Cell-Penetrating Peptides
Os CPPs são capazes de transportar ácidos nucleicos e nanomateriais para o interior das células. Os CPPs podem interagir com os materiais a serem transportados para dentro das células através de ligações covalentes ou não covalentes. Dependendo da natureza físico-químicas do complexo CPP+carregamento, o mecanismo de entrada celular pode ocorrer por endocitose clássica, macropinocitose, vias dependentes de clatrina e caveolina, e a penetração direta da membrana. Diversos métodos químicos e moleculares vem sendo aplicados para aprimorar o uso de CPPs e superar o uso de micelas e lipossomas para entregar moléculas no interior das células.
A GenOne pode produzir peptídeos sintéticos para as mais diversas aplicações, inclusive CPPs. Podemos elaborar modificações fluorescentes e químicas para alterar suas características, permitindo acompanhar a entrada nas células e facilitar o acoplamento com outras moléculas.
Entre em contato, tire suas dúvidas e peça um orçamento!
| Name | Sequence | Description | Reference | |
|---|---|---|---|---|
| (Arg)9 | RRRRRRRRR | This is a peptide comprising of 9 arginine residues. It has been shown that poly-Arg peptides composed of 9 arginine residues are able to efficiently translocate across cells. It has also been shown in model systems that Arg-9 translocation involves nucleation of transient pores enabling flow of ions across the membrane. and that it's electrostatic attraction to the phosphate groups of membranes is a key property for its translocation. | 1, Wender PA. et al.PNAS USA. 97(24):13003-13008 (2000). 2, Herce HD. et al. Biophys J. 97(7): 1917-1925 (2009). | |
| [Cys58]105Y, Cell Penetrating Peptide, α1 - antitrypsin (358 - 374) | CSIPPEVKFNKPFVYLI | This is a synthetic peptide based on the sequence corresponding to residues 359 to 374 of α1-antitrypsin. C105Y can penetrate cell membrane rapidly, enter the cytoplasm, and localize to the nucleus and nucleolus of live culture cells. C105Y peptide is routed to the nucleolus very rapidly in an energy-dependent fashion; whereas membrane translocation and nuclear localization are energy-independent. It enhances gene expression from DNA nanoparticles. | M. Rhee and P. Davis J. Biol. Chem. 281, 1233 (2006). | |
| Aminopeptidase N Ligand (CD13), NGR peptide | CNGRCG (Disulfide bridge: 1 - 5) | The NGR (Asn-Gly-Arg) peptide motif is an aminopeptidase N (CD13) ligand that targets angiogenic blood vessels. NGR-containing peptides have been proven useful for delivering cytotoxic drugs, proapoptotic peptides and tumor necrosis factor (TNF) to tumor vasculature. | Curnis, F. et al. Cancer Res. 62, 867 (2002); Curnis, F. et al. J. Clin. Invest. 110, 475 (2002). | |
| Antennapedia Leader Peptide (CT) | KKWKMRRNQFWVKVQRG | This cell-permeable carrier peptide is used to deliver the functional domain of certain proteins from the outside to the inside of intact cells. | Kanovsky, M. et al. Proc. Natl. Acad. Sci. 98, 12438 (2001). | |
| Antennapedia Peptide, acid | RQIKIWFQNRRMKWKK | This is a 16 amino acid peptide corresponding to the region within the Drosophila Antennapedia DNA binding domain that is mapped to be responsible for cellular internalization. This peptide is also called penetratin. The peptide has been shown to be able to translocate through the plasma membrane to the cytosol and nucleus of living cells, both at 37 ◦C and 4 ◦C. | Pietersz GA. et al. Vaccine. 19:1397-1405 (2001); Christiaens B. et al. Eur J Biochem. 27(16):1187-1197 (2004). | |
| Antennapedia Peptide, amide | RQIKIWFQNRRMKWKK - NH2 | This is a 16 amino acid peptide corresponding to the region within the Drosophila Antennapedia DNA binding domain that is mapped to be responsible for cellular internalization. This peptide is also called penetratin. The peptide has been shown to be able to translocate through the plasma membrane to the cytosol and nucleus of living cells, both at 37 ◦C and 4 ◦C. | Pietersz GA. et al. Vaccine. 19:1397-1405 (2001); Christiaens B. et al. Eur J Biochem. 27(16):1187-1197 (2004). | |
| Anti - BetaGamma (MPS - Phosducin - like protein C terminus) | AAVALLPAVLLALLAVTDQLGEDFFAVDLEAFLQEFGLLPEKE | This is a membrane-permeable phosphoducin-like anti-βγ peptide, whose membrane-permeable sequence (MPS) is derived from the C-terminal residues of phosducin-like protein (PhLP). This region of PhLP has been shown to confer interactions with Gβϒ-mediated signaling. Specifically, it was shown to have inhibitory effects on Go GTPase activity, demonstrating the ability to bind Gβγ, and inhibition of Gβγ-enhanced rhodopsin phosphorylation by βARK. The PhLP shares amino acid sequence homology with phosphoducin, a phosphoprotein expressed in the retina and pineal gland. These proteins have been shown to regulate G-protein signaling by binding to the beta-gamma subunits of G proteins. | Orr, A. et al. J. Biol. Chem. 277, 20453 (2002); Chang M. et al. J Biol Chem. 275:7021-7029 (2000). | |
| Bcl - 2 Binding Peptide, cell permeable | Decanoyl - KNLWAAQRYGRELRRMSDEFEGSFKGL | This is a cell permeable bcl-2 binding peptide. This peptide is derived from the BH3 domain (a death domain) of Bad, amino acid residues 140 to 165. It is cell permeable due to the N-terminal modification by a decanoyl moiety. | Wang, J. L. et al. Cancer Res. 60, 1498 (2000) | |
| Beclin - 1 | TNVFNATFHIWHSGQFGT | Beclin-1 peptide is HIV-1 Nef binding portion of full-length human Beclin-1 protein (amino acids 267-299). Beclin-1 protein is an autophagy inducing agent that may trigger cellular adaptation, survival, or cell death. When conjugated to the cell-permeable peptide, it can successfully enter cells and induce autophagy. | Shoji-Kawata, S. Nature 494, 201-209 (2013); Marquez, RT. Am J Cancer Res 2 (2), 214–221 (2012). | |
| Buforin | TRSSRAGLQFPVGRVHRLLRK | This peptide, also referred to as Buforin II peptide is a 21 amino acid peptide derived from Buforin I peptide that is isolated from the Asian toad Bufo gargarizans. The 21 amino acid peptide has been shown to possess anti-microbial activity by penetrating bacteria and inhibiting cellular functions. In comparison to magainin 2, this peptide binds DNA and RNA from E.coli with a much greater affinity. It is also considered a cell-delivery peptide and has been shown to deliver SiRNAs into cells followed by effective mRNA degradation. | Bartz, R. et al. (2011). Effective siRNA delivery and target mRNA degradation using an amphipathic peptide to facilitate pH-dependent endosomal escape. Biochem J4352, 475-487. doi: 10.1042/BJ20101021. | |
| Chimeric Rabies Virus Glycoprotein Fragment (RVG - 9R) | YTIWMPENPRPGTPCDIFTNSRGKRASNGGGGRRRRRRRRR | This chimeric peptide is a fragment derived from rabies virus glycoprotein (RVG). Because neurotropic viruses cross the blood-brain barrier to infect brain cells, the same strategy may be used to enter the central nervous system and deliver siRNA to the brain. To enable siRNA binding, this chimeric peptide was synthesized by adding nonamer arginine residues at the carboxy terminus of RVG. This RVG-9R peptide was able to bind and transduce siRNA to neuronal cells in vitro, resulting in efficient gene silencing. After intravenous injection into mice, RVG-9R delivered siRNA to the neuronal cells, resulting in specific gene silencing within the brain. RVG-9R provides a safe and noninvasive approach for the delivery of siRNA and potentially other therapeutic molecules across the blood–brain barrier. | Kumar, P. et al. Nature 448, 39 (2007). | |
| hCT (Calcitonin), Human | LGTYTQDFNKFHTFPQTAIGVGAP | hCT (Calcitonin) is a cell-penetrating peptide (CPP) that is derived from human calcitotnin protein sequence. It has good proteolytic resistance and can permeate cell membrane at low micromolar concentration without significantly affecting cell membrane. hCT can be conjugated with large molecules and used as a drug delivery vehicle. | Nasrollahi, SA. et al. Chem Biol Drug Des 08, 639 (2012); Rennert, R. et al. Biochim Biophys Acta 1758, 347 (2006). | |
| Hel 13 - 5 | KLLKLLLKLWLKLLKLLL | This synthetic peptide contains Leu and Lys residues in the ratio of 13:5. It binds to DNA and forms alpha-helical structures. It is used as an efficient way for gene transfer into cells and DNA transfection. | Pujals, S. et al. BBA - Biomembranes. 1758,3 (2006). | |
| HIV - 1 Tat (48 - 60) | GRKKRRQRRRPPQ | This is one of the cell-penetrating peptides (CPPs) derived from the human immunodeficient virus (HIV)-1 Tat protein residue 48-60. It has been used to deliver exogenous macromolecules into cells in a non-disruptive way. | Dennison, S.R. et al. Biochem. and Biophy. Res. Comm. 363, 178 (2007); Futaki, S. Advanced Drug Delivery Rev. 57, 547 (2005) | |
| KALA | WEAKLAKALAKALAKHLAKALAKALKACEA | KALA is a cationic amphipathic cell-penetrating peptide (CPP). It assumes an α-helix conformation when the pH is 7.5. KALA binds oligonucleotides and disrupts cell membrane; therefore, it can be used as a DNA transfection reagent. | Nasrollahi, SA. et al. Chem Biol Drug Des 08, 639 (2012); Wyman, TB. et al. Biochem 36 (10), 3008-3017 (1997). | |
| MAP (KLAL) | KLALKLALKALKAALKLA | MAP (KLAL) is an amphipathic ?-helical cell-penetrating peptide (CPP). KLAL peptide assumes an ?-helical secondary structure when it first binds to surface membrane and rapidly changes to ?-sheet. CPP can be conjugated with large molecules and used as a drug delivery vehicle. | Nasrollahi, SA. et al. Chem Biol Drug Des 08, 639 (2012); Kerth, A. et al. Biophys J 86, 3750-3758 (2004). | |
| Mastoparan | INLKALAALAKKIL - NH2 | This 14-residue peptide toxin from the wasp venom is originally found as a histamine releaser from mast cells. It induces mitochondrial membrane permeabilization via a CsA-inhibitable mechanism. | Hori, Y. et al. Eur. J. Biochem. 268, 302 (2001); Hirata, Y. et al. Mol. Pharmacol. 57, 1235 (2000); Yajima, Y. et al. Endocrinol. 138, 1949 (1997); Sukumar, M. et al. Biochem. 36, 3632 (1997); Higashijima, T. et al. J. Biol. Chem. 263, 6491 (1995). | |
| Mastoparan 7 | INLKALAALAKALL - NH2 | This mastoparan modification, referred as mastoparan 7 (MP7), has Lys12 replaced by Ala12, and Ile13 replaced by Leu13. Mastoparan is an amphiphilic tetradecapeptide isolated from wasp venom. It is known to possess a variety of biological activities including mast cell degranulation, mobilization of Ca2+ from cerebellar microsomes and sarcoplasmic reticulum, and modulation of various enzymes. MP7 retains the ability to form α-helices in lipids and have similar hydrophobic moments to mastoparan. Mastoparan also inhibits the ATPase. | Longland, C. et al. J. Biol. Chem. 274, 14799 (1999). | |
| Maurocalcine | GDC(acm)LPHLKLC | Maurocalcine is a short cell-penetrating peptide (CPP) derived from the venom peptide of Tunician scorpion. It can permeate cell membrane at low micromolar concentration in minutes without significantly affecting cell membrane. Maurocalcine can be conjugated with large molecules and used as a drug delivery vehicle. | Aroi, S. et al. Pharm Res 26 (4), 836-845 (2009); Tisseyre, C. et al. Pharmaceuticals 6, 320-339 (2013). | |
| MEK1 Derived Peptide Inhibitor 1 | MPKKKPTPIQLNP | This cell permeable peptide is comprised of the first 13 amino acids of human mitogen-activated protein kinase kinase-1 (MEK1). It inhibits the in-vitro activation of ERK2 by MEK1. | Kelemen, B. et al. J. Biol. Chem. 277, 8741 (2002). | |
| Membrane - Permeable Sequence, MPS | AAVALLPAVLLALLAK | This peptide corresponds to the membrane-permeable sequence designed from the carboxyl terminus of Gα subunits targeting G protein subunits. This is a membrane-translocating hydrophobic sequence derived specifically from the h-region of a signal peptide sequence of K-FGF (Kaposi fibroblast growth factor). | Orr, A. et al. J. Biol. Chem. 277, 20453 (2002); Lin Y-Z. et al. J Biol Chem. 270, 14255-14258 (1995). | |
| MPGΔNLS, HIV related | GALFLGFLGAAGSTMGAWSQPKSKRKV | This 27-residue peptide, designated MPGΔNLS,is derived from the hydrophobic fusion peptide of HIV-1 gp41 (for efficient crossing of the cell membrane) and the hydrophilic nuclear localization sequence of SV40 large T antigen (for the nuclear addressing of the peptide). MPGΔNLS contains a single mutation in which the second lysine in the NLS has been mutated to serine. | Deshayes, S. et al. Adv. Drug Deliv. Rev. 60, 537 (2008); Morris, M. et al. Nucleic Acids Res. 27, 3510 (1999); Simeoni, F. et al. Nucleic Acids Res. 31, 2717 (2003). | |
| NGR Peptide 1 | CNGRCGGklaklakklaklak - NH2 (Disulfide bridge: 1 - 5) | This is a peptide with NGR (Asn-Gly-Arg) motif having a disulfide bridge connecting cys1 to cys5 known to elicit antimicrobial property in addition to the presence of KLA sequence. This peptide shows potent cytotoxicity and activity against tumor cells due to its binding to CD13 on tumor cells. This peptide shows dose-dependent antiproliferation against tumor cells and induces cell cylce arrest at G2/M phases and apoptosis of the tumor cells. NGR motif containing peptides are useful in delivering cytotoxic drugs, proapoptotic peptides and tumor necrosis factor (TNF) to tumor vasculature. | Ellerby, HM. et al. Nat Med. 5, 1032 (1999); Colombo, G. et al. J. Biol. Chem. 277, 47891 (2002); Van Hensbergen, Y. et al. Biochem. Pharmacol. 63, 897 (2002); Plesniak, L. et al. Protein Sci. 13, 1988 (2004); Zhang Z. et al. Tum Biol. 36(10), 8167-8175 (2015). | |
| NGR Peptide 2 | CNGRCGGLVTT (Disulfide bridge: 1 - 5) | This is a peptide with NGR (Asn-Gly-Arg) motif having a disulfide bridge connecting cys1 to cys5. NGR motif containing peptides are useful in delivering cytotoxic drugs, proapoptotic peptides and tumor necrosis factor (TNF) to tumor vasculature. | Ellerby, HM. et al. Nat Med. 5, 1032 (1999); Colombo, G. et al. J. Biol. Chem. 277, 47891 (2002). | |
| NGR Peptide 3 | CNGRC - NH2 (Disulfide bridge: 1 - 5) | This is a cyclic pentapeptide with NGR (Asn-Gly-Arg) motif and has been identified as an aminopeptidase N (APN) /CD13 in the endothelium. When conjugated with Doxorubicin, this peptide shows prodrug properties with antiproliferative and anti-angiogenic effects. | Colombo, G. et al. J. Biol. Chem. 277, 47891 (2002); Van Hensbergen, Y. et al. Biochem. Pharmacol. 63, 897 (2002). | |
| NRTN (Neurturin), Human | GAAEAAARVYDLGLRRLRQRRRLRRERVRA | NRTN (Neurturin) is derived from human neurturin protein and acts as a cell-penetrating peptide (CPP). NRTN can permeate cell membrane at low micromolar concentration without significantly affecting cell membrane. It has been demonstrated that NRTN has high activity as an siRNA transfection reagent. | Nasrollahi, SA. et al. Chem Biol Drug Des 08, 639 (2012); Haas, AK. et al. Biochem J 442, 583-593 (2012). | |
| P1, Human | MGLGLHLLVLAAALQGAWSQPKKKRKV | P1 is a cell-penetrating peptide (CPP) that is derived from the human immunoglobulin heavy chain sequence. It can permeate cell membrane at low micromolar concentration without significantly affecting cell membrane. CPP can be conjugated with large molecules and used as a drug delivery vehicle. | Nasrollahi, SA. et al. Chem Biol Drug Des 08, 639 (2012). | |
| Penetratin | RQIKIWFQNRRMKWKKGG | Penetratin is a cell-penetrating peptide (CPP), also known as a protein transduction domain (PTD), of which the first 16 amino acids are derived from the third helix of the Antennapedia protein homeodomain. Penetratin linked to a phosphodiester oligonucleotide is capable of permeating through neuronal cell membranes and down-regulating genes. | Turner, J. et al. Nucleic Acids Res 33, 27 (2005). | |
| Penetratin - Arg | RQIRIWFQNRRMRWRR | Penetratin-Arg is a cell-penetrating peptide (CPP) that is derived from the 3rd helix of Drosophila Antennapedia homeodomain protein. Penetratin-Arg is the same as Penetratin except that Lysine residues were substituted with Arginines. It forms an ?-helix structure in lipid environment and can permeate cell membrane at low micromolar concentration without significantly affecting membrane. CPP can be conjugated with large molecules and used as a drug delivery vehicle. | Nasrollahi, SA. et al. Chem Biol Drug Des 08, 639 (2012); Ye, J. et al. J Am Chem Soc 132 (3), 1-21 (2010). | |
| Pep - 1 - Cysteamine | Ac - KETWWETWWTEWSQPKKKRKV - cysteamine | Pep-1 is one of the synthetic cell-penetrating peptides (CPPs), which has been successfully used to deliver a variety of proteins and other biopharmaceutical macromolecules into cells in a non-disruptive way. It is a CPP with primary amphipathicity (i.e amphipathicity resulting from the amino acid sequence itself, not from the folding structure) that comprises a tryptophan-rich so-called ‘hydrophobic’ domain, a hydrophilic domain derived from an NLS (nuclear localization signal) of SV40 (simian virus 40) large T-antigen, and a spacer between them. A cysteamine group is present at the C-terminus. The presence of cysteamine group in C terminal seems to play a crucial role in the delivery efficiency of cargoes into cells. | Henriques, S. et al. FEBS Letters Vol. 579, 4498 (2005). | |
| Pep - 1: Chariot (Non - Covalent Delivery of Peptides and Proteins) | KETWWETWWTEWSQPKKKRKV | This is a peptide carrier for the noncovalent delivery of proteins into cells. | Fischer, R. et al. Chem. Bio. Chem. 6, 2126 (2005). | |
| pVEC (Cadherin - 5) | LLIILRRRIRKQAHAHSK | pVEC is a cell-penetrating peptide (CPP) that is derived from murine vascular endothelian cadherin. It can permeate cell membrane at low micromolar concentration without significantly affecting cell membrane. pVEC can be conjugated with large molecules and used as a drug delivery vehicle. | Nasrollahi, SA. et al. Chem Biol Drug Des 08, 639 (2012); Elmquist, A. et al. Exp Cell Res 269 (2), 237-244 (2001). | |
| Rabies Virus Glycoprotein (RVG) | YTIWMPENPRPGTPCDIFTNSRGKRASNG | This peptide is a 29 amino acid fragment derived from rabies virus glycoprotein (RVG). Because neurotropic viruses cross the blood-brain barrier to infect brain cells, the same strategy may be used to enter the central nervous system and deliver siRNA to the brain. This peptide specifically binds to the acetylcholine receptor expressed by neuronal cells. | Kumar, P. et al. Nature 448, 39 (2007). | |
| SV - 40 Large T - antigen Nuclear Localization Signal (NLS) | CGGGPKKKRKVED | This peptide is derived from Large T antigen residue 47 to 55. It is a commonly used nuclear localization signal (NLS) peptide. It enables protein import into cell nucleus. | Tiganis, T. et al. J. Biol. Chem. 272, 21548 (1997) | |
| SV40 T - Ag - derived Nuclear Localization Signal (NLS) Peptide | PKKKRKVEDPYC | This peptide, a nuclear localization signal (NLS) peptide, is derived from the Large T antigen residues 47 to 56 (PKKKRKVEDP). It can be used to tag DNA. DNA tagged to this peptide efficiently translocates into the cell nucleus. | Schirmbeck, R. et al. J. Mol. Med. 79, 343 (2001); Vaysse, L. et al. J. Biol. Chem. 279,5555 (2004). | |
| Tat - Beclin - 1 | YGRKKRRQRRRGGTNVFNATFEIWHDGEFGT | Beclin-1 peptide is the HIV-1 Nef binding portion of full-length human Beclin-1 protein (amino acids 267-299). Beclin-1 protein is an autophagy inducing agent that may trigger cellular adaptation, survival or cell death. When conjugated to the cell-permeable peptide, it can successfully enter cells and induce autophagy. | Shoji-Kawata, S. Nature 494, 201-209 (2013); Marquez, RT. Am J Cancer Res 2 (2), 214–221 (2012). | |
| Tat - Beclin - 1, scrambled | YGRKKRRQRRRGGVGNDFFINHETTGFATEW | Beclin-1 peptide is the HIV-1 Nef binding portion of full-length human Beclin-1 protein (amino acids 267-299). Beclin-1 protein is an autophagy inducing agent that may trigger cellular adaptation, survival or cell death. When conjugated to the cell-permeable peptide, it can successfully enter cells and induce autophagy. Tat-Beclin-1, scrambled will not induce autophagy and can be used as a negative control. | Shoji-Kawata, S. Nature 494, 201-209 (2013); Marquez, RT. Am J Cancer Res 2 (2), 214–221 (2012). | |
| Tat - C (48 - 57) | CGRKKRRQRRR | This peptide is amino acids 48 to 57 fragment of TAT with an additional cysteine residue at the N-terminus. This peptide contains the protein transduction domain (PTD) of the HIV Tat protein that inhibits HSV-1 entry. The addition of a cysteine residue to the N-terminus of the Tat-PTD (Tat-C peptide) improves the antiviral activity against HSV-1 and HSV-2. Tat-C acts extracellularly, blocking entry of adsorbed virus immediately without eluting virions. | Bultmann, H. et al. Antimicrob. Agents Chemother. 51, 1596 (2007). | |
| TAT - GluR23A Fusion Peptide | YGRKKRRQRRRAKEGANVAG | This is the GluR23A sequence, a control inactive peptide used as a mutant counterpart to glutamate receptor endocytosis inhibitor (GluR23Y), connected to an 11 amino acid cell permeable HIV Trans-Activator of Transcription (TAT) protein transduction domain (PTD). GluR23A is derived from GluR23Y amino acids 869 to 877, with Ala substituted for Tyr, and thus lacking essential phosphorylation sites. | Ahmadian, G. et al. EMBO J 23, 1040 (2004); Wang, Y. et al. J Biol Chem 279, 41267 (2004); Yu, S. et al. J Neurochem 106, 889 (2008). | |
| Tat - GluR23Y | YGRKKRRQRRRYKEGYNVYG | The synthetic peptide (Tat-Glur23Y) contains tyrosine residues that blocks phosphorylation of alpha-amino-3-hydroxy-5-methyl-isoxazole-4-propionic acid (AMPA) receptor endocytosis. Previous research shows that Tat-Glur23Y blocks regulated AMPA and thereby prevents long-term depression (LTD) in structures such as the nucleus accumbens and dorsal hippocampus. | Dalton, G. et al. Neuropsychopharma. 33, 2416 (2008); Kim, J. et al. PNAS 104, 20955 (2007). | |
| Tat - GluR23Y, scrambled | YGRKKRRQRRRVYKYGGYNE | Tat-Glur23Y, scrambled is a control peptide. The synthetic peptide (Tat-Glur23Y), containing tyrosine residues, blocks phosphorylation of alpha-amino-3-hydroxy-5-methyl-isoxazole-4-propionic acid (AMPA) receptor endocytosis. However, the scrambled version does not have blockade properties. Previous studies show that Tat-Glur23Y, scrambled increase stress levels in mice, while Tat-Glur23Y reduces stress when administered. | Dalton, G. et al. Neuropsychopharma. 33, 2416 (2008); Kim, J. et al. PNAS 104, 20955 (2007). | |
| TAT - HA2 Fusion Peptide | RRRQRRKKRGGDIMGEWGNEIFGAIAGFLG | This sequence is amino acids 1 to 20 of influenza A virus hemagglutinin protein (HA2) connected to a 10 amino acid cell permeable HIV Trans-Activator of Transcription (TAT) protein transduction domain (PTD). TAT-HA2 is capable of being used as a large macromolecule drug delivery peptide. The TAT PTD binds to the cell surface and penetrates the membrane via lipid raft-dependent macropinocytosis. Endosomal escape and transduction of the fusion peptide are enhanced by the HA2 domain, which is a pH-sensitive lipid membrane destabilizing sequence. | Wadia, J. et al. Nature Med 10, 310 (2004). | |
| Tat - NR2Bct | YGRKKRRQRRRKLSSIESDV | This is the membrane-permeable postsynaptic density (PSD)-95-binding (decoy) peptide Tat-NR2Bct. It can transduce into neurons in cell culture. | Yang, L. et al. J. Neurosci. 24, 10846 (2004). | |
| TAT - NSF222 Fusion Peptide | YGRKKRRQRRR - GGG - LDKEFNSIFRRAFASRVFPPE | This sequence is N-ethyl-maleimide-sensitive factor (NSF) peptide connected to 11 amino acid cell permeable human immunodeficiency virus (HIV) transactivating regulatory protein (TAT) domain by Gly-Gly-Gly spacer. This peptide contains NSF domain extending from amino acids 222 to 243, which is directly amino-terminal of the Walker A motif of the D1 domain of NSF. ATPase assay shows that TAT-NSF222 inhibits NSF ATPase activity. | Matsushita, K. et al. Mol. Pharmacol. 67,1137 (2005). | |
| TAT - NSF222scr Fusion Polypeptide, scrambled | YGRKKRRQRRR - GGG - ENSFRFLADIFPAKAFPVRFE | This is a scrambled TAT-NSF222scr fusion polypeptide. It is composed of 11 amino acids from the cell permeable human immunodeficiency virus TAT polypeptide, 3 glycines as a linker, followed by scrambled N-Ethyl-maleimide-sensitive factor (NSF) D1 domain. This peptide is used as a control for the TAT-NSF222 peptide. | Matsushita, K. et al. Mol. Pharmacol. 67, 1137 (2005). | |
| TAT - NSF700 Fusion Peptide | YGRKKRRQRRR - GGG - LLDYVPIGPRFSNLVLQALLVL | his peptide is the N-Ethyl-maleimide-sensitive factor (NSF) inhibitor fusion polypeptide composed of 11-amino acid cell permeable HIV transactivating regulatory protein (TAT) domain fused to a 22 amino acid NSF domain. TAT-NSF700 inhibits thrombin-induced exocytosis of endothelial cells in a dose-responsive manner. | Matsushita, K. et al. Mol. Pharmacol. 67,1137 (2005). | |
| TAT - NSF700scr | YGRKKRRQRRRGGGIPPVYFSRLDLNLVVLLLAQL | This is a scrambled TAT-NSF222scr fusion polypeptide. It is composed of 11 amino acids from the cell permeable human immunodeficiency virus TAT polypeptide, 3 glycines as a linker, followed by scrambled N-Ethyl-maleimide-sensitive factor (NSF) D1 domain. This peptide is used as a control for the TAT-NSF222 peptide. | Matsushita, K. et al. Mol. Pharmacol. 67, 1137 (2005). | |
| TAT - NSF81scr Fusion Polypeptide , scrambled | YGRKKRRQRRR - GGG - QDGCKYFATDETIMKLSIAI | This peptide contains the TAT domain fused to 20 of N-Ethyl-maleimide-sensitive factor81 (NSF81) in a scrambled sequence. TAT-NSF81scr is used to measure the effect of the active and control peptides upon NSF activities and exocytosis. | Matsushita, K. et al. Mol Pharmacol 67, 1137 (2005). | |
| TAT (47 - 57) | YGRKKRRQRRR | This is the most characterized fragment of the HIV transactivator protein (TAT). This arginine-rich TAT peptide penetrates plasma membrane directly, but not through endocytosis. | Wang, H. et al. J. Clin. Invest. 109, 1463 (2002); Ziegler et al. Biochem. 44, 138 (2005); Wender, PA. et al. Proc. Natl. Acad. Sci. USA 97, 13003 (2000). | |
| Tat (48 - 57) | GRKKRRQRRR | This peptide is amino acid residues 48 to 57 fragment of the basic domain of HIV Tat. It contains the protein transduction domain (PTD) of the HIV Tat protein. | Hottiger, M. and G. Nabel, J. Virol. 72, 8252 (1998). | |
| TfR Targeting Peptide | THRPPMWSPVWP | This 12-mer peptide sequence is a transferrin receptor (TfR) targeting peptide. It binds to TfR and is internalized via endocytosis into TfR-expressing cells. TfR targeting peptide is a potential carrier for transportation of small molecules across the blood-brain barrier. | Wängler, C. et al. Mol Imaging Biol doi: 10.1007/s11307-010-0329-6, (2010). | |
| Transdermal Peptide | ACSSSPSKHCG | This short synthetic peptide facilitates efficient transdermal protein drug delivery through intact skin. Co-administration of the peptide and insulin to the abdominal skin of diabetic rats results in elevated systemic levels of insulin and suppresses serum glucose levels. This peptide creates a transient opening in the skin barrier to enable macromolecular drugs to reach systemic circulation. | Chen, Y. et al. Nat. Biotechnol. 24, 455 (2006). | |
| Transportan | GWTLNSAGYLLGKINLKALAALAKKIL | This peptide is Transportan (TP), a 27 amino acids (aa) long chimeric peptide containing 12 aa from the amino-terminal part of the neuropeptide galanin and the 14 aa long mastoparan (Vespula lewisii wasp venom), connected via a lysine residue. TP reveals some characteristic features of both galanin and mastoparan since it inhibits the binding of galanin to GALR-1 receptor as well as modulates the activity of G proteins due to the inhibition of GTPase activity. | Wierzbicki PM. Et al Folia Histochemica et Cytobiologica. 52(4):270-280 (2014). |