Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T31309 | Target Info | |||
| Target Name | Apoptosis regulator Bcl-2 (BCL-2) | ||||
| Synonyms |
Bcl-2
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| Target Type | Successful Target | ||||
| Gene Name | BCL2 | ||||
| Biochemical Class | B-cell lymphoma Bcl-2 | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Tubulin (TUB) | Successful Target | ||||
| UniProt ID | TBA1A_HUMAN; TBA1B_HUMAN; TBA1C_HUMAN; TBA3C_HUMAN; TBA3E_HUMAN; TBA4A_HUMAN; TBB1_HUMAN; TBB2A_HUMAN; TBB2B_HUMAN; TBB3_HUMAN; TBB4A_HUMAN; TBB4B_HUMAN; TBB5_HUMAN; TBB6_HUMAN; TBB8_HUMAN | |||||
| Gene Name | NO-GeName | |||||
| Synonyms |
Human tubulin
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| Representative Drug(s) | Taxol | Drug Info | EC50 = 31 nM | [1] | ||
| Co-Target Name | Human immunodeficiency virus Reverse transcriptase (HIV RT) | Successful Target | ||||
| UniProt ID | POL_HV1B1 | |||||
| Gene Name | HIV RT | |||||
| Synonyms |
HIV p66 RT; HIV Exoribonuclease H
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| Representative Drug(s) | Taxol | Drug Info | IC50 ~ 200 ug.mL-1 | [2] | ||
| Co-Target Name | Aldose reductase (AKR1B1) | Successful Target | ||||
| UniProt ID | ALDR_HUMAN | |||||
| Gene Name | AKR1B1 | |||||
| Synonyms |
Aldehyde reductase; AKR1B1
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| Representative Drug(s) | Gossypol | Drug Info | Ki = 500 nM | [3] | ||
| Co-Target Name | Hepatitis C virus NS3 helicase (HCV NS3) | Successful Target | ||||
| UniProt ID | POLG_HCV1 (1027-1657) | |||||
| Gene Name | HCV NS3 | |||||
| Synonyms |
HCV Hepacivirin; HCV NS3P; HCV p70
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| Representative Drug(s) | Taxol | Drug Info | IC50 ~ 1000 nM | [4] | ||
| Co-Target Name | Apoptosis regulator Bcl-xL (BCL-xL) | Clinical trial Target | ||||
| UniProt ID | B2CL1_HUMAN | |||||
| Gene Name | BCL2L1 | |||||
| Synonyms |
Bcl2like protein 1; Bcl2L1; Bcl2-L-1; Bcl-XL; Bcl-2-like protein 1; BCLX; BCL2L; Apoptosis regulator Bcl-X
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| Representative Drug(s) | ABT-263 | Drug Info | Ki = 0.055 nM | Click to Show More | [5] | |
| 2 | GDC-0199 | Drug Info | Ki = 48 nM | [8] | ||
| 3 | Gossypol | Drug Info | Ki = 310 nM | [11] | ||
| 4 | Obatoclax | Drug Info | EC50 = 900 nM | [12] | ||
| Co-Target Name | Induced myeloid leukemia cell differentiation protein Mcl-1 (MCL1) | Clinical trial Target | ||||
| UniProt ID | MCL1_HUMAN | |||||
| Gene Name | MCL1 | |||||
| Synonyms |
mcl1/EAT; Bcl2-L-3; Bcl-2-related protein EAT/mcl1; Bcl-2-like protein 3; BCL2L3
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| Representative Drug(s) | ABT-263 | Drug Info | Ki < 1 nM | Click to Show More | [6] | |
| 2 | Gossypol | Drug Info | Ki = 162 nM | [10] | ||
| 3 | GDC-0199 | Drug Info | Ki ~ 444 nM | [8] | ||
| 4 | Obatoclax | Drug Info | EC50 = 500 nM | [12] | ||
| Co-Target Name | Integrin alpha-V/beta-3 (ITGAV/B3) | Clinical trial Target | ||||
| UniProt ID | ITAV_HUMAN-ITB3_HUMAN | |||||
| Gene Name | ITGAV-ITGB3 | |||||
| Synonyms |
Integrin alphaVbeta3; Integrin alpha-v beta-3; Integrin alpha V beta 3; Alpha(v)beta(3) Integrin; Alpha v beta 3 integrin
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| Representative Drug(s) | Taxol | Drug Info | IC50 = 34 nM | [7] | ||
| Co-Target Name | Apoptosis regulator Bcl-W (BCL-W) | Clinical trial Target | ||||
| UniProt ID | B2CL2_HUMAN | |||||
| Gene Name | BCL2L2 | |||||
| Synonyms |
KIAA0271; Bcl2-L-2; Bcl-2-like protein 2; BCLW
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| Representative Drug(s) | ABT-263 | Drug Info | IC50 = 70 nM | Click to Show More | [9] | |
| 2 | GDC-0199 | Drug Info | Ki = 245 nM | [8] | ||
| 3 | Obatoclax | Drug Info | Ki = 1000 nM | [13] | ||
| Co-Target Name | Bcl-2-related protein A1 (BCL2A1) | Patented-recorded Target | ||||
| UniProt ID | B2LA1_HUMAN | |||||
| Gene Name | BCL2A1 | |||||
| Synonyms |
Protein GRS; Protein BFL-1; Hemopoietic-specific early response protein; HBPA1; GRS; Bcl2-L-5; Bcl-2-like protein 5; BFL1; BCL2L5
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| Representative Drug(s) | Obatoclax | Drug Info | EC50 = 600 nM | [12] | ||
| Co-Target Name | Liver organic anion transporter 2 (SLCO1B3) | Literature-reported Target | ||||
| UniProt ID | SO1B3_HUMAN | |||||
| Gene Name | SLCO1B3 | |||||
| Synonyms |
Solute carrier organic anion transporter family member 1B3; Solute carrier family 21 member 8; SLC21A8; Organic anion-transporting polypeptide 8; Organic anion transporter 8; OATP8; OATP1B3; OATP-8; Liver-specific organic anion transporter 2; LST2; LST-2
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| Representative Drug(s) | Taxol | Drug Info | IC50 = 260 nM | [14] | ||
| Co-Target Name | Liver organic anion transporter 1 (SLCO1B1) | Literature-reported Target | ||||
| UniProt ID | SO1B1_HUMAN | |||||
| Gene Name | SLCO1B1 | |||||
| Synonyms |
Solute carrier organic anion transporter family member 1B1; Solute carrier family 21 member 6; Sodium-independent organic anion-transporting polypeptide 2; SLC21A6; OATPC; OATP2; OATP-C; OATP-2; Liver-specific organic anion transporter 1; LST1; LST-1
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| Representative Drug(s) | Taxol | Drug Info | IC50 = 280 nM | [14] | ||
| Co-Target Name | Bcl2-antagonist of cell death (BAD) | Co-Target | ||||
| UniProt ID | BAD_HUMAN | |||||
| Gene Name | BAD | |||||
| Synonyms |
Bcl2-associated agonist of cell death; BAD; Bcl-2-binding component 6; Bcl-2-like protein 8; Bcl2-L-8; Bcl-xL/Bcl-2-associated death promoter; Bcl2 antagonist of cell death
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| Representative Drug(s) | ABT-263 | Drug Info | Ki < 0.5 nM | Click to Show More | [15] | |
| 2 | Obatoclax | Drug Info | Ki = 1000 nM | [13] | ||
| Co-Target Name | Tubulin beta-3 chain (TUBB3) | Co-Target | ||||
| UniProt ID | TBB3_HUMAN | |||||
| Gene Name | TUBB3 | |||||
| Synonyms |
Tubulin beta-4 chain; Tubulin beta-III
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| Representative Drug(s) | Taxol | Drug Info | IC50 = 7.7 nM | [16] | ||
| Co-Target Name | Bcl-2-like protein 10 (BCL2L10) | Co-Target | ||||
| UniProt ID | B2L10_HUMAN | |||||
| Gene Name | BCL2L10 | |||||
| Synonyms |
Bcl2-L-10; Anti-apoptotic protein NrH; Apoptosis regulator Bcl-B
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| Representative Drug(s) | Obatoclax | Drug Info | Ki = 1000 nM | [13] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Privileged structure-based quinazolinone natural product-templated libraries: identification of novel tubulin polymerization inhibitors. Bioorg Med Chem Lett. 2006 Feb;16(3):686-90. | ||||
| REF 2 | Evaluation of natural products as inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. J Nat Prod. 1991 Jan-Feb;54(1):143-54. | ||||
| REF 3 | Gossypol and derivatives: a new class of aldose reductase inhibitors. J Med Chem. 1991 Nov;34(11):3301-5. | ||||
| REF 4 | Control of hepatitis C: a medicinal chemistry perspective. J Med Chem. 2005 Jan 13;48(1):1-20. | ||||
| REF 5 | Beyond the Rule of 5: Lessons Learned from AbbVie's Drugs and Compound Collection. J Med Chem. 2018 Apr 12;61(7):2636-51. | ||||
| REF 6 | The chemical biology of apoptosis: Revisited after 17 years. Eur J Med Chem. 2019 Sep 1;177:63-75. | ||||
| REF 7 | Synthesis and biological evaluation of dimeric RGD peptide-paclitaxel conjugate as a model for integrin-targeted drug delivery. J Med Chem. 2005 Feb 24;48(4):1098-106. | ||||
| REF 8 | Expanding the Cancer Arsenal with Targeted Therapies: Disarmament of the Antiapoptotic Bcl-2 Proteins by Small Molecules. J Med Chem. 2017 Feb 9;60(3):821-838. | ||||
| REF 9 | Discovery and optimization of covalent Bcl-xL antagonists. Bioorg Med Chem Lett. 2019 Dec 1;29(23):126682. | ||||
| REF 10 | Gossypol with Hydrophobic Linear Esters Exhibits Enhanced Antitumor Activity as an Inhibitor of Antiapoptotic Proteins. ACS Med Chem Lett. 2016 Oct 19;7(12):1185-90. | ||||
| REF 11 | Structural modification of luteolin from Flos Chrysanthemi leads to increased tumor cell growth inhibitory activity. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3464-7. | ||||
| REF 12 | Synthesis and biological activities of polyquinoline derivatives: new Bcl-2 family protein modulators. Eur J Med Chem. 2012 Nov;57:112-25. | ||||
| REF 13 | Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19512-7. | ||||
| REF 14 | Interaction of human organic anion transporter polypeptides 1B1 and 1B3 with antineoplastic compounds. Eur J Med Chem. 2015 Mar 6;92:723-31. | ||||
| REF 15 | Recent developments in fragment-based drug discovery. J Med Chem. 2008 Jul 10;51(13):3661-80. | ||||
| REF 16 | Structure-activity relationship and in vitro and in vivo evaluation of the potent cytotoxic anti-microtubule agent N-(4-methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride and its analogues as antitumor agents. J Med Chem. 2013 Sep 12;56(17):6829-44. | ||||
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