Disulfiram is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram acts as an allosteric inhibitor of MERS-CoV PLpro but as a competitive (or mixed) inhibitor of SARS-CoV PLpro. It also inhibits pyroptosis by blocking gasdermin D pore formation.
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Aldehyde dehydrogenase can catalyze the oxidation of aldehydes by converting them to carboxylic acids, which leave the liver and are metabolized by the body's muscle and heart. Thus the accumulation of aldehydes do harm to human. Disulfiram (DSF) is currently a clinical used inhibitor for aldehyde dehydrogenase treating alcoholism with average IC50 value of 300 nM. Moreover, studies showed that DSF may also have antitumor and chemosensitizing activities. DSF treatment could inhibit growth of TNBC cells by increasing cell death and senescence and induced 38% cell death after 72 hrs treatment combined with doxorubicin. Besides, DSF also caused many MDA-MB-231 cells death and enlarged cell morphology, showing 23% X-gal-positive cells. Cancer stem cells (CSCs) in TNBC cell lines were inhibited by 5% with DSF treatment alone or by 65% with combined treatment with doxorubicin.[1] In purified rabbit 20S proteasome assay, DSF-copper complex inhibited the chymotrypsin-like activity with an IC50 value of 7.5 μM while DSF alone had no effect even at concentration of 20 μM. The complex also led to 95% reduction of the proteasomal chymotrypsin-like activity in the breast cancer cells and inhibited proliferation of MDA-MB-231 cells by 55%, 65% and 85% when the concentrations were 5, 10, 20 μM respectively. Besides, the complex induced apoptotic cell death due to the detection of PARP cleavage in the breast cancer cells, suggesting that the copper ion should be responsible for the inhibiting ability of DSF. Treated the MCF-10A (normal cells) and MCF10DCIS.com cell lines (malignant cells) with 20 μM the complex led to 97% reduction of proteasomal chymotrypsin-like activity in MCF10DCIS.com cell lines but no effect on the MCF-10A cell lines, suggesting the nontoxic effect of the DSF-copper complex in normal cells. The CuCl2-precultured MDA-MB-231 cells treated with 20 μM DSF also showed 67% inhibition of the proteasomal activity as well as the accumulation of PARP cleavage, suggesting copper ion is important for DSF treatment. Furthermore, DSF-treated tumors resulted in 74% inhibition of tumor growth and 87% inhibition of the proteasomal activity[2]. Disulfiram potently inhibited GSDMD pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells. It covalently modify a conserved Cys (Cys191 in human and Cys192 in mouse GSDMD) that is critical for pore formation[3]. It also works as a pyroptosis inhibitor by blocking gasdermin D pore formation[4].
作用机制
Disulfiram is capable of binding copper react with sulfhydryl groups.[2]
Disulfiram 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
CHO cells
Function assay
Agonist activity at human TRPA1 channel expressed in CHO cells assessed as increase in intracellular calcium levels, EC50=3 μM
20356305
human MCF10A cells
Proliferation assay
72 h
Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay, IC50=10 μM
20222671
human MDA-MB-231 cells
Proliferation assay
72 h
Antiproliferative activity against human MDA-MB-231 cells expressing BCA2 and ERalpha after 72 hrs by MTT assay, IC50=0.32 μM
20222671
human T47D cells
Proliferation assay
72 h
Antiproliferative activity against human T47D cells expressing BCA2 and estrogen receptor after 72 hrs by MTT assay, IC50=0.17 μM
Denmark
... 展开 >> Hvidovre University Hospital
Hvidovre, Copenhagen, Denmark, 2650
Hospital Of South West Denmark
Aabenraa, Denmark
Bispebjerg University Hospital
Copenhagen, Denmark 收起 <<
United States, Alabama
... 展开 >>
Tuscaloosa VAMC
Tuscaloosa, Alabama, United States, 35404
United States, California
VA San Diego Healthcare System
San Diego, California, United States, 92161
United States, New York
James J.Peters VA Medical Center
The Bronx, New York, United States, 10468 收起 <<
United States, New Mexico
... 展开 >>
University of New Mexico
Recruiting
Albuquerque, New Mexico, United States, 87131-0001
Contact: Florian Birkmayer, M.D. 505-272-2223 fbirkmayer@salud.unm.edu
Sub-Investigator: Michael Bogenschutz, M.D. 收起 <<
United States, California
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UCLA Integrated Substance Abuse Program
Los Angeles, California, United States, 90024
United States, Texas
University of Texas Hlth Sci Ctr San Ant
San Antonio, Texas, United States, 78284 7828 收起 <<
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Johns Hopkins Hospital
Baltimore, Maryland, United States, 21231
United States, North Carolina
Duke University
Durham, North Carolina, United States, 27710
United States, Pennsylvania
Thomas Jefferson Universith
Philadelphia, Pennsylvania, United States, 19107 收起 <<
United States, North Carolina
... 展开 >>
Duke University Medical Center
Recruiting
Durham, North Carolina, United States, 27710
Contact: Julia Rasmussen, MS, RN, BSN 919-681-1030 julia.rasmussen@duke.edu 收起 <<
United States, Michigan
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Beaumont Hospital
Royal Oak, Michigan, United States, 48073
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Washington University School of Medicine
Saint Louis, Missouri, United States, 63110
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John Theurer Cancer Center
Hackensack, New Jersey, United States, 07601
United States, New York
Lenox Hill Hospital
New York, New York, United States, 10075
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University of Cincinnati
Cincinnati, Ohio, United States, 45220
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Vanderbilt Ingram Cancer Center
Nashville, Tennessee, United States, 37212
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Baylor University Medical Center
Dallas, Texas, United States, 75246
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Huntsman Cancer Institute
Salt Lake City, Utah, United States, 84112-5550 收起 <<
Greece
... 展开 >> Olympion Medical Center
Not yet recruiting
Patras, Greece, 26443
Contact: Petros N Karamanakos, MD, PhD
Principal Investigator: Petros N Karamanakos, MD, PhD 收起 <<
United States, Connecticut
... 展开 >>
The APT Foundation MRU
New Haven, Connecticut, United States, 06519
Yale University School of Medicine
New Haven, Connecticut, United States, 06519 收起 <<
Norway
... 展开 >> Cancer Clinic, St.Olavs University Hospital
Recruiting
Trondheim, Norway
Contact: Tora S Solheim, MD, PhD
Principal Investigator: Tora S Solheim, MD, PhD
Sweden
Dept. of Oncology, Sahlgrenska University Hospital
Recruiting
Gothenburg, Sweden
Contact: Katja Werlenius, MD
Principal Investigator: Katja Werlenius, MD
Ryhov County Hospital
Recruiting
Jönköping, Sweden
Contact: Michael Strandéus, MD
Principal Investigator: Michael Strandéus, MD
Linköping University Hospital
Recruiting
Linkoping, Sweden
Contact: Munila Mudaisi, MD
Principal Investigator: Munila Mudaisi, MD
Lund University Hospital
Recruiting
Lund, Sweden
Contact: Sara Kinhult, MD, PhD
Principal Investigator: Sara Kinhult, MD, PhD
Karolinska University Hospital
Recruiting
Stockholm, Sweden
Contact: Sofia Hylin, MD
Principal Investigator: Sofia Hylin, MD
Uppsala University Hospital
Recruiting
Uppsala, Sweden
Contact: Magnus Lindskog, MD, PhD
Principal Investigator: Magnus Lindskog, MD, PHD
Örebro University Hospital
Recruiting
Örebro, Sweden
Contact: David Löfgren, MD
Principal Investigator: David Löfgren, MD 收起 <<
United States, New Mexico
... 展开 >>
University of New Mexico Addiction and Substance Abuse Programs
Albuquerque, New Mexico, United States, 87106 收起 <<
United States, Wisconsin
... 展开 >>
Aurora Health Care, Aurora St. Luke's Medical Center
Recruiting
Milwaukee, Wisconsin, United States, 53215
Contact: Lynda Yanny 414-649-6685 lynda.yanny@aurora.org
Principal Investigator: George Bobustuc, MD
Sub-Investigator: Richard A Rovin, MD
Sub-Investigator: Asad Khan, MD
Sub-Investigator: Amin Kassam, MD
Sub-Investigator: Santhi Konduri, PhD 收起 <<
Terminated(Halted because of s... 展开 >>low accrual and lack of study funding) 收起 <<
-
United States, California
... 展开 >>
Chao Family Comprehensive Cancer Center, University of California, Irvine
Orange, California, United States, 92868 收起 <<
United States, California
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San Francisco General Hospital
San Francisco, California, United States, 94110
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Johns Hopkins University
Baltimore, Maryland, United States, 21205 收起 <<
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... 展开 >>
San Francisco General Hospital
San Francisco, California, United States, 94110
Australia
Alfred Hospital
Melbourne, Australia, 3004 收起 <<
United States, New York
... 展开 >>
NYPInstitute
Recruiting
New York, New York, United States, 10032
Contact: Nasir H. Naqvi, MD, PhD 212-923-3031 nhn2102@columbia.edu
Principal Investigator: Nasir H. Naqvi, MD, PhD 收起 <<
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