Melanocyte-inhibiting factor explained

Melanocyte-inhibiting factor (also known as Pro-Leu-Gly-NH2, Melanostatin, MSH release–inhibiting hormone or MIF-1) is an endogenous peptide fragment derived from cleavage of the hormone oxytocin, but having generally different actions in the body.[1] [2] MIF-1 produces multiple effects, both blocking the effects of opioid receptor activation,[3] [4] [5] [6] [7] [8] while at the same time acting as a positive allosteric modulator of the D2 and D4 dopamine receptor subtypes,[9] [10] [11] [12] [13] [14] [15] [16] [17] as well as inhibiting release of other neuropeptides such as alpha-MSH,[18] [19] [20] and potentiating melatonin activity.[21]

This complex mix of actions produces a profile of antidepressant,[22] [23] [24] nootropic,[25] [26] [27] [28] and anti-Parkinsonian effects when MIF-1 is administered,[29] [30] [31] and it has been investigated for various medical uses. MIF-1 is unusually resistant to metabolism in the bloodstream,[32] and crosses the blood–brain barrier easily,[33] [34] though it is poorly active orally and is usually injected. Several other closely related peptides with important actions in the body include Tyr-MIF-1 and endomorphin-1 and -2.[35] [36] [37] [38] [39]

See also

Notes and References

  1. Celis ME, Taleisnik S, Walter R . Regulation of formation and proposed structure of the factor inhibiting the release of melanocyte-stimulating hormone . Proceedings of the National Academy of Sciences of the United States of America . 68 . 7 . 1428–33 . July 1971 . 5283931 . 389210 . 10.1073/pnas.68.7.1428. 1971PNAS...68.1428C . free .
  2. Petersson M, Uvnäs-Moberg K . Prolyl-leucyl-glycinamide shares some effects with oxytocin but decreases oxytocin levels . Physiology & Behavior . 83 . 3 . 475–81 . December 2004 . 15581670 . 10.1016/j.physbeh.2004.08.034 . 42596717 .
  3. Chiu S, Mishra RK . Antagonism of morphine-induced catalepsy by L-prolyl-L-leucyl-glycinamide . European Journal of Pharmacology . 53 . 2 . 119–25 . January 1979 . 32058 . 10.1016/0014-2999(79)90156-0.
  4. Dickinson SL, Slater P . Opiate receptor antagonism by L-prolyl-L-leucyl-glycinamide, MIF-I . Peptides . 1 . 4 . 293–9 . 1980 . 6117839 . 10.1016/0196-9781(80)90006-6. 3832175 .
  5. Contreras PC, Takemori AE . Effect of prolyl-leucyl-glycinamide and alpha-melanocyte-stimulating hormone on levorphanol-induced analgesia, tolerance and dependence . Life Sciences . 34 . 26 . 2559–66 . June 1984 . 6146083 . 10.1016/0024-3205(84)90041-9.
  6. Ehrensing RH, Kastin AJ, Michell GF . Antagonism of morphine analgesia by prolyl-leucyl-glycinamide (MIF-1) in humans . Pharmacology Biochemistry and Behavior . 21 . 6 . 975–8 . December 1984 . 6151672 . 10.1016/S0091-3057(84)80083-0. 21761862 .
  7. Galina ZH, Kastin AJ . Existence of antiopiate systems as illustrated by MIF-1/Tyr-MIF-1 . Life Sciences . 39 . 23 . 2153–9 . December 1986 . 2878336 . 10.1016/0024-3205(86)90391-7.
  8. Bocheva A, Dzambazova-Maximova E . Antiopioid properties of the TYR-MIF-1 family . Methods and Findings in Experimental and Clinical Pharmacology . 26 . 9 . 673–7 . November 2004 . 15632952 . 10.1358/mf.2004.26.9.872564.
  9. Kostrzewa RM, Spirtes MA, Klara JW, Christensen CW, Kastin AJ, Joh TH . Effects of L-prolyl-L-leucyl-glycine amide (MIF-I) on dopaminergic neurons . Pharmacology Biochemistry and Behavior . 5 . Suppl 1 . 125–7 . 1976 . 13412 . 10.1016/0091-3057(76)90340-3. 28341101 .
  10. Singhal RL, Rastogi RB . MIF-1: effects on norepinephrine, dopamine and serotonin metabolism in certain discrete brain regions . Pharmacology Biochemistry and Behavior . 16 . 2 . 229–33 . February 1982 . 6122214 . 10.1016/0091-3057(82)90153-8. 44601791 .
  11. Chiu P, Rajakumar G, Chiu S, Johnson RL, Mishra RK . Mesolimbic and striatal dopamine receptor supersensitivity: prophylactic and reversal effects of L-prolyl-L-leucyl-glycinamide (PLG) . Peptides . 6 . 2 . 179–83 . 1985 . 2863809 . 10.1016/0196-9781(85)90036-1. 41473997 .
  12. Xu DL, Yu WC, Pan GB, Chen SD . Mechanism of action of L-leucyl-glycinamide and its effect on Parkinson's disease . Advances in Neurology . 45 . 587–90 . 1987 . 2881450 .
  13. Verma V, Mann A, Costain W, Pontoriero G, Castellano JM, Skoblenick K, Gupta SK, Pristupa Z, Niznik HB, Johnson RL, Nair VD, Mishra RK . Modulation of agonist binding to human dopamine receptor subtypes by L-prolyl-L-leucyl-glycinamide and a peptidomimetic analog . The Journal of Pharmacology and Experimental Therapeutics . 315 . 3 . 1228–36 . December 2005 . 16126839 . 10.1124/jpet.105.091256 . 20193713 . https://web.archive.org/web/20190227122933/http://pdfs.semanticscholar.org/8f44/e9376f1912434982484dd40a4782134dca91.pdf . dead . 2019-02-27 .
  14. Fisher A, Mann A, Verma V, Thomas N, Mishra RK, Johnson RL . Design and synthesis of photoaffinity-labeling ligands of the L-prolyl-L-leucylglycinamide binding site involved in the allosteric modulation of the dopamine receptor . Journal of Medicinal Chemistry . 49 . 1 . 307–17 . January 2006 . 16392815 . 2533518 . 10.1021/jm050644n .
  15. Vartak AP, Skoblenick K, Thomas N, Mishra RK, Johnson RL . Allosteric modulation of the dopamine receptor by conformationally constrained type VI beta-turn peptidomimetics of Pro-Leu-Gly-NH2 . Journal of Medicinal Chemistry . 50 . 26 . 6725–9 . December 2007 . 18052024 . 2529021 . 10.1021/jm070895r .
  16. Raghavan B, Skoblenick KJ, Bhagwanth S, Argintaru N, Mishra RK, Johnson RL . Allosteric modulation of the dopamine D2 receptor by Pro-Leu-Gly-NH2 peptidomimetics constrained in either a polyproline II helix or a type II beta-turn conformation . Journal of Medicinal Chemistry . 52 . 7 . 2043–51 . April 2009 . 19271750 . 2712934 . 10.1021/jm801575w .
  17. Mann A, Verma V, Basu D, Skoblenick KJ, Beyaert MG, Fisher A, Thomas N, Johnson RL, Mishra RK . Specific binding of photoaffinity-labeling peptidomimetics of Pro-Leu-Gly-NH2 to the dopamine D2L receptor: evidence for the allosteric modulation of the dopamine receptor . European Journal of Pharmacology . 641 . 2–3 . 96–101 . September 2010 . 20639138 . 10.1016/j.ejphar.2010.05.018 . 2907365.
  18. Scimonelli T, Celis ME . Inhibition by L-prolyl-L-leucyl-glycinamide (PLG) of alpha-melanocyte stimulating hormone release from hypothalamic slices . Peptides . 3 . 6 . 885–9 . 1982 . 6132363 . 10.1016/0196-9781(82)90055-9. 3880592 .
  19. McCullen RK, Peiffer RL, Jennes L, Hernandez DE . Inhibition by MIF-I of alpha-MSH induced increase of intraocular pressure and miosis in rabbits . Neuropeptides . 12 . 4 . 213–7 . 1988 . 2907121 . 10.1016/0143-4179(88)90057-1. 54378746 .
  20. Caballero C, Celis ME . The effect of the blockade of alpha-melanocyte-stimulating hormone on LH release in the rat . The Journal of Endocrinology . 137 . 2 . 197–202 . May 1993 . 8100849 . 10.1677/joe.0.1370197.
  21. Sandyk R . MIF-induced augmentation of melatonin functions: possible relevance to mechanisms of action of MIF-1 in movement disorders . The International Journal of Neuroscience . 52 . 1–2 . 59–65 . May 1990 . 1979968 . 10.3109/00207459008994244.
  22. Pignatiello MF, Olson GA, Kastin AJ, Ehrensing RH, McLean JH, Olson RD . MIF-1 is active in a chronic stress animal model of depression . Pharmacology Biochemistry and Behavior . 32 . 3 . 737–42 . March 1989 . 2568001 . 10.1016/0091-3057(89)90027-0. 27994919 .
  23. Kostowski W, Danysz W, Dyr W, Jankowska E, Krzaścik P, Pałejko W, Stefański R, Płaźnik A . MIF-1 potentiates the action of tricyclic antidepressants in an animal model of depression . Peptides . 12 . 5 . 915–8 . 1991 . 1686934 . 10.1016/0196-9781(91)90037-p. 3846846 .
  24. Ehrensing RH, Kastin AJ, Wurzlow GF, Michell GF, Mebane AH . Improvement in major depression after low subcutaneous doses of MIF-1 . Journal of Affective Disorders . 31 . 4 . 227–33 . August 1994 . 7989637 . 10.1016/0165-0327(94)90098-1.
  25. Stratton LO, Kastin AJ . Increased acquisition of a complex appetitive task after MSH and MIF . Pharmacology Biochemistry and Behavior . 3 . 5 . 901–4 . 1975 . 1801 . 10.1016/0091-3057(75)90124-0. 7471749 .
  26. Davis JL, Pico RM, Cherkin A . Memory enhancement induced in chicks by L-prolyl-L-leucyl-glycinamide . Pharmacology Biochemistry and Behavior . 17 . 5 . 893–6 . November 1982 . 6129646 . 10.1016/0091-3057(82)90467-1. 33757710 .
  27. d'Amore A, Pieretti S, Palazzesi S, Pezzini G, Chiarotti F, Scorza T, Loizzo A . MIF-1 can accelerate neuromotor, EEG and behavioral development in mice . Peptides . 11 . 3 . 527–32 . 1990 . 1974348 . 10.1016/0196-9781(90)90054-9. 29413931 .
  28. Khan RS, Yu C, Kastin AJ, He Y, Ehrensing RH, Hsuchou H, Stone KP, Pan W . Brain Activation by Peptide Pro-Leu-Gly-NH(2) (MIF-1) . International Journal of Peptides . 2010 . 1–10. 2010 . 20721355 . 2915805 . 10.1155/2010/537639 . free .
  29. Kastin AJ, Ehrensing RH, Olson RD, Coy DH . Neurological effects of MIF-1, MSH, and opiate peptides in clinical studies . International Journal of Neurology . 14 . 2–4 . 205–9 . 1980 . 6152908 .
  30. Katzenschlager R, Jackson MJ, Rose S, Stockwell K, Tayarani-Binazir KA, Zubair M, Smith LA, Jenner P, Lees AJ . Antiparkinsonian activity of L-propyl-L-leucyl-glycinamide or melanocyte-inhibiting factor in MPTP-treated common marmosets . Movement Disorders . 22 . 5 . 715–9 . April 2007 . 17373723 . 10.1002/mds.21256 . 32101673 .
  31. Castellano JM, Batrynchuk J, Dolbeare K, Verma V, Mann A, Skoblenick KJ, Johnson RL, Mishra RK . MIF-1 and its peptidomimetic analogs attenuate haloperidol-induced vacuous chewing movements and modulate apomorphine-induced rotational behavior in 6-hydroxydopamine-lesioned rats . Peptides . 28 . 10 . 2009–15 . October 2007 . 17766011 . 10.1016/j.peptides.2007.07.026 . 12114315 .
  32. Kastin AJ, Hahn K, Erchegyi J, Zadina JE, Hackler L, Palmgren M, Banks WA . Differential metabolism of Tyr-MIF-1 and MIF-1 in rat and human plasma . . 47 . 4 . 699–709 . February 1994 . 7907473 . 10.1016/0006-2952(94)90133-3.
  33. Reed GW, Olson GA, Olson RD . The Tyr-MIF-1 family of peptides . Neuroscience and Biobehavioral Reviews . 18 . 4 . 519–25 . 1994 . 7708364 . 10.1016/0149-7634(94)90005-1. 8794727 .
  34. Banks WA, Kastin AJ . Opposite direction of transport across the blood–brain barrier for Tyr-MIF-1 and MIF-1: comparison with morphine . Peptides . 15 . 1 . 23–9 . January 1994 . 7912427 . 10.1016/0196-9781(94)90165-1. 3851330 .
  35. Kastin AJ, Hahn K, Zadina JE, Banks WA, Hackler L . Melanocyte-stimulating hormone release-inhibiting factor-1 (MIF-1) can be formed from Tyr-MIF-1 in brain mitochondria but not in brain homogenate . Journal of Neurochemistry . 64 . 4 . 1855–9 . April 1995 . 7891114 . 10.1046/j.1471-4159.1995.64041855.x. 2655168 .
  36. Zadina JE, Hackler L, Ge LJ, Kastin AJ . A potent and selective endogenous agonist for the mu-opiate receptor . Nature . 386 . 6624 . 499–502 . April 1997 . 9087409 . 10.1038/386499a0 . 1997Natur.386..499Z . 4314764 .
  37. Pan W, Kastin AJ . From MIF-1 to endomorphin: the Tyr-MIF-1 family of peptides . Peptides . 28 . 12 . 2411–34 . December 2007 . 17988762 . 10.1016/j.peptides.2007.10.006 . 23173843 .
  38. Rotzinger S, Lovejoy DA, Tan LA . Behavioral effects of neuropeptides in rodent models of depression and anxiety . Peptides . 31 . 4 . 736–56 . April 2010 . 20026211 . 10.1016/j.peptides.2009.12.015 . 44705573 .
  39. Dyck B, Guest K, Sookram C, Basu D, Johnson R, Mishra RK . PAOPA, a potent analogue of Pro-Leu-glycinamide and allosteric modulator of the dopamine D2 receptor, prevents NMDA receptor antagonist (MK-801)-induced deficits in social interaction in the rat: implications for the treatment of negative symptoms in schizophrenia . Schizophrenia Research . 125 . 1 . 88–92 . January 2011 . 21036015 . 10.1016/j.schres.2010.09.025 . 3010311.

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