Literature summary for 3.4.22.15 extracted from

Dana, D.; Garcia, J.; Bhuiyan, A.I.; Rathod, P.; Joo, L.; Novoa, D.A.; Paroly, S.; Fath, K.R.; Chang, E.J.; Pathak, S.K.
Cell penetrable, clickable and tagless activity-based probe of human cathepsin L (2019), Bioorg. Chem., 85, 505-514 .

Search for more literature for 3.4.22.15

Application

Application	Comment	Organism
drug development	a clickable and tagless activity-based probe of cathepsin L probe is a highly effective tool in dissecting cathepsin L biology at the proteome levels in both normal physiology and human diseases, thereby facilitating drug-discovery efforts targeting cathepsin L	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
(2Z)-1-[(12R)-22-amino-12-[(1S)-2-(4-benzoylphenyl)-1-[[(benzyloxy)carbonyl]amino]ethyl]-6,13,22-trioxo-17,20-dioxa-7,14-diazadocos-1-yl]-2-[(2E)-3-(1-ethyl-3,3-dimethyl-5-sulfo-2,3-dihydro-1H-indol-2-yl)prop-2-en-1-ylidene]-3,3-dimethyl-2,3-dihydro-1H-indole-5-sulfonic acid	-	Homo sapiens
3-[(E)-(4-[[4-([2-[([[3-cyclohexyl-N-(morpholin-4-ylcarbonyl)-L-alanyl]amino][(6-[(2Z)-2-[(2E,4E,6Z)-7-(1-ethyl-3,3-dimethyl-5-sulfo-2,3-dihydro-1H-indol-2-yl)hepta-2,4,6-trien-1-ylidene]-3,3-dimethyl-5-sulfo-2,3-dihydro-1H-indol-1-yl]hexanoyl)amino]acetyl)amino]ethyl]amino)-4-oxobutyl](methyl)amino]phenyl)diazenyl]-7-(diethylamino)-5-phenylphenazin-5-ium	-	Homo sapiens
4-bromophenyl (1E,3S)-3-([N-[(benzyloxy)carbonyl]-L-phenylalanyl]amino)-5-methylhex-1-ene-1-sulfonate	i.e. KD-1	Homo sapiens
4-bromophenyl (S,E)-3-((S)-2-((((4-ethynylbenzyl)oxy)carbonyl)amino)-3-phenylpropanamido)-5-methylhex-1-ene-1-sulfonate	i.e. KDP-1, in vivo inhibition of cathepsin L. Inhibition of cathepsin L compared to other cathepsins, overview	Homo sapiens
E-64	a pan cysteine cathepsin inhibitor	Homo sapiens
additional information	development and synthesis of a clickable and tagless activity-based probes of cathepsin L, method, overview. The probe KDP-1 is highly efficient, active-site directed and activity-dependent, selective, cell penetrable, and non-toxic to human cells. Using a zebrafish model, it is schown that the probe can inhibit cathepsin L function in vivo during the hatching process. KDP-1 exhibits a strong time dependent inactivation of cathepsin L activity, although with about 10fold lower rate than KD-1	Homo sapiens
N-[6-[(6-[3,3-dimethyl-2-[(1E,3E,5E)-5-(1,3,3-trimethyl-1,3-dihydro-2H-indol-2-ylidene)penta-1,3-dien-1-yl]-3H-indolium-1-yl]hexanoyl)amino]hexanoyl]-L-histidyl-L-threonyl-N-[(2R)-1-(benzylsulfanyl)-4-[(2,6-dimethylbenzoyl)oxy]-3-oxobutan-2-yl]-2,3,4,5,6-pentafluoro-L-phenylalaninamide	-	Homo sapiens
N2-[(benzyloxy)carbonyl]-L-lysyl-N-[4-([[(5-methyl-7-oxo-7,8-dihydronaphthalen-2-yl)carbamoyl]oxy]methyl)phenyl]-L-lysinamide	-	Homo sapiens
Nalpha-[(benzyloxy)carbonyl]-N-[(3S)-7-[(6-[(2Z)-3,3-dimethyl-5-sulfo-2-[(2E,4E)-5-(1,3,3-trimethyl-5-sulfo-2,3-dihydro-1H-indol-2-yl)penta-2,4-dien-1-ylidene]-2,3-dihydro-1H-indol-1-yl]hexanoyl)amino]-2-oxo-1-(2,3,5,6-tetrafluoro-4-[[2-([[1-(2-[(3E)-3-(5-sulfo-2,3-dihydro-1H-indolium-1-ylidene)-6-(5-sulfo-2,3-dihydro-1H-indol-1-yl)-3H-xanthen-9-yl]benzene-1-sulfonyl)piperidin-4-yl]carbonyl]amino)ethyl]carbamoyl]phenoxy)heptan-3-yl]-L-phenylalaninamide	-	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P07711	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
breast cancer cell	-	Homo sapiens	-
commercial preparation	-	Homo sapiens	-
MDA-MB-231 cell	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
benzyloxycarbonyl-L-Phe-L-Arg-7-amido-4-methylcoumarin + H2O	-	Homo sapiens	benzyloxycarbonyl-L-Phe-L-Arg + 7-amino-4-methylcoumarin	-	?

Synonyms

Synonyms	Comment	Organism
cathepsin L1	-	Homo sapiens

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
5.6	-	assay at	Homo sapiens

General Information

General Information	Comment	Organism
evolution	cathepsin L is a member of the cysteine cathepsin protease family	Homo sapiens

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Release 2023.1 (January 2023)