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. 2021 Sep 22;22(19):10186. doi: 10.3390/ijms221910186

Table 1.

Connexin regulating peptides.

Year Peptide Sequence/Formula Known Target Cx Linker Properties Increase Cx43-PKC Refs.
Cx Region
Non-Mimetic Peptides—Indirect Effects
1980 AAP10 H-GAG-4hyp-PY-CONH Cx43 *
Cx40 *		 Indirect: Unknown GPCR pathway - Increases Cx synthesis, expression, phosphorylation, membrane targeting, and GJ opening Y [58,72,76,77,84]
2003 Rotagaptide (ZP123) H2N-GDAGD-4hyp-DPDY-Ac Cx43 * NT Acetyl Y [51]
2013 Danegaptide (ZP1609, GAP134) C14H17N3O4 Cx43 * - Y [69,74]
Extracellular Loop 1 (EL1)
1997 Gap26 VCYDKSFPISHVR Cx43, Cx32, Cx26 64–76 - HC block Y [92,93]
2001 43Gap26 VCYDKSFPISHVR Cx43 64–76 - HC block Y [94,95]
2009 43Gap26M VCYDKSFPISHVR Cx43 64–76 NT Acetyl HC block Y [95,96]
2001 37,40Gap26 VCYDQAFPISHIR Cx37, Cx40 64–76 - HC block ND [94]
1999 Unlabelled ICNTLQPGCNSV Cx32 52–63 - GJ block ND [97]
2007 Peptide 1848 CNTQQPCCENVCY Cx43 54–66 - GJ Block ND [98]
Extracellular Loop 2 (EL2)
1999 Unlabelled SLSAVYTCKRDPCPHE Cx43 180–195 - GJ block ND [99]
1999 Unlabelled FLDTLHVCRRSPCPHP Cx40 177–192 - GJ block ND [99]
2001 37,43Gap27 SRPTEKTIFII Cx43, Cx37, Cx32, Cx26 201–211 - HC block Y [92,93,94,95,100]
2001 40Gap27 SRPTEKNVFIV Cx40 201–211 - GJ block ND [93,94,100]
2011 32Gap27 SRPTEKTVFT Cx32 182–191 - HC block ND [101]
2021 62Gap27 SRPTEKTIFML CX62 201–211 - HC & GJ block ND [102]
2008 Peptide 5 VDCFLSRPTEKT EL2 EL2 s-lipidation HC & GJ block ND [103,104,105,106]
2013 SRPTEKT/GAP21 SRPTEKT Cx32
Cx43		 182–188
204–210		 - HC block ND [92,101]
2018 SRPTEKT-Hdc
(Gap21)		 SRPTEKT-Hdc Cx43 EL2 Hexadecyl (HC) lipid moeity HC & GJ block Y [107,108]
2013 C12-Cx43 MP and C12-C12-Cx43 MP C12-VDCFLSRPTEKT
C12-C12-VDCFLSRPTEKT 		Cx43 199–210 1/2 C12-Laa moieties HC block ND [109]
Intracellular Loop (IL)
2006 32GAP24
TAT-GAP24		 GHGDPLHLEEVKC
YGRKKRRQRRRGHGDPLHLEEVKC		 Cx32
Cx43
Panx1		 110–122 +/− TAT HC block
Inhibit GJ formation		 ND [10,110,111]
2004 L2 (Cx43L2) DGVNVEMHLKQIEIKKFKYGIEEHGK Cx43 119–142 - HC block, not GJ
GJ block		 ND [42,112,113]
2010 TAT-L2 TAT-DGANVDMHLKQIEIKKFKYGIEEHGK Cx43 119–142 TAT HC block ND [114]
2013 Gap19 KQIEIKKFK Cx43 128–136 - HC block ND [111,115,116]
2014 TAT-Gap19 KQIEIKKFK Cx43 128–136 TAT HC block ND [117]
2020 Xentry-Gap19 KQIEIKKFK Cx43 128–136 LCLRPV HC block [118]
2010 TAT-Cx50L2 GGERAPLAADQGSVKKSSSSSKGTKK Cx50 122–147 TAT ND Cx50,
No effect on Cx43 HC		 ND [114]
Gap 20 EIKKFKYGC Cx43 131–138 - No effect ND [119]
Gap 22 AELSCNKEVNG Cx40 130–140 - No effect ND [92]
N-terminus/C-terminus
2005 Alpha CT1 RPRPDDLEI Cx43 374–382 Antenna-pedia Promotes GJ formation, enhance GJ,
HC block		 Y [120,121,122]
2009 Alpha CT11
aka (Alpha CT2)		 RPRPDDLEI Cx43 374–382 None Promotes GJ formation, enhance GJ,
HC block		 Y [122,123]
2009 Alpha CT3 RQPKIWFPNRRKPWKKRPSSRASSRASSRPRPDDLEI Cx43 359–382 Antenna-pedia ND ND [122]
2010 TAT-Cx43CT SRPRPDDLEI Cx43 373–382 TAT Maintains open channel and permits dye transfer. Inhibits HC block ND [114]
2011 CT9 RPRPDDLEI Cx43 374–382 +/− TAT HC block Y [101,124,125]
2013 TAT-CT10 SRPRPDDLEI Cx43 373–382 TAT Inhibits the effect of CxL2 peptides—stops L2 hemichannel blockade ND [115]
2010 TAT-Cx50CT SRARSDDLTV Cx50 431–440 TAT ND–Cx50,
No effect on Cx43 HC		 ND [114]
2010 ZP2519 AcRRK-(4 hydroxy benzoyl) Cx43
C-term		 - - GJ opening ND [126]
2015 Juxtamembrane 2 (JM2) VFFK-GVKDRVKGRSD Cx43 231–245 Antenna-pedia HC block ND [127]
2020 TAT-Cx43 266–283 AYFNGCSSPTAPLSPMSP Cx43 266–283 TAT ND ND [128,129]

* indicates alterations through a GPCR pathway. Abbreviations used in the table: Cx—connexin; GJ—gap junction; HC—hemichannel; GPCR—G protein-coupled receptor; ND—not demonstrated; CT—carboxyl-terminus; EL—extracellular loop; IL—intracellular loop; NT—amino-terminus.