強力かつ選択的なCyaA阻害剤 、細胞膜上のアデニルシクラーゼ阻害剤
MANT* Nucleotides
Jena Bioscience makes available the largest selection of NANT nucleotide analogs. The blue-fluorescent MANT* nucleotide analogs have been used in biological research for several decades. Their modified ribose moiety is particularly useful for studying nucleotide-binding proteins that are sensitive to modifications of the nucleobase such as many GTPases. The compact nature of the MANT* fluorophore (Figure 1) results in fluorescent nucleotide analogs that induce minimal perturbation of nucleotide-protein interactions. MANT* fluorescence is highly sensitive to the environment of the fluorophore, thus making nucleotide-protein interactions easily detectable[1].
Figure 1: Structure of 2'/3'-O-MANT*-labeled nucleotides – monoacyl derivatives of cis-1,2-diols undergo isomerization by acyl migration, leading to an equilibrium of the 2'/3'-O-isomers
MANT*-nucleotides have recently been reported as:
- Potent and selective CyaA inhibitors (CyaA = calmodulin-activated adenylyl cyclase toxin) – the major virulence factor of whooping cough[2].
- Potent inhibitors of membranous adenylyl cyclases (ACs) – promising drug targets due to their key role in signal transduction[3],[4].
Selected references:
[1] Jameson et al. (1997) Fluorescent nucleotide analogs: synthesis and applications. Methods in Enzymology 278:363.
[2] Seifert et al. (2012) Towards selective inhibitors of adenylyl cyclase toxin from Bordetella pertussis. Trends in Microbiology 20(7):343.
[3] Pinto et al. (2011) Structure-activity relationships for the interactions of 2'- and 3'-(O)-(N-methyl)anthraniloyl-substituted purine and pyrimidine nucleotides with mammalian adenylyl cyclases. Biochemical Pharmacology 82:358.
[4] Seifert et al. (2012) Inhibitors of membranous adenylyl cyclases. Trends in Pharmacological Sciences 33(2):64.
[1] Jameson et al. (1997) Fluorescent nucleotide analogs: synthesis and applications. Methods in Enzymology 278:363.
[2] Seifert et al. (2012) Towards selective inhibitors of adenylyl cyclase toxin from Bordetella pertussis. Trends in Microbiology 20(7):343.
[3] Pinto et al. (2011) Structure-activity relationships for the interactions of 2'- and 3'-(O)-(N-methyl)anthraniloyl-substituted purine and pyrimidine nucleotides with mammalian adenylyl cyclases. Biochemical Pharmacology 82:358.
[4] Seifert et al. (2012) Inhibitors of membranous adenylyl cyclases. Trends in Pharmacological Sciences 33(2):64.
| Fluorescent analog | λabs [nm] | λem [nm] | εmax [l/(mol*cm)] | Notes/Advantages |
| 2',3'-Mant... | 355 | 448 | 5.8 | "THE CLASSICS" for small GTPases, heterotrimeric G-proteins, GPCRs, and motor protein kinetics. Small MW and environmentally sensitive fluorescence. FRET-probe for protein-intrinsic Tyr and Trp residues. |
| Mant-AMP | |||
| Product | Cat. No. | Amount | |
| S pack | NU-236S | 150 Units | http://www.jenabioscience.com/images/29c8187439/NU-236.pdf |
| L pack | NU-236L | 750 Units | |
| Mant-ADP | |||
| Product | Cat. No. | Amount | |
| S pack | NU-201S | 150 Units | http://www.jenabioscience.com/images/29c8187439/NU-201.pdf |
| L pack | NU-201L | 750 Units | |
| Mant-ATP | |||
| Product | Cat. No. | Amount | |
| S pack | NU-202S | 150 Units | http://www.jenabioscience.com/images/29c8187439/NU-202.pdf |
| L pack | NU-202L | 750 Units | |
| Mant-N6-Methyl-ATP | |||
| Product | Cat. No. | Amount | |
| S pack | NU-216S | 30 Units | http://www.jenabioscience.com/images/29c8187439/NU-216.pdf |
| L pack | NU-216L | 150 Units | |
| Mant-dATP | |||
| Product | Cat. No. | Amount | |
| S pack | NU-203S | 50 Units | http://www.jenabioscience.com/images/29c8187439/NU-203.pdf |
| L pack | NU-203L | 250 Units | |
| 2'-Mant-3'-dATP | |||
| Product | Cat. No. | Amount | |
| S pack | NU-223S | 20 Units | http://www.jenabioscience.com/images/29c8187439/NU-223.pdf |
| L pack | NU-223L | 100 Units | |
| Mant-AppNHp | |||
| Product | Cat. No. | Amount | |
| S pack | NU-214S | 10 Units | http://www.jenabioscience.com/images/29c8187439/NU-214.pdf |
| L pack | NU-214L | 50 Units | |
| Mant-ATPγS | |||
| Product | Cat. No. | Amount | |
| S pack | NU-232S | 20 Units | http://www.jenabioscience.com/images/29c8187439/NU-232.pdf |
| L pack | NU-232L | 100 Units | |
| Mant-GMP | |||
| Product | Cat. No. | Amount | |
| S pack | NU-237S | 150 Units | http://www.jenabioscience.com/images/29c8187439/NU-237.pdf |
| L pack | NU-237L | 750 Units | |
| Mant-GDP | |||
| Product | Cat. No. | Amount | |
| S pack | NU-204S | 150 Units | http://www.jenabioscience.com/images/29c8187439/NU-204.pdf |
| L pack | NU-204L | 750 Units | |
| Mant-dGDP | |||
| Product | Cat. No. | Amount | |
| S pack | NU-205S | 30 Units | http://www.jenabioscience.com/images/29c8187439/NU-205.pdf |
| L pack | NU-205L | 150 Units | |
| Mant-GTP | |||
| Product | Cat. No. | Amount | |
| S pack | NU-206S | 150 Units | http://www.jenabioscience.com/images/29c8187439/NU-206.pdf |
| L pack | NU-206L | 750 Units | |
| Mant-dGTP | |||
| Product | Cat. No. | Amount | |
| S pack | NU-212S | 50 Units | http://www.jenabioscience.com/images/29c8187439/NU-212.pdf |
| L pack | NU-212L | 250 Units | |
| NPE-caged-Mant-dGTP | |||
| Product | Cat. No. | Amount | |
| S pack | NU-303S | 10 Units | http://www.jenabioscience.com/images/91fdf4d49e/NU-303.pdf |
| L pack | NU-303L | 50 Units | |
| Mant-GppNHp (Mant-GMPPNP) | |||
| Product | Cat. No. | Amount | |
| S pack | NU-207S | 10 Units | http://www.jenabioscience.com/images/29c8187439/NU-207.pdf |
| L pack | NU-207L | 50 Units | |
| Mant-dGppNHp (Mant-dGMPPNP) | |||
| Product | Cat. No. | Amount | |
| S pack | NU-208S | 10 Units | http://www.jenabioscience.com/images/29c8187439/NU-208.pdf |
| L pack | NU-208L | 50 Units | |
| Mant-GTPγS | |||
| Product | Cat. No. | Amount | |
| S pack | NU-209S | 10 Units | http://www.jenabioscience.com/images/29c8187439/NU-209.pdf |
| L pack | NU-209L | 50 Units | |
| 2'-Mant-3'-dGTP | |||
| Product | Cat. No. | Amount | |
| S pack | NU-231S | 10 Units | http://www.jenabioscience.com/images/29c8187439/NU-231.pdf |
| L pack | NU-231L | 50 Units | |
| Mant-XDP | |||
| Product | Cat. No. | Amount | |
| S pack | NU-210S | 10 Units | http://www.jenabioscience.com/images/29c8187439/NU-210.pdf |
| L pack | NU-210L | 50 Units | |
| Mant-XTP | |||
| Product | Cat. No. | Amount | |
| S pack | NU-213S | 10 Units | http://www.jenabioscience.com/images/29c8187439/NU-213.pdf |
| L pack | NU-213L | 50 Units | |
| Mant-XppNHp (Mant-XMPPNP) | |||
| Product | Cat. No. | Amount | |
| S pack | NU-211S | 5 Units | http://www.jenabioscience.com/images/29c8187439/NU-211.pdf |
| L pack | NU-211L | 25 Units | |
| Mant-ITPγS | |||
| Product | Cat. No. | Amount | |
| S pack | NU-215S | 10 Units | http://www.jenabioscience.com/images/29c8187439/NU-215.pdf |
| L pack | NU-215L | 50 Units | |