Skip to main content

Research Repository

Advanced Search

CYP enzymes, expressed within live human suspension cells, are superior to widely-used microsomal enzymes in identifying potent CYP1A1/CYP1B1 inhibitors: Identification of quinazolinones as CYP1A1/CYP1B1 inhibitors that efficiently reverse B[a]P toxicity (2019)
Journal Article
Williams, I. S., Sonawane, V. R., Mohd Usman, M. S., Gatchie, L., .Bharate, S. B., Jayaprakash, V., …Chaudhuri, B. (2019). CYP enzymes, expressed within live human suspension cells, are superior to widely-used microsomal enzymes in identifying potent CYP1A1/CYP1B1 inhibitors: Identification of quinazolinones as CYP1A1/CYP1B1 inhibitors that efficiently reverse B[a]P toxicity and cisplatin resistance. European Journal of Pharmaceutical Sciences, 131, 177-194. https://doi.org/10.1016/j.ejps.2019.02.016

Microsomal cytochrome P450 (CYP) enzymes, isolated from recombinant bacterial/insect/yeast cells, are extensively used for drug metabolism studies. However, they may not always portray how a developmental drug would behave in human cells with intact... Read More about CYP enzymes, expressed within live human suspension cells, are superior to widely-used microsomal enzymes in identifying potent CYP1A1/CYP1B1 inhibitors: Identification of quinazolinones as CYP1A1/CYP1B1 inhibitors that efficiently reverse B[a]P toxicity .

Furanoflavones pongapin and lanceolatin B blocks the cell cycle and induce senescence in CYP1A1-overexpressing breast cancer cells (2018)
Journal Article
Sharma, R., Williams, I. S., Linda, G., Sonawane, V. R., Chaudhuri, B., & Bharate, S. B. (2018). Furanoflavones pongapin and lanceolatin B blocks the cell cycle and induce senescence in CYP1A1-overexpressing breast cancer cells. Bioorganic and Medicinal Chemistry, 26(23-24), 6076-6086. https://doi.org/10.1016/j.bmc.2018.11.013

© 2018 Elsevier Ltd Expression of cytochrome P450-1A1 (CYP1A1) is suppressed under physiologic conditions but is induced (a) by polycyclic aromatic hydrocarbons (PAHs) which can be metabolized by CYP1A1 to carcinogens, and (b) in majority of breast c... Read More about Furanoflavones pongapin and lanceolatin B blocks the cell cycle and induce senescence in CYP1A1-overexpressing breast cancer cells.

Khellinoflavanone, a Semisynthetic Derivative of Khellin, Overcomes Benzo[ a]pyrene Toxicity in Human Normal and Cancer Cells That Express CYP1A1 (2018)
Journal Article
Sharma, R., Williams, I. S., Gatchie, L., Sonawane, V. R., Chaudhuri, B., & Bharate, S. B. (2018). Khellinoflavanone, a Semisynthetic Derivative of Khellin, Overcomes Benzo[ a]pyrene Toxicity in Human Normal and Cancer Cells That Express CYP1A1. ACS Omega, 3(8), 8553-8566. https://doi.org/10.1021/acsomega.8b01088

Copyright © 2018 American Chemical Society. Cytochrome P450 family 1 (CYP1) enzymes catalyze the metabolic activation of environmental procarcinogens such as benzo[a]pyrene, B[a]P, into carcinogens, which initiates the process of carcinogenesis. Thus... Read More about Khellinoflavanone, a Semisynthetic Derivative of Khellin, Overcomes Benzo[ a]pyrene Toxicity in Human Normal and Cancer Cells That Express CYP1A1.

Nonantioxidant Tetramethoxystilbene Abrogates α-Synuclein-Induced Yeast Cell Death but Not That Triggered by the Bax or βa4 Peptide (2018)
Journal Article
Derf, A., Mudududdla, R., Akintade, D., Williams, I. S., Abdullaha, M., Chaudhuri, B., & Bharate, S. B. (2018). Nonantioxidant Tetramethoxystilbene Abrogates α-Synuclein-Induced Yeast Cell Death but Not That Triggered by the Bax or βa4 Peptide. ACS Omega, 3(8), 9513-9532. https://doi.org/10.1021/acsomega.8b01154

© 2018 American Chemical Society. The overexpression of α-synuclein (α-syn) and its aggregation is the hallmark of Parkinson's disease. The α-syn aggregation results in the formation of Lewy bodies that causes neuronal cell death. Therefore, the smal... Read More about Nonantioxidant Tetramethoxystilbene Abrogates α-Synuclein-Induced Yeast Cell Death but Not That Triggered by the Bax or βa4 Peptide.

Biotransformation, Using Recombinant CYP450-Expressing Baker's Yeast Cells, Identifies a Novel CYP2D6.10A122V Variant Which Is a Superior Metabolizer of Codeine to Morphine Than the Wild-Type Enzyme (2018)
Journal Article
Williams, I. S., Gatchie, L., Bharate, S. B., & Chaudhuri, B. (2018). Biotransformation, Using Recombinant CYP450-Expressing Baker's Yeast Cells, Identifies a Novel CYP2D6.10A122V Variant Which Is a Superior Metabolizer of Codeine to Morphine Than the Wild-Type Enzyme. ACS Omega, 3(8), 8903-8912. https://doi.org/10.1021/acsomega.8b00809

© Copyright 2018 American Chemical Society. CYP2D6, a cytochrome P450 (CYP) enzyme, metabolizes codeine to morphine. Within the human body, 0-15% of codeine undergoes O-demethylation by CYP2D6 to form morphine, a far stronger analgesic than codeine.... Read More about Biotransformation, Using Recombinant CYP450-Expressing Baker's Yeast Cells, Identifies a Novel CYP2D6.10A122V Variant Which Is a Superior Metabolizer of Codeine to Morphine Than the Wild-Type Enzyme.

Glycyrrhiza glabra extract and quercetin reverses cisplatin resistance in triple-negative MDA-MB-468 breast cancer cells via inhibition of cytochrome P450 1B1 enzyme (2017)
Journal Article
Bharate, S. B., Chaudhuri, B., Vishwakarma, R. A., Jain, S. K., Sharma, R., Gatchie, L., & Williams, I. S. (2017). Glycyrrhiza glabra extract and quercetin reverses cisplatin resistance in triple-negative MDA-MB-468 breast cancer cells via inhibition of cytochrome P450 1B1 enzyme. Bioorganic and Medicinal Chemistry Letters, 27(24), 5400-5403. https://doi.org/10.1016/j.bmcl.2017.11.013

© 2017 Elsevier Ltd The development of multi-drug resistance to existing anticancer drugs is one of the major challenges in cancer treatment. The over-expression of cytochrome P450 1B1 enzyme has been reported to cause resistance to cisplatin. With a... Read More about Glycyrrhiza glabra extract and quercetin reverses cisplatin resistance in triple-negative MDA-MB-468 breast cancer cells via inhibition of cytochrome P450 1B1 enzyme.

(E)-3-(3,4,5-Trimethoxyphenyl)-1-(pyridin-4-yl)prop-2-en-1-one, a heterocyclic chalcone is a potent and selective CYP1A1 inhibitor and cancer chemopreventive agent (2017)
Journal Article
Horley, N. J., Beresford, K. J., Kaduskar, S., Joshi, P., McCann, G. J., Ruparelia, K. C., …Chaudhuri, B. (2017). (E)-3-(3,4,5-Trimethoxyphenyl)-1-(pyridin-4-yl)prop-2-en-1-one, a heterocyclic chalcone is a potent and selective CYP1A1 inhibitor and cancer chemopreventive agent. Bioorganic and Medicinal Chemistry Letters, 27(24), 5409-5414. https://doi.org/10.1016/j.bmcl.2017.11.009

The overexpression of CYP1 family of enzymes is reported to be associated with development of human carcinomas. It has been well reported that CYP1A1 specific inhibitors prevents carcinogenesis. Herein, thirteen pyridine-4-yl series of chalcones were... Read More about (E)-3-(3,4,5-Trimethoxyphenyl)-1-(pyridin-4-yl)prop-2-en-1-one, a heterocyclic chalcone is a potent and selective CYP1A1 inhibitor and cancer chemopreventive agent.

Biotransformation of Chrysin to Baicalein: Selective C6-Hydroxylation of 5,7-Dihydroxyflavone Using Whole Yeast Cells Stably Expressing Human CYP1A1 Enzyme (2017)
Journal Article
Bharate, S. B., Nuthakki, V. K., Williams, I. S., Chib, S., Gatchie, L., Joshi, P., …Chaudhuri, B. (2017). Biotransformation of Chrysin to Baicalein: Selective C6-Hydroxylation of 5,7-Dihydroxyflavone Using Whole Yeast Cells Stably Expressing Human CYP1A1 Enzyme. Journal of Agricultural and Food Chemistry, 65(34), 7440-7446. https://doi.org/10.1021/acs.jafc.7b02690

© 2017 American Chemical Society. Naturally occurring polyphenolic compounds are of medicinal importance because of their unique antioxidant, anticancer, and chemopreventive properties. Baicalein, a naturally occurring polyhydroxy flavonoid possessin... Read More about Biotransformation of Chrysin to Baicalein: Selective C6-Hydroxylation of 5,7-Dihydroxyflavone Using Whole Yeast Cells Stably Expressing Human CYP1A1 Enzyme.

Discovery and characterization of novel CYP1B1 inhibitors based on heterocyclic chalcones: Overcoming cisplatin resistance in CYP1B1-overexpressing lines (2017)
Journal Article
Horley, N. J., Beresford, K. J., Chawla, T., McCann, G. J., Ruparelia, K. C., Gatchie, L., …Chaudhuri, B. (2017). Discovery and characterization of novel CYP1B1 inhibitors based on heterocyclic chalcones: Overcoming cisplatin resistance in CYP1B1-overexpressing lines. European Journal of Medicinal Chemistry, 129, 159-174. https://doi.org/10.1016/j.ejmech.2017.02.016

© 2017 Elsevier Masson SAS The structure of alpha-napthoflavone (ANF), a potent inhibitor of CYP1A1 and CYP1B1, mimics the structure of chalcones. Two potent CYP1B1 inhibitors 7k (DMU2105) and 6j (DMU2139) have been identified from two series of syn... Read More about Discovery and characterization of novel CYP1B1 inhibitors based on heterocyclic chalcones: Overcoming cisplatin resistance in CYP1B1-overexpressing lines.

Synthesis and biological evaluation of pyrrole-based chalcones as CYP1 enzyme inhibitors, for possible prevention of cancer and overcoming cisplatin resistance (2017)
Journal Article
Satti, N. K., Williams, I. S., Joshi, P., Gatchie, L., Sharma, M., Vishwakarma, R. A., …Bharate, S. B. (2017). Synthesis and biological evaluation of pyrrole-based chalcones as CYP1 enzyme inhibitors, for possible prevention of cancer and overcoming cisplatin resistance. Bioorganic and Medicinal Chemistry Letters, 27(16), 3683-3687. https://doi.org/10.1016/j.bmcl.2017.07.010

© 2017 Elsevier Ltd Inhibitors of CYP1 enzymes may play vital roles in the prevention of cancer and overcoming chemo-resistance to anticancer drugs. In this letter, we report synthesis of twenty-three pyrrole based heterocyclic chalcones which were s... Read More about Synthesis and biological evaluation of pyrrole-based chalcones as CYP1 enzyme inhibitors, for possible prevention of cancer and overcoming cisplatin resistance.

Biphenyl urea derivatives as selective CYP1B1 inhibitors (2016)
Journal Article
Sinha, B. N., Williams, I. S., McCann, G. J., Mohd Siddique, M. U., Siddique,, M. U. M., McCann,, G. J. P., …Chaudhuri, B. (2016). Biphenyl urea derivatives as selective CYP1B1 inhibitors. Organic and Biomolecular Chemistry, 14(38), 8931-8936. https://doi.org/10.1039/c6ob01506a

© 2016 The Royal Society of Chemistry. Highly selective CYP1B1 inhibitors have potential in the treatment of hormone-induced breast and prostate cancers. Mimicry of potent and selective CYP1B1 inhibitors, α-naphthoflavone and stilbenes, revealed that... Read More about Biphenyl urea derivatives as selective CYP1B1 inhibitors.


;