Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T69707 Target Info
Target Name Proteasome (PS)
Target Type Successful Target
Gene Name NO-GeName
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 Collagen (CO) Successful Target
UniProt ID CP3A4_HUMAN; CP3A5_HUMAN; CP3A7_HUMAN; CP343_HUMAN
Gene Name NO-GeName
Representative Drug(s) Carfilzomib Drug Info IC50 = 490 nM [2]
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) Delanzomib Drug Info EC50 = 13.5 nM Click to Show More [3]
2 Bortezomib Drug Info IC50 = 520 nM [4]
Co-Target Name Glutathione S-transferase omega-1 (GSTO-1) Literature-reported Target
UniProt ID GSTO1_HUMAN
Gene Name GSTO1
Synonyms
SPG-R; S-(Phenacyl)glutathione reductase; Monomethylarsonic acid reductase; MMA(V) reductase; Glutathione-dependent dehydroascorbate reductase; Glutathione S-transferase omega 1-1; GSTTLP28; GSTO-1; GSTO 1-1
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Representative Drug(s) Carfilzomib Drug Info IC50 = 150 nM [5]
Co-Target Name Chymotrypsinogen B (CTRB1) Co-Target
UniProt ID CTRB1_HUMAN
Gene Name CTRB1
Representative Drug(s) Bortezomib Drug Info Ki = 320 nM [6]
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 Clinical pharmacokinetics, metabolism, and drug-drug interaction of carfilzomib. Drug Metab Dispos. 2013 Jan;41(1):230-7.
REF 3 Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives. J Med Chem. 2010 Oct 14;53(19):6779-810.
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 Reviewing Hit Discovery Literature for Difficult Targets: Glutathione Transferase Omega-1 as an Example. J Med Chem. 2018 Sep 13;61(17):7448-7470.
REF 6 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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