Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure–Activity Relationship Studies
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DOI: 10.1021/acs.jmedchem.0c01376
Abstract: Fusion of nonopioid pharmacophores, such as neurotensin, with opioid ligands represents an attractive approach for pain treatment. Herein, the μ-/δ-opioid agonist tetrapeptide H-Dmt-d-Arg-Aba-β-Ala-NH2 (KGOP01) was fused to NT(8-13) analogues. Since the NTS1 receptor has been… read more here.
Keywords: multitarget peptides; affinity; optimized opioid; peptides design ... See more keywords
Comparative Study of Chemical Stability of a PK20 Opioid–Neurotensin Hybrid Peptide and Its Analogue [Ile9]PK20—The Effect of Isomerism of a Single Amino Acid
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DOI: 10.3390/ijms231810839
Abstract: Chemical stability is one of the main problems during the discovery and development of potent drugs. When ignored, it may lead to unreliable biological and pharmacokinetics data, especially regarding the degradation of products’ possible toxicity.… read more here.
Keywords: pk20; chemical stability; opioid neurotensin; amino acid ... See more keywords