|
|
| Line 26: |
Line 26: |
| **[[2bm2]], [[2fww]] - hTRP-β2 + piperidine derivative<br /> | | **[[2bm2]], [[2fww]] - hTRP-β2 + piperidine derivative<br /> |
| **[[5f03]] - hTRP-β2 + oxazolidine derivative<br /> | | **[[5f03]] - hTRP-β2 + oxazolidine derivative<br /> |
| **[[4a6l]] - hTRP-α/β1 + piperidine derivative<br /> | | **[[4a6l]], [[6p0p]] - hTRP-α/β1 + piperidine derivative<br /> |
| **[[4mpu]], [[4mpv]], [[4mpw]], [[4mpx]], [[4mqa]] - hTRP-α/β1 + drug<br /> | | **[[4mpu]], [[4mpv]], [[4mpw]], [[4mpx]], [[4mqa]] - hTRP-α/β1 + drug<br /> |
| **[[6o1f]] - hTRP-α/β1 + trypsin inhibitor + antibody<br /> | | **[[6o1f]] - hTRP-α/β1 + trypsin inhibitor + antibody<br /> |
Revision as of 10:03, 21 December 2020
| Function
Tryptase (TRP) is a serine protease found in mast cells[1].
Relevance
TRP is used as a marker for mast cell activation[2]. Inhibitors of TRP have therapeutic potential for treating allergic or inflammatory disorders such as asthma and inflammatory bowel diseases[3].
Structural highlights
The biological assembly of Human tryptase is homotetramer (2zeb). The piperidine derivative TRP inhibitor interacts with both subunits of TRP[4]. Water molecules are shown as red spheres.
- ↑ Payne V, Kam PC. Mast cell tryptase: a review of its physiology and clinical significance. Anaesthesia. 2004 Jul;59(7):695-703. PMID:15200544 doi:https://dx.doi.org/10.1111/j.1365-2044.2004.03757.x
- ↑ Proud D, Bailey GS, Naclerio RM, Reynolds CJ, Cruz AA, Eggleston PA, Lichtenstein LM, Togias AG. Tryptase and histamine as markers to evaluate mast cell activation during the responses to nasal challenge with allergen, cold, dry air, and hyperosmolar solutions. J Allergy Clin Immunol. 1992 Jun;89(6):1098-110. PMID:1607547
- ↑ Hallgren J, Pejler G. Biology of mast cell tryptase. An inflammatory mediator. FEBS J. 2006 May;273(9):1871-95. PMID:16640553 doi:https://dx.doi.org/10.1111/j.1742-***************.x
- ↑ Costanzo MJ, Yabut SC, Zhang HC, White KB, de Garavilla L, Wang Y, Minor LK, Tounge BA, Barnakov AN, Lewandowski F, Milligan C, Spurlino JC, Abraham WM, Boswell-Smith V, Page CP, Maryanoff BE. Potent, nonpeptide inhibitors of human mast cell tryptase. Synthesis and biological evaluation of novel spirocyclic piperidine amide derivatives. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2114-21. Epub 2008 Jan 30. PMID:18272363 doi:10.1016/j.bmcl.2008.01.093
|
3D Structures of tryptase
Updated on 21-December-2020
{"openlevels":0}
- Tryptase
- 2zeb – hTRP-α1 - human
- 2f9o - hTRP-α1 (mutant)
- 5wi6 - hTRP-α/β1 (mutant)
- Tryptase complex with inhibitor
- 1a0l – hTRP-β + APPA
- 2f9n, 2f9p - hTRP-α1 (mutant) + leupeptin
- 2bm2, 2fww - hTRP-β2 + piperidine derivative
- 5f03 - hTRP-β2 + oxazolidine derivative
- 4a6l, 6p0p - hTRP-α/β1 + piperidine derivative
- 4mpu, 4mpv, 4mpw, 4mpx, 4mqa - hTRP-α/β1 + drug
- 6o1f - hTRP-α/β1 + trypsin inhibitor + antibody
- 2fxr - hTRP-β2 + ketone inhibitor
- 2fpz - hTRP-β2 + benzimidazole inhibitor
- 2fs9, 2fs8, 2gdd, 2za5, 2zeb, 2zec - hTRP-β2 + inhibitor
- 3v7t - hTRP-β2 + tropanylamide inhibitor
References
