Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T57361 Target Info
Target Name Kallikrein-related peptidase (KLK)
Synonyms
Human kallikrein
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Target Type Successful Target
Gene Name NO-GeName
Biochemical Class Peptidase
UniProt ID
NOUNIPROTAC
Co-Targets of This Target  Top
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 [1]
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 [2]
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 [3]
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 [4]
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 [5]
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 [5]
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 [6]
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 [7]
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 [3]
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 [7]
Co-Target Name Chymotrypsinogen B (CTRB1) Co-Target
UniProt ID CTRB1_HUMAN
Gene Name CTRB1
Representative Drug(s) Bortezomib Drug Info Ki = 320 nM [8]
References  Top
REF 1 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 2 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 3 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 4 Exploration of novel macrocyclic dipeptide N-benzyl amides as proteasome inhibitors. Eur J Med Chem. 2019 Feb 15;164:423-439.
REF 5 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 6 Oxathiazole-2-one derivative of bortezomib: Synthesis, stability and proteasome inhibition activity. Med. Chem. Commun. 2011;2:1083-1086.
REF 7 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 8 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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