduces the design, synthesis, and screening of a peptide combinatorial library to obtain multiple glutathione analogs. Combinatorial libraries will be composed of mixtures of peptides (consisting of natural or noncoded amino acids) on solid support. After cleavage from the resin, the mixtures of the peptides will be screened directly in different specific assays. 

Amino Acids, Chemical Properties of Click Peptides, Design and Application of Peptide Combinatorial Libraries Solid-Phase Synthesis of Biomolecules... 

Ja WW, Roberts RW. G-protein-directed ligand discovery with peptide combinatorial libraries. Trends Biochem. Sci. 2005 30 318-324. 

Houghten RA, Dooley CT. The use of synthetic peptide combinatorial libraries for the determination of peptide ligands in radio-receptor assays opoid peptides. Bioorg. Med. Chem. Lett. 49. 1993 3 405-412. 

Eichler I, Lucka AW, Pinhla C, Houghten RA. Novel a-glucosidase inhibitors identified using multiple cyclic peptide combinatorial libraries. Mol. Diversity 1995 1 233-240. 

---