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| [[Cathepsin]] (CTS) is a protease which becomes activated at low pH. It is found in lysosomes. Members of the CTS group are denoted as CTSA, CTSB etc and cleave proteins at different peptide bonds. The CTSs are expressed as an inactive precursor '''pro-CTS''' (PCTS) which becomes active when a long residue prosegment is cleaved off producing the mature CTS (MCTS).<ref>PMID:15751268</ref> For details on pro-CTS see [[Molecular Playground/Human PPCA]]. | | [[Cathepsin]] (CTS) is a protease which becomes activated at low pH. It is found in lysosomes. Members of the CTS group are denoted as CTSA, CTSB etc and cleave proteins at different peptide bonds. The CTSs are expressed as an inactive precursor '''pro-CTS''' (PCTS) which becomes active when a long residue prosegment is cleaved off producing the mature CTS (MCTS).<ref>PMID:15751268</ref> For details on pro-CTS see [[Molecular Playground/Human PPCA]]. |
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- | *'''CTS B, F, H, L, L1, L2''' are cysteine proteases.<br /> | + | *'''CTS B, F, H, L, L1, L2 or V''' are cysteine proteases.<br /> |
| *'''CTS D, E''' are aspartyl proteases which degrade insulin.<br /> | | *'''CTS D, E''' are aspartyl proteases which degrade insulin.<br /> |
| *'''CTS G''' is a serine protease with activity similar to chymotrypsin C.<br /> | | *'''CTS G''' is a serine protease with activity similar to chymotrypsin C.<br /> |
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| == Structural highlights == | | == Structural highlights == |
| | | |
- | CTS B is a cysteine protease. The <scene name='42/421669/Cv/4'>active site</scene> contains a <scene name='42/421669/Cv/10'>C29 residue from the N-terminal domain and H199 residue from the C-terminal domain</scene> (in cyan).<ref>PMID:21598397</ref> | + | CTS B is a cysteine protease. The <scene name='42/421669/Cv/11'>active site</scene> contains a <scene name='42/421669/Cv/13'>C26 residue from the N-terminal domain and H199 residue from the C-terminal domain</scene> (in cyan).<ref>PMID:21598397</ref> |
- | </StructureSection>
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| == 3D Structures of Cathepsin == | | == 3D Structures of Cathepsin == |
| + | [[Cathepsin 3D structures]] |
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- | Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}}
| + | </StructureSection> |
- | {{#tree:id=OrganizedByTopic|openlevels=0|
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- | | + | |
- | * Procathepsin-A (Lysosomal protective protein)
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- | | + | |
- | **[[4ci9]], [[1ivy]], [[4mws]], [[4mwt]] - hCTSB – human<br />
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- | **[[4cia]], [[4cib]] - hCTSB + inhibitor<br />
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- | | + | |
- | * Procathepsin-B
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- | | + | |
- | **[[1pbh]], [[2pbh]], [[3pbh]] – hPCTSB <br />
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- | **[[1mir]] - rPCTSB (mutant) - rat<br />
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- | **[[4n4z]], [[4hwy]] - TbCTSB – ''Trypanosoma brucei''<br />
| + | |
- | **[[5fpw]] – TbCTSB (mutant)<br />
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- | | + | |
- | * Cathepsin-B mature
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- | | + | |
- | **[[3hhi]] – TbCTSB (mutant) residues 23-340+CA074 <br />
| + | |
- | **[[3mor]] - TbCTSB residues 23-340<br />
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- | **[[3qsd]], [[3s3q]], [[3s3r]] - CTSB (mutant) residues 87-340+ inhibitor – ''Schistosoma mansoni''<br />
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- | **[[3k9m]] – hMCTSB+stefin A<br />
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- | **[[3ai8]] – hMCTSB + antibiotic<br />
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- | **[[2ipp]], [[1huc]] – hMCTSB<br />
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- | **[[3cbj]], [[3cbk]] – hMCTSB (mutant)+chagasin<br />
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- | **[[2dc6]], [[2dc7]], [[2dc8]], [[2dc9]], [[2dca]], [[2dcb]], [[2dcc]], [[2dcd]] – bMCTSB+inhibitor – bovine<br />
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- | **[[1sp4]], [[1csb]] – bMCTSB+epoxysuccinyl inhibitor<br />
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- | **[[1ito]], [[1qdq]] – bMCTSB +inhibitor<br />
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- | **[[1gmy]] - bMCTSB +dipeptidyl nitrile<br />
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- | **[[1the]] – rMCTSB (mutant)+butanone inhibitor – rat<br />
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- | **[[1cpj]] - rMCTSB (mutant)<br />
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- | **[[1cte]] - rMCTSB+pyrimidine inhibitor<br />
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- | | + | |
- | * Cathepsin-C mature or [[Dipeptidyl peptidase]]-I
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- | | + | |
- | **[[2djf]], [[2djg]], [[4oel]], [[4oem]] – hMCTSC + dipeptide<br />
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- | **[[1jqp]] – rMCTSC <br />
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- | **[[1k3b]] – hMCTSC <br />
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- | **[[3pdf]], [[4cdc]], [[4cdd]], [[4cde]], [[4cdf]] – hMCTSC + inhibitor<br />
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- | | + | |
- | * Cathepsin-D mature
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- | | + | |
- | **[[1lyw]], [[1lya]] – hMCTSD <br />
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- | **[[1lyb]] - hMCTSD+pepstatin<br />
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- | **[[4obz]], [[4oc6]], [[4od9]] – hMCTSD + non-peptidic inhibitor<br />
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- | | + | |
- | * Cathepsin-E mature
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- | | + | |
- | **[[1tzs]] – hMCTSE+activation peptide from CTSE<br />
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- | | + | |
- | * Cathepsin-F mature
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- | | + | |
- | **[[1m6d]] – hMCTSF+piperidine inhibitor<br />
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- | | + | |
- | * Cathepsin-G mature
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- | | + | |
- | **[[1kyn]] – hMCTSG +naphthalene inhibitor<br />
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- | **[[1au8]], [[1cgh]] - hMCTSG +phosphonate inhibitor<br />
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- | **[[1t32]] - hMCTSG +piperidine inhibitor
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- | | + | |
- | * Cathepsin-H mature
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- | | + | |
- | **[[1nb3]], [[1nb5]] – pMCTSH +stefin A – pig<br />
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- | **[[8pch]] - pMCTSH <br />
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- | | + | |
- | * Procathepsin-K
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- | | + | |
- | **[[1by8]], [[7pck]] – hPCTSK<br />
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- | | + | |
- | * Cathepsin-K mature
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- | | + | |
- | **[[4n79]], [[5tun]], [[4yva]] – hMCTSK<br />
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- | **[[5jh3]] – hMCTSK (mutant) <br />
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- | **[[5t6u]] – mMCTSK<br />
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- | **[[3o1g]], [[3n3g]], [[2r6n]], [[1bgo]], [[3kwz]], [[3kx1]], [[3o0u]] – hMCTSK+ pyrimidine inhibitor<br />
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- | **[[3mpe]], [[3mpf]] – hMCTSK (mutant) + pyrimidine inhibitor<br />
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- | **[[3h7d]] - hMCTSK (mutant) + chondroitin-4-sulfate<br />
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- | **[[3c9e]], [[4n8w]] - hMCTSK + chondroitin-4-sulfate<br />
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- | **[[3kwb]] - hMCTSK (mutant)+dioxo-triazine<br />
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- | **[[3kw9]] - hMCTSK +triazine<br />
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- | **[[1yk8]] - hMCTSK + cyanamide inhibitor<br />
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- | **[[1yt7]] - hMCTSK + ketoamide inhibitor<br />
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- | **[[2aux]], [[2auz]] - hMCTSK + semicarbazone inhibitor<br />
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- | **[[1ayu]], [[1ayv]], [[1ayw]] - hMCTSK + carbohydrazide inhibitor<br />
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- | **[[2bdl]], [[1yk7]], [[1tu6]], [[1au3]], [[1au4]], [[4dmx]], [[4dmy]] - hMCTSK + pyrrolidine inhibitor<br />
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- | **[[1snk]] - hMCTSK + norleucine inhibitor<br />
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- | **[[1nl6]], [[1nlj]] - hMCTSK+ azepanone inhibitor<br />
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- | **[[1q6k]] - hMCTSK+carbamate inhibitor<br />
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- | **[[1au0]] - hMCTSK+ diacylaminoethyl ketone inhibitor<br />
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- | **[[1au2]] - hMCTSK+ propanone inhibitor<br />
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- | **[[1atk]] – hMCTSK+guanidine inhibitor<br />
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- | **[[1vsn]], [[5j94]], [[4x6h]], [[4x6i]] - hMCTSK+ inhibitor<br />
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- | **[[2ato]] – hMCTSK+myocrisin<br />
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- | **[[1u9v]], [[1u9x]], [[1mem]] – hMCTSK+piperazine inhibitor<br />
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- | **[[1u9w]] - hMCTSK+imidazole inhibitor<br />
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- | **[[5tdi]] – hMCTSK + odanacatib<br />
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- | **[[5tdi]] – hMCTSK + lichostatinal<br />
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- | **[[5ja7]] – hMCTSK (mutant) + effector<br />
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- | **[[2ftd]] – MCTSK+azepan inhibitor – ''Macaca mulatta''<br />
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- | **[[2f7d]] – MCTSK (mutant)+nitrile inhibitor - rabbit<br />
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- | | + | |
- | *Procathepsin-L
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- | | + | |
- | **[[1cjl]], [[1cs8]] - hPCTS-L (mutant)<br />
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- | **[[3qj3]] - PCTS-L (mutant) – ''Tenebrio molitor''<br />
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- | | + | |
- | * Cathepsin-L mature
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- | | + | |
- | **[[3f75]] – MCTSL +CTSL propeptide – ''Toxoplasma gondii''<br />
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- | **[[2p86]] – TbMCTSL +K11002<br />
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- | **[[2nqd]] - CTSL residues 1-220 (mutant)+chagasin – ''Trypanosoma cruzi''<br />
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- | **[[4axl]] – hMCTSL catalytic domain<br />
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- | **[[4axm]] – hMCTSL catalytic domain + inhibitor<br />
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- | **[[1mhw]] – hMCTSL +tripeptide<br />
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- | **[[1icf]] – hMCTSL +MHC class II fragment<br />
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- | | + | |
- | * Procathepsin-L1
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- | | + | |
- | **[[2o6x]] – hPCTSL1 (mutant) – ''Fasciola hepatica''<br />
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- | | + | |
- | * Cathepsin-L1 mature
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- | | + | |
- | **[[4axl]] – hMCTSL1 catalytic domain<br />
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- | **[[3iv2]], [[5i4h]] – hMCTSL1 (mutant) <br />
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- | **[[3k24]] - hMCTSL1 (mutant) +tripeptide<br />
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- | **[[3of8]] - hMCTSL1 + dipeptidyl inhibitor<br />
| + | |
- | **[[2xu1]], [[2xu3]], [[2xu4]], [[2xu5]], [[2yj2]], [[2yj8]], [[2yj9]], [[2yjb]], [[2yjc]] - hMCTSL1 catalytic domain (mutant)+nitrile inhibitor<br />
| + | |
- | **[[3h89]], [[3h8b]], [[3h8c]] - hMCTSL1 (mutant) + retro-binding inhibitor<br />
| + | |
- | **[[3hwn]], [[3hha]] – hMCTSL1+pyrazole inhibitor<br />
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- | **[[3kse]] – hMCTSL1 (mutant)+stefin<br />
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- | **[[4axm]], [[5mae]], [[5maj]], [[5f02]], [[3bc3]], [[3of9]] – hMCTSL1 catalytic domain + inhibitor<br />
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- | | + | |
- | * Cathepsin-L2 mature
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- | | + | |
- | **[[3h6s]] – hMCTSL2+clitocypin<br />
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- | **[[1fh0]] – hMCTSL2 (mutant) +vinyl sulfone inhibitor<br />
| + | |
- | **[[3kfq]] - hMCTSL2 (mutant)+stefin
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- | | + | |
- | * Procathepsin-S
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- | | + | |
- | **[[2c0y]] – hPCTSS (mutant)<br />
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- | | + | |
- | * Cathepsin-S mature
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- | | + | |
- | **[[3n3g]], [[3n4c]] - hMCTSS+ pyrimidine inhibitor<br />
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- | **[[3ovx]] - hMCTSS+ aldehyde inhibitor<br />
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- | **[[3ovz]] - hMCTSS+ ketoamide inhibitor<br />
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- | **[[3kwn]] – hMCTSS (mutant)+ thioether acetamide<br />
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- | **[[3iej]] - hMCTSS (mutant)+pyrazole inhibitor<br />
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- | **[[2h7j]], [[2hxz]]- hMCTSS+triazole inhibitor<br />
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- | **[[2r9m]], [[2r9n]], [[2r9o]] – hMCTSS+piperidine inhibitor<br />
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- | **[[2op3]], [[2hhn]], [[2g7y]], [[2hh5]], [[2f1g]] – hMCTSS+aryl inhibitor<br />
| + | |
- | **[[2fud]], [[2fra]], [[2frq]], [[2ft2]], [[1npz]], [[1nqc]], [[4p6e]], [[4p6g]] – hMCTSS+inhibitor<br />
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- | **[[2fye]], [[2g6d]] – hMCTSS (mutant)+inhibitor<br />
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- | **[[2fq9]], [[1ms6]] – hMCTSS +nitrile inhibitor<br />
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- | **[[1glo]] - hMCTSS (mutant)<br />
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- | **[[4bs5]], [[4mzo]], [[4mzs]] - mMCTSS+ pyrrolidine inhibitor<br />
| + | |
- | **[[4bsq]] - mMCTSS+ morpholine inhibitor<br />
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- | **[[4bpv]], [[4bqv]], [[4bs6]] - mMCTSS +nitrile inhibitor<br />
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- | * Procathepsin-X
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- | | + | |
- | **[[1deu]] - hPCTSX<br />
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- | | + | |
- | * Cathepsin-X mature
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- | | + | |
- | **[[1ef7]] – hMCTSX<br />
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- | }}
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