Gap 26

- Overview
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    Background
    
    Gap26 (Val-Cys-Tyr-Asp-Lys-Ser-Phe-Pro-Ile-Ser-His-Val-Arg) is a connexin mimetic peptide, corresponding to residues 63-75 of connexin 43, which is a gap junction blocker.
    Connexins, or gap junctions, are a family of structurally-related transmembrane proteins. Gap junctions contain channels that allow the passage of ions and small molecules between adjacent cells molecules. Calcium and inositol phosphates are among the second messengers that can pass through gap junction channels. [1] It was showed that gap26 attenuates rhythmic contractile activity of rabbit arterial smooth muscle (IC50 = 28.4 mM). It also blocks movement of IP3-induced ATP and Ca2+ across connexin hemichannels, i.e. hexameric channels yet to dock with partners in aligned cells and to generate the gap junction cell–cell conduit. [2]
    
    1. Boitano, S. and H. Evans Am. J. Physiol. Lung Cell Mol. Physiol. 279, L623 (2000).
    2. T. Desplantez, V. Verma, L. Leybaert, W.H. Evans, R. Weingart, Gap26, a connexin mimetic peptide, inhibits currents carried by connexin43 hemichannels and gap junction channels, Pharmacological Research, Volume 65, Issue 5, May 2012, Pages 546-552.
- Properties
  - Categories
    
    Gap junction blocker peptide, mapping to connexin 43 residue 63-75
    
    Alternative Name
    
    Val-Cys-Tyr-Asp-Lys-Ser-Phe-Pro-Ile-Ser-His-Val-Arg
    
    CAS Number
    
    197250-15-0
    
    Molecular Formula
    
    C70H107N19O19S
    
    Molecular Weight
    
    1550.79
    
    Appearance
    
    A solid
    
    Purity
    
    97.96%
    
    Solubility
    
    insoluble in EtOH; ≥155.1 mg/mL in H2O with ultrasonic; ≥77.55 mg/mL in DMSO with gentle warming and ultrasonic
    
    Storage
    
    Desiccate at -20°C
    
    * For Research Use Only
- Reference
  - 1. Chenyu Liang, Qian Zhang, et al. "Human cancer cells generate spontaneous calcium transients and intercellular waves that modulate tumor growth." Biomaterials. 2022 Oct 5;290:121823. PMID: 36209577
    2. Xuqing Qin, Wenjun He, et al. "Inhibition of Connexin 43 reverses ox-LDL-mediated inhibition of autophagy in VSMC by inhibiting the PI3K/Akt/mTOR signaling pathway." PeerJ. 2022 Mar 16;10:e12969. PMID: 35313522
    3. Guo-Li Zhao, Hong Zhou, et al. "Modulation of Rac1/PAK1/connexin43-Mediated ATP Release from Astrocytes Contributes to Retinal Ganglion Cell Survival in Experimental Glaucoma." Research Square. rs-770147/v1.
    4. Rui-Juan Gao, Ai-Mei Zhang, et al. "The promoting role of Cx43 on the proliferation and migration of arterial smooth muscle cells for angiotensin II-dependent hypertension." Pulm Pharmacol Ther. 2021 Oct;70:102072. PMID: 34428599
    5. Zhou Z, Ni J, et al. "Angiotensin II induces RAW264. 7 macrophage polarization to the M1-type through the connexin 43/NF-κB pathway." Mol Med Rep. 2020;21(5):2103-2112. PMID: 32186758
    6. Steven Condamine. "Organisation anatomique et rôle du couplage astrocytaire dans l’activité rythmique du noyau sensoriel du trijumeau." Université de Montréal. 2019.
    7. Wang M, Wu Y, et al. "Rutaecarpine prevented ox-LDL-induced VSMCs dysfunction through inhibiting overexpression of connexin 43." Eur J Pharmacol. 2019 Jun 15;853:84-92. PMID: 30880182
    8. Mederos S, Hernández-Vivanco A, et al. "Melanopsin for precise optogenetic activation of astrocyte-neuron networks." Glia. 2019 Jan 11. PMID: 30632636
    9. Zhang X, Chen D, et al. "Involvement of sphingosine-1-phosphate receptors 2/3 in IR-induced sudden cardiac death." Heart Vessels. 2019 Jan 2. PMID: 30604190
    10. Condamine S, Lavoie R, et al. "Functional Rhythmogenic Domains Defined by Astrocytic Networks in the Trigeminal Main Sensory Nucleus." Glia. 2017 Oct 23. PMID: 29058348
    11. Yang G, Peng X, et al. "Involvement of connexin 43 phosphorylation and gap junctional communication between smooth muscle cells in vasopressin-induced ROCK-dependent vasoconstriction after hemorrhagic shock." Am J Physiol Cell Physiol. 2017 Oct 1;313(4):C362-C370. PMID: 28974518
    12. Li X, Jiang S, et al. "Breakthrough Cancer Pain Is Associated with Spinal Gap Junction Activation via Regulation of Connexin 43 in a Mouse Model." Front Cell Neurosci. 2017 Jul 17;11:207. PMID: 28769766
    13. Chu H, Huang C, et al. "Reduction of Ischemic Brain Edema by Combined use of Paeoniflorin and Astragaloside IV via Down-Regulating Connexin 43." Phytother Res. 2017 Jul 28. PMID: 28752625
    14. Zhou, Ziyi, et al. "Protection of erythropoietin against ischemic neurovascular unit injuries through the effects of connexin43." Biochemical and biophysical research communications 458.3 (2015): 656-662. PMID: 25684187