In vitro and direct in vivo testing of mixture-based combinatorial libraries for the identification of highly active and specific opiate ligands.
The use of combinatorial libraries for the identification of novel opiate and related ligands in opioid receptor assays is reviewed. Case studies involving opioid assays used to demonstrate the viability of combinatorial libraries are described. The identification of new opioid peptides composed of L-amino acids, D-amino acids, or L-, D-, and unnatural amino acids is reviewed. New opioid compounds have also been identified from peptidomimetic libraries, such as peptoids and alkylated dipeptides, and those identified from acyclic (eg, polyamine, urea) and heterocyclic (eg, bicyclic guanidine) libraries are reviewed.
Houghten
Richard A
RA
Torrey Pines Institute for Molecular Studies, 3550 General Atomics Court, San Diego, CA 92121, USA. houghten@tpims.org
Dooley
Colette T
CT
Appel
Jon R
JR
D000596:Amino Acids / Q000737:chemistry / Q000378:metabolism; D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D008024:Ligands; D009294:Narcotics / Q000737:chemistry* / Q000378:metabolism*; D010455:Peptides / Q000737:chemistry / Q000378:metabolism; D011957:Receptors, Opioid / Q000737:chemistry* / Q000378:metabolism*
D000596:Amino Acids; D008024:Ligands; D009294:Narcotics; D010455:Peptides; D011957:Receptors, Opioid