Target Information
| Target General Information | Top | |||||
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| Target ID |
T57361
(Former ID: TTDR00005)
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| Target Name |
Kallikrein-related peptidase (KLK)
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| Synonyms |
Human kallikrein
Click to Show/Hide
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| Gene Name |
NO-GeName
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 4 Target-related Diseases | + | ||||
| 1 | Mature B-cell lymphoma [ICD-11: 2A85] | |||||
| 2 | Multiple myeloma [ICD-11: 2A83] | |||||
| 3 | Peptic ulcer [ICD-11: DA61] | |||||
| 4 | Retinal vascular occlusion [ICD-11: 9B74] | |||||
| BioChemical Class |
Peptidase
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| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 3 Approved Drugs | + | ||||
| 1 | Bortezomib | Drug Info | Approved | Multiple myeloma | [2], [3] | |
| 2 | Cetraxate | Drug Info | Approved | Peptic ulcer | [4] | |
| 3 | Ecallantide | Drug Info | Approved | Retina venous occlusion | [5], [6] | |
| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | LM-030 | Drug Info | Phase 2 | Congenital ichthyosiform erythroderma | [7] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Inhibitor | [+] 7 Inhibitor drugs | + | ||||
| 1 | Bortezomib | Drug Info | [8] | |||
| 2 | Ecallantide | Drug Info | [1] | |||
| 3 | LM-030 | Drug Info | [7] | |||
| 4 | Benzoxazinone derivative 2 | Drug Info | [10] | |||
| 5 | Benzyl amine derivative 1 | Drug Info | [10] | |||
| 6 | Benzyl amine derivative 2 | Drug Info | [10] | |||
| 7 | Heteroaryl-carboxamide derivative 11 | Drug Info | [10] | |||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | Cetraxate | Drug Info | [4], [9] | |||
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Ecallantide (DX-88), a plasma kallikrein inhibitor for the treatment of hereditary angioedema and the prevention of blood loss in on-pump cardiothoracic surgery. Expert Opin Biol Ther. 2008 Aug;8(8):1187-99. | |||||
| REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6391). | |||||
| REF 3 | New developments in immunosuppressive therapy for heart transplantation. Expert Opin Emerg Drugs. 2009 Mar;14(1):1-21. | |||||
| REF 4 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 5 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6955). | |||||
| REF 6 | ClinicalTrials.gov (NCT00969293) Study to Assess the Safety and Tolerability of a Single Administration of FOV2302 (Ecallantide) in Patients With Macular Edema Associated With Central Retinal Vein Occlusion. U.S. National Institutes of Health. | |||||
| REF 7 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 8 | Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin. J Med Chem. 1995 Apr 28;38(9):1511-22. | |||||
| REF 9 | A new broad spectrum inhibitor of esteroproteases, 4-(2-carboxyethyl) phenyl-trans-4-aminomethyl cyclohexane carboxylate hydrochloride (DV 1006). Tohoku J Exp Med. 1972 Mar;106(3):233-48. | |||||
| REF 10 | Serine protease inhibitors to treat inflammation: a patent review (2011-2016).Expert Opin Ther Pat. 2018 Feb;28(2):93-110. | |||||
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