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Tachykinin peptides

April 12, 2024

Tachykinin peptides are one of the largest families of neuropeptides, found from amphibians to mammals. They were so named due to their ability to rapidly induce contraction of gut tissue.[2] The tachykinin family is characterized by a common C-terminal sequence, Phe-X-Gly-Leu-Met-NH2, where X is either an Aromatic or an Aliphatic amino acid. The genes that produce tachykinins encode precursor proteins called preprotachykinins, which are chopped apart into smaller peptides by posttranslational proteolytic processing. The genes also code for multiple splice forms that are made up of different sets of peptides.

Tachykinin family
Structure of the tachykinin peptide Kassinin.[1]
Identifiers
SymbolTachykinin
PfamPF02202
InterProIPR002040
SMARTTK
PROSITEPDOC00240
SCOP21myu / SCOPe / SUPFAM
OPM superfamily143
OPM protein1myu
Available protein structures:
Pfam  structures / ECOD  
PDBRCSB PDB; PDBe; PDBj
PDBsumstructure summary

Tachykinins[3][4][5] excite neurons, evoke behavioral responses, are potent vasodilators, and contract (directly or indirectly) many smooth muscles. Tachykinins are from ten to twelve residues long.

The two human tachykinin genes are called TAC1 and TAC3 for historical reasons, and are equivalent to Tac1 and Tac2 of the mouse, respectively. TAC1 encodes neurokinin A (formerly known as substance K), neuropeptide K (which has also been called neurokinin K[6]), neuropeptide gamma, and Substance P.[7] Alpha, beta, and gamma splice forms are produced; the alpha form lacks exon 6 and the gamma form lacks exon 4. All three splice forms of TAC1 produce substance P, but only the beta and gamma forms produce the other three peptides. Neuropeptide K and neuropeptide gamma are N-terminally longer versions of neurokinin A that appear to be final peptide products in some tissues.[2]

TAC3 encodes neurokinin B.[8]

The best known tachykinin is Substance P.

Receptors edit

Main article: Tachykinin receptor

There are three known mammalian tachykinin receptors termed NK1, NK2 and NK3. All are members of the 7 transmembrane g protein-coupled family of receptors and induce the activation of phospholipase C, producing inositol triphosphate. NK1, NK2 and NK3 selectively bind to substance P, neurokinin A, and neurokinin B, respectively. Whilst the receptors are not specific to any individual tachykinin, they do have differing affinity for the tachykinins:

  • NK1: SP > NKA > NKB
  • NK2: NKA > NKB > SP
  • NK3: NKB > NKA > SP

Antagonists of neurokinin-1 (NK1) receptors (NK1 receptor antagonists), through which substance P acts, have been proposed to belong to a new class of antidepressants,[9][10] while NK2 antagonists have been proposed as anxiolytics[11][12] and NK3 antagonists have been proposed as antipsychotics.[13][14]

Tachykinin peptides are also involved in inflammation, and tachykinin receptor antagonists have been researched for use in treating inflammatory conditions such as asthma and irritable bowel syndrome.[15][16][17] The main use for which these antagonist drugs have been applied so far, however, is as antiemetics, in both human and veterinary medicine.[18][19]

Examples of tachykinin antagonists include:[20]

Subfamilies edit

References edit

  1. ^ Grace RC, Lynn AM, Cowsik SM (February 2001). "Lipid induced conformation of the tachykinin peptide Kassinin". J. Biomol. Struct. Dyn. 18 (4): 611–21, 623–5. doi:10.1080/07391102.2001.10506693. PMID 11245256. S2CID 42266413.
  2. ^ a b Carter MS, Krause JE (July 1990). "Structure, expression, and some regulatory mechanisms of the rat preprotachykinin gene encoding substance P, neurokinin A, neuropeptide K, and neuropeptide gamma". J. Neurosci. 10 (7): 2203–14. doi:10.1523/JNEUROSCI.10-07-02203.1990. PMC 6570392. PMID 1695945.
  3. ^ Maggio JE (1988). "Tachykinins". Annu. Rev. Neurosci. 11: 13–28. doi:10.1146/annurev.ne.11.030188.000305. PMID 3284438.
  4. ^ Helke CJ, Krause JE, Mantyh PW, Couture R, Bannon MJ (1990). "Diversity in mammalian tachykinin peptidergic neurons: multiple peptides, receptors, and regulatory mechanisms". FASEB J. 4 (6): 1606–15. doi:10.1096/fasebj.4.6.1969374. PMID 1969374. S2CID 25935155.
  5. ^ Avanov AIa (1992). "Tachykinins and conformational aspects of their interactions with receptors". Mol. Biol. (Mosk). 26 (1): 5–24. PMID 1324401.
  6. ^ Dornan WA, Vink KL, Malen P, Short K, Struthers W, Barrett C (August 1993). "Site-specific effects of intracerebral injections of three neurokinins (neurokinin A, neurokinin K, and neurokinin gamma) on the expression of male rat sexual behavior". Physiol. Behav. 54 (2): 249–58. doi:10.1016/0031-9384(93)90107-Q. PMID 7690487. S2CID 33412235.
  7. ^ Online Mendelian Inheritance in Man (OMIM): TAC1 - 162320
  8. ^ Online Mendelian Inheritance in Man (OMIM): TAC3 - 162330
  9. ^ Alvaro G, Di Fabio R (September 2007). "Neurokinin 1 receptor antagonists--current prospects". Curr Opin Drug Discov Dev. 10 (5): 613–21. PMID 17786860.
  10. ^ Duffy RA (May 2004). "Potential therapeutic targets for neurokinin-1 receptor antagonists". Expert Opin Emerg Drugs. 9 (1): 9–21. doi:10.1517/eoed.9.1.9.32956. PMID 15155133.
  11. ^ Salomé N, Stemmelin J, Cohen C, Griebel G (April 2006). "Selective blockade of NK2 or NK3 receptors produces anxiolytic- and antidepressant-like effects in gerbils". Pharmacol. Biochem. Behav. 83 (4): 533–9. doi:10.1016/j.pbb.2006.03.013. PMID 16624395. S2CID 15134994.
  12. ^ Louis C, Stemmelin J, Boulay D, Bergis O, Cohen C, Griebel G (March 2008). "Additional evidence for anxiolytic- and antidepressant-like activities of saredutant (SR48968), an antagonist at the neurokinin-2 receptor in various rodent-models". Pharmacol. Biochem. Behav. 89 (1): 36–45. doi:10.1016/j.pbb.2007.10.020. PMID 18045668. S2CID 21490514.
  13. ^ Spooren W, Riemer C, Meltzer H (December 2005). "Opinion: NK3 receptor antagonists: the next generation of antipsychotics?". Nat Rev Drug Discov. 4 (12): 967–75. doi:10.1038/nrd1905. PMID 16341062. S2CID 13270787.
  14. ^ Chahl LA (August 2006). "Tachykinins and neuropsychiatric disorders". Curr Drug Targets. 7 (8): 993–1003. doi:10.2174/138945006778019309. PMID 16918327.
  15. ^ Groneberg DA, Harrison S, Dinh QT, Geppetti P, Fischer A (August 2006). "Tachykinins in the respiratory tract". Curr Drug Targets. 7 (8): 1005–10. doi:10.2174/138945006778019318. PMID 16918328.
  16. ^ Improta G, Broccardo M (August 2006). "Tachykinins: role in human gastrointestinal tract physiology and pathology". Curr Drug Targets. 7 (8): 1021–9. doi:10.2174/138945006778019354. PMID 16918330.
  17. ^ Boot JD, de Haas S, Tarasevych S, et al. (March 2007). "Effect of an NK1/NK2 receptor antagonist on airway responses and inflammation to allergen in asthma". Am. J. Respir. Crit. Care Med. 175 (5): 450–7. doi:10.1164/rccm.200608-1186OC. PMID 17170385. S2CID 22707433.
  18. ^ Navari RM (December 2007). "Fosaprepitant (MK-0517): a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting". Expert Opin Investig Drugs. 16 (12): 1977–85. doi:10.1517/13543784.16.12.1977. PMID 18042005. S2CID 21437603.
  19. ^ Hickman MA, Cox SR, Mahabir S, et al. (June 2008). "Safety, pharmacokinetics and use of the novel NK-1 receptor antagonist maropitant (Cerenia) for the prevention of emesis and motion sickness in cats". J. Vet. Pharmacol. Ther. 31 (3): 220–9. doi:10.1111/j.1365-2885.2008.00952.x. PMID 18471143.
  20. ^ Quartara L, Altamura M (August 2006). "Tachykinin receptors antagonists: from research to clinic". Curr Drug Targets. 7 (8): 975–92. doi:10.2174/138945006778019381. PMID 16918326.

External links edit

This article incorporates text from the public domain Pfam and InterPro: IPR002040

April 12, 2024
tachykinin, peptides, largest, families, neuropeptides, found, from, amphibians, mammals, they, were, named, their, ability, rapidly, induce, contraction, tissue, tachykinin, family, characterized, common, terminal, sequence, where, either, aromatic, aliphatic. Tachykinin peptides are one of the largest families of neuropeptides found from amphibians to mammals They were so named due to their ability to rapidly induce contraction of gut tissue 2 The tachykinin family is characterized by a common C terminal sequence Phe X Gly Leu Met NH2 where X is either an Aromatic or an Aliphatic amino acid The genes that produce tachykinins encode precursor proteins called preprotachykinins which are chopped apart into smaller peptides by posttranslational proteolytic processing The genes also code for multiple splice forms that are made up of different sets of peptides Tachykinin familyStructure of the tachykinin peptide Kassinin 1 IdentifiersSymbolTachykininPfamPF02202InterProIPR002040SMARTTKPROSITEPDOC00240SCOP21myu SCOPe SUPFAMOPM superfamily143OPM protein1myuAvailable protein structures Pfam structures ECOD PDBRCSB PDB PDBe PDBjPDBsumstructure summaryTachykinins 3 4 5 excite neurons evoke behavioral responses are potent vasodilators and contract directly or indirectly many smooth muscles Tachykinins are from ten to twelve residues long The two human tachykinin genes are called TAC1 and TAC3 for historical reasons and are equivalent to Tac1 and Tac2 of the mouse respectively TAC1 encodes neurokinin A formerly known as substance K neuropeptide K which has also been called neurokinin K 6 neuropeptide gamma and Substance P 7 Alpha beta and gamma splice forms are produced the alpha form lacks exon 6 and the gamma form lacks exon 4 All three splice forms of TAC1 produce substance P but only the beta and gamma forms produce the other three peptides Neuropeptide K and neuropeptide gamma are N terminally longer versions of neurokinin A that appear to be final peptide products in some tissues 2 TAC3 encodes neurokinin B 8 The best known tachykinin is Substance P Contents 1 Receptors 2 Subfamilies 3 References 4 External linksReceptors editMain article Tachykinin receptor There are three known mammalian tachykinin receptors termed NK1 NK2 and NK3 All are members of the 7 transmembrane g protein coupled family of receptors and induce the activation of phospholipase C producing inositol triphosphate NK1 NK2 and NK3 selectively bind to substance P neurokinin A and neurokinin B respectively Whilst the receptors are not specific to any individual tachykinin they do have differing affinity for the tachykinins NK1 SP gt NKA gt NKB NK2 NKA gt NKB gt SP NK3 NKB gt NKA gt SPAntagonists of neurokinin 1 NK1 receptors NK1 receptor antagonists through which substance P acts have been proposed to belong to a new class of antidepressants 9 10 while NK2 antagonists have been proposed as anxiolytics 11 12 and NK3 antagonists have been proposed as antipsychotics 13 14 Tachykinin peptides are also involved in inflammation and tachykinin receptor antagonists have been researched for use in treating inflammatory conditions such as asthma and irritable bowel syndrome 15 16 17 The main use for which these antagonist drugs have been applied so far however is as antiemetics in both human and veterinary medicine 18 19 Examples of tachykinin antagonists include 20 Aprepitant Casopitant Fosaprepitant Maropitant Nepadutant Osanetant Saredutant TalnetantSubfamilies editTachykinin InterPro IPR008215References edit Grace RC Lynn AM Cowsik SM February 2001 Lipid induced conformation of the tachykinin peptide Kassinin J Biomol Struct Dyn 18 4 611 21 623 5 doi 10 1080 07391102 2001 10506693 PMID 11245256 S2CID 42266413 a b Carter MS Krause JE July 1990 Structure expression and some regulatory mechanisms of the rat preprotachykinin gene encoding substance P neurokinin A neuropeptide K and neuropeptide gamma J Neurosci 10 7 2203 14 doi 10 1523 JNEUROSCI 10 07 02203 1990 PMC 6570392 PMID 1695945 Maggio JE 1988 Tachykinins Annu Rev Neurosci 11 13 28 doi 10 1146 annurev ne 11 030188 000305 PMID 3284438 Helke CJ Krause JE Mantyh PW Couture R Bannon MJ 1990 Diversity in mammalian tachykinin peptidergic neurons multiple peptides receptors and regulatory mechanisms FASEB J 4 6 1606 15 doi 10 1096 fasebj 4 6 1969374 PMID 1969374 S2CID 25935155 Avanov AIa 1992 Tachykinins and conformational aspects of their interactions with receptors Mol Biol Mosk 26 1 5 24 PMID 1324401 Dornan WA Vink KL Malen P Short K Struthers W Barrett C August 1993 Site specific effects of intracerebral injections of three neurokinins neurokinin A neurokinin K and neurokinin gamma on the expression of male rat sexual behavior Physiol Behav 54 2 249 58 doi 10 1016 0031 9384 93 90107 Q PMID 7690487 S2CID 33412235 Online Mendelian Inheritance in Man OMIM TAC1 162320 Online Mendelian Inheritance in Man OMIM TAC3 162330 Alvaro G Di Fabio R September 2007 Neurokinin 1 receptor antagonists current prospects Curr Opin Drug Discov Dev 10 5 613 21 PMID 17786860 Duffy RA May 2004 Potential therapeutic targets for neurokinin 1 receptor antagonists Expert Opin Emerg Drugs 9 1 9 21 doi 10 1517 eoed 9 1 9 32956 PMID 15155133 Salome N Stemmelin J Cohen C Griebel G April 2006 Selective blockade of NK2 or NK3 receptors produces anxiolytic and antidepressant like effects in gerbils Pharmacol Biochem Behav 83 4 533 9 doi 10 1016 j pbb 2006 03 013 PMID 16624395 S2CID 15134994 Louis C Stemmelin J Boulay D Bergis O Cohen C Griebel G March 2008 Additional evidence for anxiolytic and antidepressant like activities of saredutant SR48968 an antagonist at the neurokinin 2 receptor in various rodent models Pharmacol Biochem Behav 89 1 36 45 doi 10 1016 j pbb 2007 10 020 PMID 18045668 S2CID 21490514 Spooren W Riemer C Meltzer H December 2005 Opinion NK3 receptor antagonists the next generation of antipsychotics Nat Rev Drug Discov 4 12 967 75 doi 10 1038 nrd1905 PMID 16341062 S2CID 13270787 Chahl LA August 2006 Tachykinins and neuropsychiatric disorders Curr Drug Targets 7 8 993 1003 doi 10 2174 138945006778019309 PMID 16918327 Groneberg DA Harrison S Dinh QT Geppetti P Fischer A August 2006 Tachykinins in the respiratory tract Curr Drug Targets 7 8 1005 10 doi 10 2174 138945006778019318 PMID 16918328 Improta G Broccardo M August 2006 Tachykinins role in human gastrointestinal tract physiology and pathology Curr Drug Targets 7 8 1021 9 doi 10 2174 138945006778019354 PMID 16918330 Boot JD de Haas S Tarasevych S et al March 2007 Effect of an NK1 NK2 receptor antagonist on airway responses and inflammation to allergen in asthma Am J Respir Crit Care Med 175 5 450 7 doi 10 1164 rccm 200608 1186OC PMID 17170385 S2CID 22707433 Navari RM December 2007 Fosaprepitant MK 0517 a neurokinin 1 receptor antagonist for the prevention of chemotherapy induced nausea and vomiting Expert Opin Investig Drugs 16 12 1977 85 doi 10 1517 13543784 16 12 1977 PMID 18042005 S2CID 21437603 Hickman MA Cox SR Mahabir S et al June 2008 Safety pharmacokinetics and use of the novel NK 1 receptor antagonist maropitant Cerenia for the prevention of emesis and motion sickness in cats J Vet Pharmacol Ther 31 3 220 9 doi 10 1111 j 1365 2885 2008 00952 x PMID 18471143 Quartara L Altamura M August 2006 Tachykinin receptors antagonists from research to clinic Curr Drug Targets 7 8 975 92 doi 10 2174 138945006778019381 PMID 16918326 External links editTachykinins at the U S National Library of Medicine Medical Subject Headings MeSH This article incorporates text from the public domain Pfam and InterPro IPR002040 Retrieved from https en wikipedia org w index php title Tachykinin peptides amp oldid 1215607835, wikipedia, wiki, book, books, library,

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