Tertomotide

Tertomotide
Identifiers
  • (2S)-6-amino-2-[[(2S)-1-[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-carboxybutanoyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-phenylpropanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbonyl]amino]hexanoic acid
CAS Number
PubChem CID
Chemical and physical data
FormulaC85H146N26O21
Molar mass1868.264 g·mol−1
3D model (JSmol)
  • CC[C@H](C)[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)O)NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)N
  • InChI=1S/C85H146N26O21/c1-12-47(8)65(81(130)111-38-22-30-63(111)78(127)102-56(82(131)132)25-16-17-33-86)108-75(124)60(42-51-23-14-13-15-24-51)106-71(120)53(26-18-34-94-83(88)89)99-72(121)58(40-45(4)5)104-70(119)54(27-19-35-95-84(90)91)100-76(125)61(43-112)107-79(128)66(50(11)113)109-74(123)59(41-46(6)7)105-73(122)57(39-44(2)3)103-68(117)49(10)98-77(126)62-29-21-37-110(62)80(129)55(28-20-36-96-85(92)93)101-67(116)48(9)97-69(118)52(87)31-32-64(114)115/h13-15,23-24,44-50,52-63,65-66,112-113H,12,16-22,25-43,86-87H2,1-11H3,(H,97,118)(H,98,126)(H,99,121)(H,100,125)(H,101,116)(H,102,127)(H,103,117)(H,104,119)(H,105,122)(H,106,120)(H,107,128)(H,108,124)(H,109,123)(H,114,115)(H,131,132)(H4,88,89,94)(H4,90,91,95)(H4,92,93,96)/t47-,48-,49-,50+,52-,53-,54-,55-,56-,57-,58-,59-,60-,61-,62-,63-,65-,66-/m0/s1
  • Key:WZJRQXZSYQYFJV-QAXVQDKQSA-N

Tertomotide (GV1001, EARPALLTSRLRFIPK) is a 16-amino acid peptide based on the 616‑626 position fragment of human telomerase reverse transcriptase protein (hTERT). It was originally developed as a peptide vaccine for cancer, as it can trigger immune attack against cancer cells which overexpress telomerase, a common mutation found in malignant tumors.[1][2] However, it does not block telomerase activity in healthy tissue and has been found to produce various useful activities in its own right including antiviral,[3] antiinflammatory[4][5] and antidepressant effects, and has been trialled for numerous other medical applications including Alzheimer's disease[6][7][8][9][10][11] as well as its original role in the treatment of cancer.[12]

See also

References

  1. ^ Nava-Parada P, Emens LA (October 2007). "GV-1001, an injectable telomerase peptide vaccine for the treatment of solid cancers". Current Opinion in Molecular Therapeutics. 9 (5): 490–497. PMID 17932813.
  2. ^ Relitti N, Saraswati AP, Federico S, Khan T, Brindisi M, Zisterer D, et al. (2020). "Telomerase-based Cancer Therapeutics: A Review on their Clinical Trials". Current Topics in Medicinal Chemistry. 20 (6): 433–457. doi:10.2174/1568026620666200102104930. PMID 31894749.
  3. ^ Choi YM, Kim H, Lee SA, Lee SY, Kim BJ (2020). "A Telomerase-Derived Peptide Exerts an Anti-Hepatitis B Virus Effect via Mitochondrial DNA Stress-Dependent Type I Interferon Production". Frontiers in Immunology. 11 652. doi:10.3389/fimmu.2020.00652. PMC 7253625. PMID 32508804.
  4. ^ Kim JH, Bhusal A, Kwon J, Lee JY, Song MS, Lee WH, et al. (January 2026). "Therapeutic effects of telomerase-derived peptide GV1001 in experimental autoimmune encephalomyelitis: Inhibiting neuroinflammation and promoting remyelination". Biochemical Pharmacology. 243 (Pt 1) 117514. doi:10.1016/j.bcp.2025.117514. PMID 41187882.
  5. ^ Park H, Kwon HS, Lee KY, Kim YE, Son JW, Choi NY, et al. (January 2024). "GV1001 modulates neuroinflammation and improves memory and behavior through the activation of gonadotropin-releasing hormone receptors in a triple transgenic Alzheimer's disease mouse model". Brain, Behavior, and Immunity. 115: 295–307. doi:10.1016/j.bbi.2023.10.021. PMID 37884161.
  6. ^ Chen W, Shin KH, Kim S, Shon WJ, Kim RH, Park NH, et al. (June 2018). "hTERT peptide fragment GV1001 demonstrates radioprotective and antifibrotic effects through suppression of TGF‑β signaling". International Journal of Molecular Medicine. 41 (6): 3211–3220. doi:10.3892/ijmm.2018.3566. PMC 5881842. PMID 29568955.
  7. ^ Kwon HS, Koh SH, Choi SH, Jeong JH, Na HR, Lee CN, et al. (July 2023). "Effects of GV1001 on Language Dysfunction in Patients With Moderate-to-Severe Alzheimer's Disease: Post Hoc Analysis of Severe Impairment Battery Subscales". Dementia and Neurocognitive Disorders. 22 (3): 100–108. doi:10.12779/dnd.2023.22.3.100. PMC 10400345. PMID 37545861.
  8. ^ Park HH, Kwon HS, Lee KY, Kim YE, Son JW, Choi NY, et al. (January 2024). "GV1001 reduces neurodegeneration and prolongs lifespan in 3xTg-AD mouse model through anti-aging effects". Aging. 16 (3): 1983–2004. doi:10.18632/aging.205489. PMC 10911355. PMID 38301041.
  9. ^ Piao M, Lee SH, Hwang JW, Kim HS, Han YH, Lee KY (July 2024). "The Cell-Penetrating Peptide GV1001 Enhances Bone Formation via Pin1-Mediated Augmentation of Runx2 and Osterix Stability". Biomolecules. 14 (7): 812. doi:10.3390/biom14070812. PMC 11274716. PMID 39062525.
  10. ^ Shin TJ, Ha JY, Kwon SY, Park DJ, Kim JH, Lee SW, et al. (June 2025). "A randomized, active-controlled, multicenter, phase 3 clinical trial to evaluate the efficacy and safety of GV1001 in patients with benign prostatic hyperplasia". Prostate International. 13 (2): 81–89. doi:10.1016/j.prnil.2024.10.001. PMC 12223535. PMID 40620871.
  11. ^ Kim D, Lee Y, Kim S, Yu SW (October 2025). "Anti-depressant effects of a human telomerase-derived peptide GV1001 in an animal model of chronic restraint stress". Behavioural Brain Research. 494 115724. doi:10.1016/j.bbr.2025.115724. PMID 40617302.
  12. ^ Chen W, Beheshtian C, Kim S, Kim R, Kim S, Park NH (November 2025). "GV1001, an hTERT-Derived Peptide, Prevents Cisplatin-Induced Nephrotoxicity by Preserving Mitochondrial Function". Cells. 14 (22): 1818. doi:10.3390/cells14221818. PMC 12651939. PMID 41294871.
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