Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T27602 | Target Info | |||
Target Name | Cationic trypsinogen (PRSS1) | ||||
Synonyms |
Trypsin-1; Trypsin I; TRYP1; TRY1; TRP1; Serine protease 1; Beta-trypsin
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Target Type | Successful Target | ||||
Gene Name | PRSS1 | ||||
Biochemical Class | Peptidase | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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Co-Target Name | Coagulation factor IIa (F2) | Successful Target | ||||
UniProt ID | THRB_HUMAN | |||||
Gene Name | F2 | |||||
Synonyms |
Prothrombin; Coagulation factor II
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Representative Drug(s) | MELAGATRAN | Drug Info | Ki = 1.2 nM | [1] | ||
Co-Target Name | Nuclear factor NF-kappa-B (NFKB) | Successful Target | ||||
UniProt ID | NFKB1_HUMAN; NFKB2_HUMAN; TF65_HUMAN; RELB_HUMAN; REL_HUMAN | |||||
Gene Name | NFKB1; NFKB2; RELA; RELB; REL | |||||
Synonyms |
Nuclear factor of kappa light polypeptide gene enhancer in B-cells; DNA-binding factor KBF
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Representative Drug(s) | Bortezomib | Drug Info | IC50 = 9.7 nM | [2] | ||
Co-Target Name | Plasminogen (PLG) | Successful Target | ||||
UniProt ID | PLMN_HUMAN | |||||
Gene Name | PLG | |||||
Synonyms |
Plasmin
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Representative Drug(s) | MELAGATRAN | Drug Info | Ki = 700 nM | [3] | ||
Co-Target Name | Tissue-type plasminogen activator (PLAT) | Successful Target | ||||
UniProt ID | TPA_HUMAN | |||||
Gene Name | PLAT | |||||
Synonyms |
TPA; T-plasminogen activator; T-PA; Reteplase; Alteplase
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Representative Drug(s) | MELAGATRAN | Drug Info | Ki = 900 nM | [3] | ||
Co-Target Name | Cathepsin G (CTSG) | Clinical trial Target | ||||
UniProt ID | CATG_HUMAN | |||||
Gene Name | CTSG | |||||
Synonyms |
CG
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Representative Drug(s) | Bortezomib | Drug Info | IC50 = 520 nM | [4] | ||
Co-Target Name | Proteasome beta-5 (PS beta-5) | Patented-recorded Target | ||||
UniProt ID | PSB5_HUMAN | |||||
Gene Name | PSMB5 | |||||
Synonyms |
Proteasome subunit beta type-5; Proteasome subunit X; Proteasome subunit MB1; Proteasome epsilon chain; Proteasome chain 6; Multicatalytic endopeptidase complex epsilon chain; Macropain epsilon chain; MB1; LMPX
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Representative Drug(s) | Bortezomib | Drug Info | IC50 = 0.5 nM | [5] | ||
Co-Target Name | Proteasome beta-9 (PS beta-9) | Patented-recorded Target | ||||
UniProt ID | PSB9_HUMAN | |||||
Gene Name | PSMB9 | |||||
Synonyms |
Really interesting new gene 12 protein; RING12; Proteasome subunit beta-1i; Proteasome subunit beta type-9; Proteasome chain 7; PSMB6i; Multicatalytic endopeptidase complex chain 7; Macropain chain 7; Low molecular mass protein 2; LMP2
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Representative Drug(s) | Bortezomib | Drug Info | IC50 = 3 nM | [6] | ||
Co-Target Name | Proteasome beta-8 (PS beta-8) | Patented-recorded Target | ||||
UniProt ID | PSB8_HUMAN | |||||
Gene Name | PSMB8 | |||||
Synonyms |
Y2; Really interesting new gene 10 protein; RING10; Proteasome subunit beta-5i; Proteasome subunit beta type-8; Proteasome component C13; PSMB5i; Multicatalytic endopeptidase complex subunit C13; Macropain subunit C13; Low molecular mass protein 7; LMP7
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Representative Drug(s) | Bortezomib | Drug Info | IC50 = 3.3 nM | [7] | ||
Co-Target Name | Proteasome beta-10 (PS beta-10) | Patented-recorded Target | ||||
UniProt ID | PSB10_HUMAN | |||||
Gene Name | PSMB10 | |||||
Synonyms |
Proteasome subunit beta-2i; Proteasome subunit beta type-10; Proteasome MECl-1; Multicatalytic endopeptidase complex subunit MECl-1; Macropain subunit MECl-1; MECL1; Low molecular mass protein 10; LMP10
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Representative Drug(s) | Bortezomib | Drug Info | IC50 = 940 nM | [7] | ||
Co-Target Name | 26S proteasome (PS 26S) | Co-Target | ||||
UniProt ID | ADRM1_HUMAN; PRS10_HUMAN; PRS4_HUMAN; PRS6A_HUMAN; PRS7_HUMAN; PRS8_HUMAN; PSD11_HUMAN; PSD12_HUMAN; PSD13_HUMAN; PSMD1_HUMAN; PSMD2_HUMAN; PSMD3_HUMAN; PSMD4_HUMAN; PSMD6_HUMAN; PSMD7_HUMAN; PSMD8_HUMAN; SEM1_HUMAN | |||||
Gene Name | NO-GeName | |||||
Representative Drug(s) | Bortezomib | Drug Info | IC50 = 2.56 nM | [8] | ||
Co-Target Name | Trypsin (TRY) | Co-Target | ||||
UniProt ID | TRY1_HUMAN; TRY2_HUMAN; TRY3_HUMAN | |||||
Gene Name | PRSS1; PRSS2; PRSS3 | |||||
Representative Drug(s) | MELAGATRAN | Drug Info | Ki = 4.3 nM | [9] | ||
Co-Target Name | 20S proteasome (PS 20S) | Co-Target | ||||
UniProt ID | PSA1_HUMAN; PSA2_HUMAN; PSA3_HUMAN; PSA4_HUMAN; PSA5_HUMAN; PSA6_HUMAN; PSA7_HUMAN; PSB1_HUMAN; PSB2_HUMAN; PSB3_HUMAN; PSB4_HUMAN; PSB5_HUMAN; PSB6_HUMAN; PSB7_HUMAN; PSB8_HUMAN; PSB9_HUMAN; PSB10_HUMAN; PSB11_HUMAN; PSMA8_HUMAN | |||||
Gene Name | NO-GeName | |||||
Representative Drug(s) | Bortezomib | Drug Info | IC50 = 10.8 nM | [10] | ||
Co-Target Name | Proteasome component C5 (PSMB1) | Co-Target | ||||
UniProt ID | PSB1_HUMAN | |||||
Gene Name | PSMB1 | |||||
Synonyms |
Proteasome subunit beta type-1; Macropain subunit C5; Multicatalytic endopeptidase complex subunit C5; Proteasome gamma chain
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Representative Drug(s) | Bortezomib | Drug Info | IC50 = 19 nM | [5] | ||
Co-Target Name | Proteasome subunit beta type-2 (PSMB2) | Co-Target | ||||
UniProt ID | PSB2_HUMAN | |||||
Gene Name | PSMB2 | |||||
Synonyms |
Macropain subunit C7-I; Multicatalytic endopeptidase complex subunit C7-I; Proteasome component C7-I
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Representative Drug(s) | Bortezomib | Drug Info | IC50 = 128 nM | [10] | ||
Co-Target Name | Chymotrypsinogen B (CTRB1) | Co-Target | ||||
UniProt ID | CTRB1_HUMAN | |||||
Gene Name | CTRB1 | |||||
Representative Drug(s) | Bortezomib | Drug Info | Ki = 320 nM | [11] |
References | Top | ||||
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REF 1 | Noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1. Bioorg Med Chem Lett. 2002 Apr 8;12(7):1017-22. | ||||
REF 2 | Optimization of a series of dipeptides with a P3 beta-neopentyl asparagine residue as non-covalent inhibitors of the chymotrypsin-like activity of human 20S proteasome. Medchemcomm. 2012;3:710-9. | ||||
REF 3 | Fibrinolysis Inhibitors: Potential Drugs for the Treatment and Prevention of Bleeding. J Med Chem. 2020 Feb 27;63(4):1445-1472. | ||||
REF 4 | Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer. J Med Chem. 2008 Feb 28;51(4):1068-72. | ||||
REF 5 | Ridaifen-F conjugated with cell-penetrating peptides inhibits intracellular proteasome activities and induces drug-resistant cell death. Eur J Med Chem. 2018 Feb 25;146:636-650. | ||||
REF 6 | Exploration of novel macrocyclic dipeptide N-benzyl amides as proteasome inhibitors. Eur J Med Chem. 2019 Feb 15;164:423-439. | ||||
REF 7 | Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases. Eur J Med Chem. 2019 Nov 15;182:111646. | ||||
REF 8 | Oxathiazole-2-one derivative of bortezomib: Synthesis, stability and proteasome inhibition activity. Med. Chem. Commun. 2011;2:1083-1086. | ||||
REF 9 | Antithrombotic effects of LB30870, a potent, orally active, selective and direct thrombin inhibitor, and pharmacokinetics of its prodrug. Bioorg Med Chem Lett. 2013 Sep 1;23(17):4779-84. | ||||
REF 10 | Covalent docking modelling-based discovery of tripeptidyl epoxyketone proteasome inhibitors composed of aliphatic-heterocycles. Eur J Med Chem. 2019 Feb 15;164:602-614. | ||||
REF 11 | Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids. Bioorg Med Chem Lett. 1998 Feb 17;8(4):333-8. |
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