| Target
Information |
| Name | Cathepsin L |
| Type of target | Research target |
| Synonyms | MEP |
| Major excreted protein |
| Disease | Autoimmune diseases
[ICD9: 279.4 ICD10: D84.9, M35.9] | [1] |
Melanoma
[ICD9: 172 ICD10: C43] | [1] |
| BioChemical Class | Hydrolases acting on peptide bonds (Peptidases) |
| EC Number | EC 3.4.22.15 |
| Pathway | Antigen processing and presentation |
| Lysosome |
| UniProt ID | P07711 |
| PDB Structure | 1CJL; 1CS8; 1ICF; 1MHW; 2NQD; 2VHS; 2XU1; 2XU3; 2XU4; 2XU5; 2YJ2; 2YJ8; 2YJ9; 2YJB; 2YJC; 3BC3; 3H89; 3H8B; 3H8C; 3HHA; 3HWN; 3IV2; 3K24; 3KSE; 3OF8; 3OF9; 4AXL; 4AXM. |
| Function | Important for the overall degradation of proteins in lysosomes. |
| Sequence | MNPTLILAAFCLGIASATLTFDHSLEAQWTKWKAMHNRLYGMNEEGWRRAVWEKNMKMIE
LHNQEYREGKHSFTMAMNAFGDMTSEEFRQVMNGFQNRKPRKGKVFQEPLFYEAPRSVDW
REKGYVTPVKNQGQCGSCWAFSATGALEGQMFRKTGRLISLSEQNLVDCSGPQGNEGCNG
GLMDYAFQYVQDNGGLDSEESYPYEATEESCKYNPKYSVANDTGFVDIPKQEKALMKAVA
TVGPISVAIDAGHESFLFYKEGIYFEPDCSSEDMDHGVLVVGYGFESTESDNNKYWLVKN
SWGEEWGMGGYVKMAKDRRNHCGIASAASYPTV
|
| Related US Patent | 6,313,119 |
| 6,420,364 |
| 6,436,925 |
| 6,455,502 |
| 6,476,026 |
| 6,492,362 |
| 6,525,036 |
| 6,525,052 |
| 6,576,630 |
| 6,593,327 |
| 6,608,057 |
| 6,635,621 |
| 6,649,642 |
| Target Validation | Click to Find Target Validation Information. |
| Inhibitor | (3-Bromobenzoylpyridine)thiosemicarbazone |  | [2] |
| (S)-1-benzylcyclopentyl 1-oxohexan-2-ylcarbamate | | [3] |
| (S)-tert-butyl 1-oxohexan-2-ylcarbamate | | [3] |
| 1- (1,3-diphenylpropylidene)thiosemicarbazide | | [4] |
| 1- (phenyl | | [4] |
| 6- (benzylamino)-9-butyl-9H-purine-2-carbonitrile | | [5] |
| 9-benzyl-6- (benzylamino)-9H-purine-2-carbonitrile | | [5] |
| BIPHENYL-4-YL-ACETALDEHYDE | | [6] |
| BOCEPREVIR | | [7] |
| Bis (3-Fluorophenyl)-ketone]thiosemicarbazone | | [8] |
| Bis (3-bromophenyl) | | [2] |
| Bis (3-bromophenyl) | | [2] |
| Cysteinesulfonic Acid | | [9] |
| L-006235-1 | | [10] |
| L-873724 | | [11] |
| MDL-2170, MDL-28170 | | [12] |
| N- (4-phenylbenzoyl)-phenylalanyl-glycine-nitrile | | [13] |
| N- (benzyloxycarbonyl)-leucyl-glycine-nitrile | | [13] |
| N- (tert-butoxycarbonyl)-isoleucyl-glycine-nitrile | | [13] |
| N- (tert-butoxycarbonyl)-leucyl-glycine-nitrile | | [13] |
| N- (tert-butoxycarbonyl)-methionyl-glycine-nitrile | | [13] |
| N- (tert-butoxycarbonyl)-norleucyl-glycine-nitrile | | [13] |
| N- (tert-butoxycarbonyl)-tyrosyl-glycine-nitrile | | [13] |
| N- (tert-butoxycarbonyl)-valyl-glycine-nitrile | | [13] |
| N-acetyl-phenylalanyl-glycine-nitrile | | [13] |
| N-benzoyl-phenylalanyl-glycine-nitrile | | [13] |
| PEPSTATIN A | | [12] |
| [ (3-Bromophenyl)-m-tolyl-ketone]thiosemicarbazone | | [8] |
| [ (3-Bromophenyl)-p-tolyl-ketone]thiosemicarbazone | | [8] |
| [2-Phenylacetophenone]thiosemicarbazone | | [2] |
| Cross References |
3D Structure
Related Literature
On-Line
Medical Dictionary |
| Ref 1 | Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. To Reference |
| Ref 2 | Bioorg Med Chem Lett. 2010 Nov 15;20(22):6610-5. Epub 2010 Sep 15.Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L. To Reference |
| Ref 3 | Bioorg Med Chem Lett. 2006 Feb 15;16(4):978-83. Epub 2005 Nov 15.Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors? To Reference |
| Ref 4 | Bioorg Med Chem Lett. 2008 May 1;18(9):2883-5. Epub 2008 Apr 8.Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB. To Reference |
| Ref 5 | J Med Chem. 2008 Feb 14;51(3):545-52. Epub 2008 Jan 4.Development of potent purine-derived nitrile inhibitors of the trypanosomal protease TbcatB. To Reference |
| Ref 6 | Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference |
| Ref 7 | Antimicrob Agents Chemother. 2010 Jan;54(1):305-11. Epub 2009 Oct 19.MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. To Reference |
| Ref 8 | Bioorg Med Chem Lett. 2010 Feb 15;20(4):1415-9. Epub 2010 Jan 6.Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors. To Reference |
| Ref 9 | Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference |
| Ref 10 | J Med Chem. 2005 Dec 1;48(24):7535-43.Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. To Reference |
| Ref 11 | Bioorg Med Chem Lett. 2007 Sep 1;17(17):4929-33. Epub 2007 Jun 10.The identification of potent, selective, and bioavailable cathepsin S inhibitors. To Reference |
| Ref 12 | J Med Chem. 2009 May 14;52(9):3093-7.Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity. To Reference |
| Ref 13 | J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles. To Reference |
