Combinatorial library approaches combining organic synthesis and molecular biology have made promising developments in the discovery of new ligands and antagonists binding to proteins that participate in dysfunction and disease. The peptide and oligonucleotide sequences, referred to as aptamers (latin= to fit) are evolved from random libraries and bind proteins such as neurotransmitter receptors and a transporter with high affinity and specificity and mimic the tertiary structure of natural agonists or antagonists. Several investigations revealed that the transduction of signals by neurotransmitter receptors, regulated by an equilibrium between open and closed channels is disturbed during dysfunction caused by drug abuse and disease. Mechanism-based strategies and future perspectives for the discovery of compounds using peptide and oligonucleotide aptamers that protect normal protein function are discussed.
Keywords: SELEX TECHNIQUE, PHAGE DISPLAY, Tenocyclidine, Phencyclidine, Lidocaine, carbamoylcholine
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