Matches in SemOpenAlex for { <https://semopenalex.org/work/W2085156914> ?p ?o ?g. }
- W2085156914 endingPage "102" @default.
- W2085156914 startingPage "86" @default.
- W2085156914 abstract "Abstract The introduction of the Dmt (2′,6′‐dimethyl‐ L ‐tyrosine)–Tic pharmacophore into the design of opioid ligands produced an extraordinary family of potent δ‐opioid receptor antagonists and heralded a new phase in opioid research. First reviewed extensively in 1998, the incorporation of Dmt into a diverse group of opioid molecules stimulated the opioid field leading to the development of unique analogues with remarkable properties. This overview will document the crucial role played by this residue in the proliferation of opioid peptides with high receptor affinity (K i equal to or less than 1 nM) and potent bioactivity. The discussion will include the metamorphosis between δ‐opioid receptor antagonists to δ‐agonists based solely on subtle structural changes at the C‐terminal region of the Dmt–Tic pharmacophore as well as their behavior in vivo. Dmt may be considered promiscuous due to the acquisition of potent μ‐agonism by dermorphin and endomorphin derivatives as well as by a unique class of opioidmimetics containing two Dmt residues separated by alkyl or pyrazinone linkers. Structural studies on the Dmt–Tic compounds were enhanced tremendously by x‐ray diffraction data for three potent and biologically diverse Dmt–Tic opioidmimetics that led to the development of pharmacophores for both δ‐opioid receptor agonists and antagonists. Molecular modeling studies of other unique Dmt opioid analogues illuminated structural differences between δ‐ and μ‐receptor ligand interactions. The future of these compounds as therapeutic applications for various medical syndromes including the control of cancer‐associated pain is only a matter of time and perseverance. © 2003 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 71:86–102, 2003" @default.
- W2085156914 created "2016-06-24" @default.
- W2085156914 creator A5011730338 @default.
- W2085156914 creator A5022567148 @default.
- W2085156914 creator A5030809281 @default.
- W2085156914 creator A5057689563 @default.
- W2085156914 creator A5091795015 @default.
- W2085156914 date "2003-01-01" @default.
- W2085156914 modified "2023-10-18" @default.
- W2085156914 title "Dmt and opioid peptides: A potent alliance" @default.
- W2085156914 cites W1551339145 @default.
- W2085156914 cites W1597233068 @default.
- W2085156914 cites W1963855581 @default.
- W2085156914 cites W1965534248 @default.
- W2085156914 cites W1965623630 @default.
- W2085156914 cites W1967487490 @default.
- W2085156914 cites W1971724091 @default.
- W2085156914 cites W1973344026 @default.
- W2085156914 cites W1974674594 @default.
- W2085156914 cites W1975262853 @default.
- W2085156914 cites W1976812888 @default.
- W2085156914 cites W1977221227 @default.
- W2085156914 cites W1977935604 @default.
- W2085156914 cites W1984619216 @default.
- W2085156914 cites W1984853842 @default.
- W2085156914 cites W1985967865 @default.
- W2085156914 cites W1986077790 @default.
- W2085156914 cites W1986098410 @default.
- W2085156914 cites W1987339118 @default.
- W2085156914 cites W1987766469 @default.
- W2085156914 cites W1988338544 @default.
- W2085156914 cites W1988625374 @default.
- W2085156914 cites W1991523383 @default.
- W2085156914 cites W1991646887 @default.
- W2085156914 cites W1994098774 @default.
- W2085156914 cites W1994104893 @default.
- W2085156914 cites W1997780054 @default.
- W2085156914 cites W1998535824 @default.
- W2085156914 cites W2002519530 @default.
- W2085156914 cites W2005310645 @default.
- W2085156914 cites W2006796554 @default.
- W2085156914 cites W2009804107 @default.
- W2085156914 cites W2010051841 @default.
- W2085156914 cites W2010173667 @default.
- W2085156914 cites W2013021248 @default.
- W2085156914 cites W2014371883 @default.
- W2085156914 cites W2014474360 @default.
- W2085156914 cites W2016703716 @default.
- W2085156914 cites W2020580775 @default.
- W2085156914 cites W2022120454 @default.
- W2085156914 cites W2022441490 @default.
- W2085156914 cites W2022932392 @default.
- W2085156914 cites W2024851283 @default.
- W2085156914 cites W2027763219 @default.
- W2085156914 cites W2031578012 @default.
- W2085156914 cites W2032062138 @default.
- W2085156914 cites W2033680879 @default.
- W2085156914 cites W2033759946 @default.
- W2085156914 cites W2037481177 @default.
- W2085156914 cites W2039210433 @default.
- W2085156914 cites W2040310294 @default.
- W2085156914 cites W2040594488 @default.
- W2085156914 cites W2041962358 @default.
- W2085156914 cites W2044761726 @default.
- W2085156914 cites W2045112376 @default.
- W2085156914 cites W2050145459 @default.
- W2085156914 cites W2053427358 @default.
- W2085156914 cites W2053603079 @default.
- W2085156914 cites W2054119130 @default.
- W2085156914 cites W2056714297 @default.
- W2085156914 cites W2057512241 @default.
- W2085156914 cites W2057516070 @default.
- W2085156914 cites W2057823189 @default.
- W2085156914 cites W2061179713 @default.
- W2085156914 cites W2063339464 @default.
- W2085156914 cites W2064601885 @default.
- W2085156914 cites W2066930335 @default.
- W2085156914 cites W2070557013 @default.
- W2085156914 cites W2082359230 @default.
- W2085156914 cites W2084282289 @default.
- W2085156914 cites W2084318337 @default.
- W2085156914 cites W2086139880 @default.
- W2085156914 cites W2086755157 @default.
- W2085156914 cites W2086791693 @default.
- W2085156914 cites W2086876254 @default.
- W2085156914 cites W2087603137 @default.
- W2085156914 cites W2088254495 @default.
- W2085156914 cites W2089462923 @default.
- W2085156914 cites W2093559862 @default.
- W2085156914 cites W2095283315 @default.
- W2085156914 cites W2102426282 @default.
- W2085156914 cites W2112288430 @default.
- W2085156914 cites W2115814542 @default.
- W2085156914 cites W2121899752 @default.
- W2085156914 cites W2126320656 @default.
- W2085156914 cites W2149571912 @default.
- W2085156914 cites W2153430658 @default.
- W2085156914 cites W2153791073 @default.