Combinatorial libraries opioid receptors

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. 

Dooley, . T., Ny, P, Bidlack, J. M., Houghten, R. A. (1998) Selective ligands for the i, S, and opioid receptors identified from a single mixture based tetrapeptide positional scanning combinatorial library. / Biol Chem 273, 18848-18856. 

Peptides and Peptidomimetics from Combinatorial Libraries. Mixture-based combinatorial peptide libraries have been extensively explored by Houghten and coworkers and have led to the identification of a variety of peptides with affinity for opioid receptors (see Ref 946 for a review). Early hexapeptide libraries, deconvoluted by binding to p opioid receptors and either iterative deconvolution (947)or positional scanning (948 see Ref 946 for a description of these deconvolution techniques), identified sequences related to the enkephalins. Other nonacetylated peptide libraries have identified more varied peptides, some that resemble opioid peptides and some that do not. Iterative deconvolution of a hexapeptide library resulted in identification of both Tyr-Pro-Phe-Gly-Phe-XNH, (X = one of 20 natural amino acids), reminiscent of the... 

Peptidomimetic ligands for opioid receptors have also been identified from combinatorial libraries. Screening of an N-(substi-tuted)glycine peptoid library for affinity for ix opioid receptors yielded novel structures (251) with high affinity for these receptors (K = 6-46 nM) (953). A library of dipeptide amides with alkyl substituents on both the interior and C-terminal amides were prepared, and high affinity agonists for all three opioid receptors identified from the library (see Ref 946). Peptide libraries can also be further modified ["libraries from libraries" (954)] to yield new potential ligands for receptors. Thus an acety-... 

Dooley, C.T., Chung, N.N., Schiller, P.W. and Houghten, R.A., Acetalins Opioid receptor antagonists determined through the use of synthetic peptide combinatorial libraries, Proc. Natl. Acad. Sci. USA, 90 (1993) 10811-10815. 

Boyce, R., Li, G., Nestler, H. P., Suenaga, T. and Still, W. C. (1994) Peptidosteroidal receptors for opioid peptides. Sequence-selective binding using a synthetic receptor library, J. Am. Chem. Soc. 116, 7955 Cheng, Y. A., Suenaga, T. and Still, W. C. (1996) Sequence-selective peptide binding with a peptido-A,B-trans-steroidal receptor selected from an encoded combinatorial receptor library, J. Am. Chem. Soc. 118, 1813-1814. 

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