Urea-containing peptide boronic acids as potent proteasome inhibitors
A novel class of urea-containing peptide boronic acids as proteasome inhibitors was designed by introducing a urea scaffold to replace an amido bond. Compounds were synthesized and their antitumor activities were evaluated. After two rounds of optimizations, the compound I-14 was found to be a poten...
Ausführliche Beschreibung
Gespeichert in:
| Autor*in: |
Han, Li-Qiang [verfasserIn] |
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| Format: |
E-Artikel |
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| Sprache: |
Englisch |
| Erschienen: |
2017transfer abstract |
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| Umfang: |
15 |
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| Übergeordnetes Werk: |
Enthalten in: Electrochemical synthesis, photodegradation and antibacterial properties of PEG capped zinc oxide nanoparticles - Jose, Ajay ELSEVIER, 2018, Amsterdam [u.a.] |
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| Übergeordnetes Werk: |
volume:125 ; year:2017 ; day:5 ; month:01 ; pages:925-939 ; extent:15 |
| Links: |
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| DOI / URN: |
10.1016/j.ejmech.2016.10.023 |
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| 520 | |a A novel class of urea-containing peptide boronic acids as proteasome inhibitors was designed by introducing a urea scaffold to replace an amido bond. Compounds were synthesized and their antitumor activities were evaluated. After two rounds of optimizations, the compound I-14 was found to be a potent proteasome inhibitor. Compared with Bortezomib, I-14 showed higher potency against the chymotrypsin-like activity of human 20S proteasome (IC50 < 1 pM), similar potency against four different cancer cell lines (IC50 < 10 nM), and better pharmacokinetic profile. Furthermore, I-14 significantly inhibited tumor growth in Bel7404 mouse xenograft model. The excellent proteasome inhibition by I-14 was rationalized through docking and molecular dynamics studies. | ||
| 520 | |a A novel class of urea-containing peptide boronic acids as proteasome inhibitors was designed by introducing a urea scaffold to replace an amido bond. Compounds were synthesized and their antitumor activities were evaluated. After two rounds of optimizations, the compound I-14 was found to be a potent proteasome inhibitor. Compared with Bortezomib, I-14 showed higher potency against the chymotrypsin-like activity of human 20S proteasome (IC50 < 1 pM), similar potency against four different cancer cell lines (IC50 < 10 nM), and better pharmacokinetic profile. Furthermore, I-14 significantly inhibited tumor growth in Bel7404 mouse xenograft model. The excellent proteasome inhibition by I-14 was rationalized through docking and molecular dynamics studies. | ||
| 650 | 7 | |a Proteasome inhibitor |2 Elsevier | |
| 650 | 7 | |a Structure-activity relationship |2 Elsevier | |
| 650 | 7 | |a Anti-tumor activity |2 Elsevier | |
| 650 | 7 | |a Low toxicity |2 Elsevier | |
| 650 | 7 | |a Urea-containing peptide boronic acids |2 Elsevier | |
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| 700 | 1 | |a Li, Ri-Dong |4 oth | |
| 700 | 1 | |a Xu, Bo |4 oth | |
| 700 | 1 | |a Cheng, Qing |4 oth | |
| 700 | 1 | |a Liu, Zhen-Ming |4 oth | |
| 700 | 1 | |a Zhou, Tian-Yan |4 oth | |
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| 700 | 1 | |a Wang, Xin |4 oth | |
| 700 | 1 | |a Cheng, Tie-Ming |4 oth | |
| 700 | 1 | |a Ge, Ze-Mei |4 oth | |
| 700 | 1 | |a Cui, Jing-Rong |4 oth | |
| 700 | 1 | |a Li, Run-Tao |4 oth | |
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10.1016/j.ejmech.2016.10.023 doi GBVA2017007000009.pica (DE-627)ELV020124953 (ELSEVIER)S0223-5234(16)30886-8 DE-627 ger DE-627 rakwb eng 610 610 DE-600 570 540 VZ BIODIV DE-30 fid 42.00 bkl Han, Li-Qiang verfasserin aut Urea-containing peptide boronic acids as potent proteasome inhibitors 2017transfer abstract 15 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier A novel class of urea-containing peptide boronic acids as proteasome inhibitors was designed by introducing a urea scaffold to replace an amido bond. Compounds were synthesized and their antitumor activities were evaluated. After two rounds of optimizations, the compound I-14 was found to be a potent proteasome inhibitor. Compared with Bortezomib, I-14 showed higher potency against the chymotrypsin-like activity of human 20S proteasome (IC50 < 1 pM), similar potency against four different cancer cell lines (IC50 < 10 nM), and better pharmacokinetic profile. Furthermore, I-14 significantly inhibited tumor growth in Bel7404 mouse xenograft model. The excellent proteasome inhibition by I-14 was rationalized through docking and molecular dynamics studies. A novel class of urea-containing peptide boronic acids as proteasome inhibitors was designed by introducing a urea scaffold to replace an amido bond. Compounds were synthesized and their antitumor activities were evaluated. After two rounds of optimizations, the compound I-14 was found to be a potent proteasome inhibitor. Compared with Bortezomib, I-14 showed higher potency against the chymotrypsin-like activity of human 20S proteasome (IC50 < 1 pM), similar potency against four different cancer cell lines (IC50 < 10 nM), and better pharmacokinetic profile. Furthermore, I-14 significantly inhibited tumor growth in Bel7404 mouse xenograft model. The excellent proteasome inhibition by I-14 was rationalized through docking and molecular dynamics studies. Proteasome inhibitor Elsevier Structure-activity relationship Elsevier Anti-tumor activity Elsevier Low toxicity Elsevier Urea-containing peptide boronic acids Elsevier Yuan, Xia oth Wu, Xing-Yu oth Li, Ri-Dong oth Xu, Bo oth Cheng, Qing oth Liu, Zhen-Ming oth Zhou, Tian-Yan oth An, Hao-Yun oth Wang, Xin oth Cheng, Tie-Ming oth Ge, Ze-Mei oth Cui, Jing-Rong oth Li, Run-Tao oth Enthalten in Elsevier Science Jose, Ajay ELSEVIER Electrochemical synthesis, photodegradation and antibacterial properties of PEG capped zinc oxide nanoparticles 2018 Amsterdam [u.a.] (DE-627)ELV000457477 volume:125 year:2017 day:5 month:01 pages:925-939 extent:15 https://doi.org/10.1016/j.ejmech.2016.10.023 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-BIODIV SSG-OLC-PHA 42.00 Biologie: Allgemeines VZ AR 125 2017 5 0105 925-939 15 045F 610 |
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10.1016/j.ejmech.2016.10.023 doi GBVA2017007000009.pica (DE-627)ELV020124953 (ELSEVIER)S0223-5234(16)30886-8 DE-627 ger DE-627 rakwb eng 610 610 DE-600 570 540 VZ BIODIV DE-30 fid 42.00 bkl Han, Li-Qiang verfasserin aut Urea-containing peptide boronic acids as potent proteasome inhibitors 2017transfer abstract 15 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier A novel class of urea-containing peptide boronic acids as proteasome inhibitors was designed by introducing a urea scaffold to replace an amido bond. Compounds were synthesized and their antitumor activities were evaluated. After two rounds of optimizations, the compound I-14 was found to be a potent proteasome inhibitor. Compared with Bortezomib, I-14 showed higher potency against the chymotrypsin-like activity of human 20S proteasome (IC50 < 1 pM), similar potency against four different cancer cell lines (IC50 < 10 nM), and better pharmacokinetic profile. Furthermore, I-14 significantly inhibited tumor growth in Bel7404 mouse xenograft model. The excellent proteasome inhibition by I-14 was rationalized through docking and molecular dynamics studies. A novel class of urea-containing peptide boronic acids as proteasome inhibitors was designed by introducing a urea scaffold to replace an amido bond. Compounds were synthesized and their antitumor activities were evaluated. After two rounds of optimizations, the compound I-14 was found to be a potent proteasome inhibitor. Compared with Bortezomib, I-14 showed higher potency against the chymotrypsin-like activity of human 20S proteasome (IC50 < 1 pM), similar potency against four different cancer cell lines (IC50 < 10 nM), and better pharmacokinetic profile. Furthermore, I-14 significantly inhibited tumor growth in Bel7404 mouse xenograft model. The excellent proteasome inhibition by I-14 was rationalized through docking and molecular dynamics studies. Proteasome inhibitor Elsevier Structure-activity relationship Elsevier Anti-tumor activity Elsevier Low toxicity Elsevier Urea-containing peptide boronic acids Elsevier Yuan, Xia oth Wu, Xing-Yu oth Li, Ri-Dong oth Xu, Bo oth Cheng, Qing oth Liu, Zhen-Ming oth Zhou, Tian-Yan oth An, Hao-Yun oth Wang, Xin oth Cheng, Tie-Ming oth Ge, Ze-Mei oth Cui, Jing-Rong oth Li, Run-Tao oth Enthalten in Elsevier Science Jose, Ajay ELSEVIER Electrochemical synthesis, photodegradation and antibacterial properties of PEG capped zinc oxide nanoparticles 2018 Amsterdam [u.a.] (DE-627)ELV000457477 volume:125 year:2017 day:5 month:01 pages:925-939 extent:15 https://doi.org/10.1016/j.ejmech.2016.10.023 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-BIODIV SSG-OLC-PHA 42.00 Biologie: Allgemeines VZ AR 125 2017 5 0105 925-939 15 045F 610 |
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10.1016/j.ejmech.2016.10.023 doi GBVA2017007000009.pica (DE-627)ELV020124953 (ELSEVIER)S0223-5234(16)30886-8 DE-627 ger DE-627 rakwb eng 610 610 DE-600 570 540 VZ BIODIV DE-30 fid 42.00 bkl Han, Li-Qiang verfasserin aut Urea-containing peptide boronic acids as potent proteasome inhibitors 2017transfer abstract 15 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier A novel class of urea-containing peptide boronic acids as proteasome inhibitors was designed by introducing a urea scaffold to replace an amido bond. Compounds were synthesized and their antitumor activities were evaluated. After two rounds of optimizations, the compound I-14 was found to be a potent proteasome inhibitor. Compared with Bortezomib, I-14 showed higher potency against the chymotrypsin-like activity of human 20S proteasome (IC50 < 1 pM), similar potency against four different cancer cell lines (IC50 < 10 nM), and better pharmacokinetic profile. Furthermore, I-14 significantly inhibited tumor growth in Bel7404 mouse xenograft model. The excellent proteasome inhibition by I-14 was rationalized through docking and molecular dynamics studies. A novel class of urea-containing peptide boronic acids as proteasome inhibitors was designed by introducing a urea scaffold to replace an amido bond. Compounds were synthesized and their antitumor activities were evaluated. After two rounds of optimizations, the compound I-14 was found to be a potent proteasome inhibitor. Compared with Bortezomib, I-14 showed higher potency against the chymotrypsin-like activity of human 20S proteasome (IC50 < 1 pM), similar potency against four different cancer cell lines (IC50 < 10 nM), and better pharmacokinetic profile. Furthermore, I-14 significantly inhibited tumor growth in Bel7404 mouse xenograft model. The excellent proteasome inhibition by I-14 was rationalized through docking and molecular dynamics studies. Proteasome inhibitor Elsevier Structure-activity relationship Elsevier Anti-tumor activity Elsevier Low toxicity Elsevier Urea-containing peptide boronic acids Elsevier Yuan, Xia oth Wu, Xing-Yu oth Li, Ri-Dong oth Xu, Bo oth Cheng, Qing oth Liu, Zhen-Ming oth Zhou, Tian-Yan oth An, Hao-Yun oth Wang, Xin oth Cheng, Tie-Ming oth Ge, Ze-Mei oth Cui, Jing-Rong oth Li, Run-Tao oth Enthalten in Elsevier Science Jose, Ajay ELSEVIER Electrochemical synthesis, photodegradation and antibacterial properties of PEG capped zinc oxide nanoparticles 2018 Amsterdam [u.a.] (DE-627)ELV000457477 volume:125 year:2017 day:5 month:01 pages:925-939 extent:15 https://doi.org/10.1016/j.ejmech.2016.10.023 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-BIODIV SSG-OLC-PHA 42.00 Biologie: Allgemeines VZ AR 125 2017 5 0105 925-939 15 045F 610 |
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10.1016/j.ejmech.2016.10.023 doi GBVA2017007000009.pica (DE-627)ELV020124953 (ELSEVIER)S0223-5234(16)30886-8 DE-627 ger DE-627 rakwb eng 610 610 DE-600 570 540 VZ BIODIV DE-30 fid 42.00 bkl Han, Li-Qiang verfasserin aut Urea-containing peptide boronic acids as potent proteasome inhibitors 2017transfer abstract 15 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier A novel class of urea-containing peptide boronic acids as proteasome inhibitors was designed by introducing a urea scaffold to replace an amido bond. Compounds were synthesized and their antitumor activities were evaluated. After two rounds of optimizations, the compound I-14 was found to be a potent proteasome inhibitor. Compared with Bortezomib, I-14 showed higher potency against the chymotrypsin-like activity of human 20S proteasome (IC50 < 1 pM), similar potency against four different cancer cell lines (IC50 < 10 nM), and better pharmacokinetic profile. Furthermore, I-14 significantly inhibited tumor growth in Bel7404 mouse xenograft model. The excellent proteasome inhibition by I-14 was rationalized through docking and molecular dynamics studies. A novel class of urea-containing peptide boronic acids as proteasome inhibitors was designed by introducing a urea scaffold to replace an amido bond. Compounds were synthesized and their antitumor activities were evaluated. After two rounds of optimizations, the compound I-14 was found to be a potent proteasome inhibitor. Compared with Bortezomib, I-14 showed higher potency against the chymotrypsin-like activity of human 20S proteasome (IC50 < 1 pM), similar potency against four different cancer cell lines (IC50 < 10 nM), and better pharmacokinetic profile. Furthermore, I-14 significantly inhibited tumor growth in Bel7404 mouse xenograft model. The excellent proteasome inhibition by I-14 was rationalized through docking and molecular dynamics studies. Proteasome inhibitor Elsevier Structure-activity relationship Elsevier Anti-tumor activity Elsevier Low toxicity Elsevier Urea-containing peptide boronic acids Elsevier Yuan, Xia oth Wu, Xing-Yu oth Li, Ri-Dong oth Xu, Bo oth Cheng, Qing oth Liu, Zhen-Ming oth Zhou, Tian-Yan oth An, Hao-Yun oth Wang, Xin oth Cheng, Tie-Ming oth Ge, Ze-Mei oth Cui, Jing-Rong oth Li, Run-Tao oth Enthalten in Elsevier Science Jose, Ajay ELSEVIER Electrochemical synthesis, photodegradation and antibacterial properties of PEG capped zinc oxide nanoparticles 2018 Amsterdam [u.a.] (DE-627)ELV000457477 volume:125 year:2017 day:5 month:01 pages:925-939 extent:15 https://doi.org/10.1016/j.ejmech.2016.10.023 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-BIODIV SSG-OLC-PHA 42.00 Biologie: Allgemeines VZ AR 125 2017 5 0105 925-939 15 045F 610 |
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10.1016/j.ejmech.2016.10.023 doi GBVA2017007000009.pica (DE-627)ELV020124953 (ELSEVIER)S0223-5234(16)30886-8 DE-627 ger DE-627 rakwb eng 610 610 DE-600 570 540 VZ BIODIV DE-30 fid 42.00 bkl Han, Li-Qiang verfasserin aut Urea-containing peptide boronic acids as potent proteasome inhibitors 2017transfer abstract 15 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier A novel class of urea-containing peptide boronic acids as proteasome inhibitors was designed by introducing a urea scaffold to replace an amido bond. Compounds were synthesized and their antitumor activities were evaluated. After two rounds of optimizations, the compound I-14 was found to be a potent proteasome inhibitor. Compared with Bortezomib, I-14 showed higher potency against the chymotrypsin-like activity of human 20S proteasome (IC50 < 1 pM), similar potency against four different cancer cell lines (IC50 < 10 nM), and better pharmacokinetic profile. Furthermore, I-14 significantly inhibited tumor growth in Bel7404 mouse xenograft model. The excellent proteasome inhibition by I-14 was rationalized through docking and molecular dynamics studies. A novel class of urea-containing peptide boronic acids as proteasome inhibitors was designed by introducing a urea scaffold to replace an amido bond. Compounds were synthesized and their antitumor activities were evaluated. After two rounds of optimizations, the compound I-14 was found to be a potent proteasome inhibitor. Compared with Bortezomib, I-14 showed higher potency against the chymotrypsin-like activity of human 20S proteasome (IC50 < 1 pM), similar potency against four different cancer cell lines (IC50 < 10 nM), and better pharmacokinetic profile. Furthermore, I-14 significantly inhibited tumor growth in Bel7404 mouse xenograft model. The excellent proteasome inhibition by I-14 was rationalized through docking and molecular dynamics studies. Proteasome inhibitor Elsevier Structure-activity relationship Elsevier Anti-tumor activity Elsevier Low toxicity Elsevier Urea-containing peptide boronic acids Elsevier Yuan, Xia oth Wu, Xing-Yu oth Li, Ri-Dong oth Xu, Bo oth Cheng, Qing oth Liu, Zhen-Ming oth Zhou, Tian-Yan oth An, Hao-Yun oth Wang, Xin oth Cheng, Tie-Ming oth Ge, Ze-Mei oth Cui, Jing-Rong oth Li, Run-Tao oth Enthalten in Elsevier Science Jose, Ajay ELSEVIER Electrochemical synthesis, photodegradation and antibacterial properties of PEG capped zinc oxide nanoparticles 2018 Amsterdam [u.a.] (DE-627)ELV000457477 volume:125 year:2017 day:5 month:01 pages:925-939 extent:15 https://doi.org/10.1016/j.ejmech.2016.10.023 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U FID-BIODIV SSG-OLC-PHA 42.00 Biologie: Allgemeines VZ AR 125 2017 5 0105 925-939 15 045F 610 |
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Enthalten in Electrochemical synthesis, photodegradation and antibacterial properties of PEG capped zinc oxide nanoparticles Amsterdam [u.a.] volume:125 year:2017 day:5 month:01 pages:925-939 extent:15 |
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Enthalten in Electrochemical synthesis, photodegradation and antibacterial properties of PEG capped zinc oxide nanoparticles Amsterdam [u.a.] volume:125 year:2017 day:5 month:01 pages:925-939 extent:15 |
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Electrochemical synthesis, photodegradation and antibacterial properties of PEG capped zinc oxide nanoparticles |
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A novel class of urea-containing peptide boronic acids as proteasome inhibitors was designed by introducing a urea scaffold to replace an amido bond. Compounds were synthesized and their antitumor activities were evaluated. After two rounds of optimizations, the compound I-14 was found to be a potent proteasome inhibitor. Compared with Bortezomib, I-14 showed higher potency against the chymotrypsin-like activity of human 20S proteasome (IC50 < 1 pM), similar potency against four different cancer cell lines (IC50 < 10 nM), and better pharmacokinetic profile. Furthermore, I-14 significantly inhibited tumor growth in Bel7404 mouse xenograft model. The excellent proteasome inhibition by I-14 was rationalized through docking and molecular dynamics studies. |
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A novel class of urea-containing peptide boronic acids as proteasome inhibitors was designed by introducing a urea scaffold to replace an amido bond. Compounds were synthesized and their antitumor activities were evaluated. After two rounds of optimizations, the compound I-14 was found to be a potent proteasome inhibitor. Compared with Bortezomib, I-14 showed higher potency against the chymotrypsin-like activity of human 20S proteasome (IC50 < 1 pM), similar potency against four different cancer cell lines (IC50 < 10 nM), and better pharmacokinetic profile. Furthermore, I-14 significantly inhibited tumor growth in Bel7404 mouse xenograft model. The excellent proteasome inhibition by I-14 was rationalized through docking and molecular dynamics studies. |
| abstract_unstemmed |
A novel class of urea-containing peptide boronic acids as proteasome inhibitors was designed by introducing a urea scaffold to replace an amido bond. Compounds were synthesized and their antitumor activities were evaluated. After two rounds of optimizations, the compound I-14 was found to be a potent proteasome inhibitor. Compared with Bortezomib, I-14 showed higher potency against the chymotrypsin-like activity of human 20S proteasome (IC50 < 1 pM), similar potency against four different cancer cell lines (IC50 < 10 nM), and better pharmacokinetic profile. Furthermore, I-14 significantly inhibited tumor growth in Bel7404 mouse xenograft model. The excellent proteasome inhibition by I-14 was rationalized through docking and molecular dynamics studies. |
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