Exploring the Potential of Sulfur Moieties in Compounds Inhibiting Steroidogenesis

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt

Standard

Exploring the Potential of Sulfur Moieties in Compounds Inhibiting Steroidogenesis. / Wróbel, Tomasz M.; Sharma, Katyayani; Mannella, Iole; Oliaro-Bosso, Simonetta; Nieckarz, Patrycja; Du Toit, Therina; Voegel, Clarissa Daniela; Rojas Velazquez, Maria Natalia; Yakubu, Jibira; Matveeva, Anna; Therkelsen, Søren; Jørgensen, Flemming Steen; Pandey, Amit V.; Pippione, Agnese C.; Lolli, Marco L.; Boschi, Donatella; Björkling, Fredrik.

I: Biomolecules, Bind 13, Nr. 9, 1349, 2023.

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt

Harvard

Wróbel, TM, Sharma, K, Mannella, I, Oliaro-Bosso, S, Nieckarz, P, Du Toit, T, Voegel, CD, Rojas Velazquez, MN, Yakubu, J, Matveeva, A, Therkelsen, S, Jørgensen, FS, Pandey, AV, Pippione, AC, Lolli, ML, Boschi, D & Björkling, F 2023, 'Exploring the Potential of Sulfur Moieties in Compounds Inhibiting Steroidogenesis', Biomolecules, bind 13, nr. 9, 1349. https://doi.org/10.3390/biom13091349

APA

Wróbel, T. M., Sharma, K., Mannella, I., Oliaro-Bosso, S., Nieckarz, P., Du Toit, T., Voegel, C. D., Rojas Velazquez, M. N., Yakubu, J., Matveeva, A., Therkelsen, S., Jørgensen, F. S., Pandey, A. V., Pippione, A. C., Lolli, M. L., Boschi, D., & Björkling, F. (2023). Exploring the Potential of Sulfur Moieties in Compounds Inhibiting Steroidogenesis. Biomolecules, 13(9), [1349]. https://doi.org/10.3390/biom13091349

Vancouver

Wróbel TM, Sharma K, Mannella I, Oliaro-Bosso S, Nieckarz P, Du Toit T o.a. Exploring the Potential of Sulfur Moieties in Compounds Inhibiting Steroidogenesis. Biomolecules. 2023;13(9). 1349. https://doi.org/10.3390/biom13091349

Author

Wróbel, Tomasz M. ; Sharma, Katyayani ; Mannella, Iole ; Oliaro-Bosso, Simonetta ; Nieckarz, Patrycja ; Du Toit, Therina ; Voegel, Clarissa Daniela ; Rojas Velazquez, Maria Natalia ; Yakubu, Jibira ; Matveeva, Anna ; Therkelsen, Søren ; Jørgensen, Flemming Steen ; Pandey, Amit V. ; Pippione, Agnese C. ; Lolli, Marco L. ; Boschi, Donatella ; Björkling, Fredrik. / Exploring the Potential of Sulfur Moieties in Compounds Inhibiting Steroidogenesis. I: Biomolecules. 2023 ; Bind 13, Nr. 9.

Bibtex

@article{c9c0cd4804e149ffaf3ae822d0074064,
title = "Exploring the Potential of Sulfur Moieties in Compounds Inhibiting Steroidogenesis",
abstract = "This study reports on the synthesis and evaluation of novel compounds replacing the nitrogen-containing heterocyclic ring on the chemical backbone structure of cytochrome P450 17α-hydroxylase/12,20-lyase (CYP17A1) inhibitors with a phenyl bearing a sulfur-based substituent. Initial screening revealed compounds with marked inhibition of CYP17A1 activity. The selectivity of compounds was thereafter determined against cytochrome P450 21-hydroxylase, cytochrome P450 3A4, and cytochrome P450 oxidoreductase. Additionally, the compounds showed weak inhibitory activity against aldo-keto reductase 1C3 (AKR1C3). The compounds{\textquoteright} impact on steroid hormone levels was also assessed, with some notable modulatory effects observed. This work paves the way for developing more potent dual inhibitors specifically targeting CYP17A1 and AKR1C3.",
keywords = "AKR1C3, CYP17A1, enzyme inhibition, prostate cancer",
author = "Wr{\'o}bel, {Tomasz M.} and Katyayani Sharma and Iole Mannella and Simonetta Oliaro-Bosso and Patrycja Nieckarz and {Du Toit}, Therina and Voegel, {Clarissa Daniela} and {Rojas Velazquez}, {Maria Natalia} and Jibira Yakubu and Anna Matveeva and S{\o}ren Therkelsen and J{\o}rgensen, {Flemming Steen} and Pandey, {Amit V.} and Pippione, {Agnese C.} and Lolli, {Marco L.} and Donatella Boschi and Fredrik Bj{\"o}rkling",
note = "Publisher Copyright: {\textcopyright} 2023 by the authors.",
year = "2023",
doi = "10.3390/biom13091349",
language = "English",
volume = "13",
journal = "Biomolecules",
issn = "2218-273X",
publisher = "MDPI",
number = "9",

}

RIS

TY - JOUR

T1 - Exploring the Potential of Sulfur Moieties in Compounds Inhibiting Steroidogenesis

AU - Wróbel, Tomasz M.

AU - Sharma, Katyayani

AU - Mannella, Iole

AU - Oliaro-Bosso, Simonetta

AU - Nieckarz, Patrycja

AU - Du Toit, Therina

AU - Voegel, Clarissa Daniela

AU - Rojas Velazquez, Maria Natalia

AU - Yakubu, Jibira

AU - Matveeva, Anna

AU - Therkelsen, Søren

AU - Jørgensen, Flemming Steen

AU - Pandey, Amit V.

AU - Pippione, Agnese C.

AU - Lolli, Marco L.

AU - Boschi, Donatella

AU - Björkling, Fredrik

N1 - Publisher Copyright: © 2023 by the authors.

PY - 2023

Y1 - 2023

N2 - This study reports on the synthesis and evaluation of novel compounds replacing the nitrogen-containing heterocyclic ring on the chemical backbone structure of cytochrome P450 17α-hydroxylase/12,20-lyase (CYP17A1) inhibitors with a phenyl bearing a sulfur-based substituent. Initial screening revealed compounds with marked inhibition of CYP17A1 activity. The selectivity of compounds was thereafter determined against cytochrome P450 21-hydroxylase, cytochrome P450 3A4, and cytochrome P450 oxidoreductase. Additionally, the compounds showed weak inhibitory activity against aldo-keto reductase 1C3 (AKR1C3). The compounds’ impact on steroid hormone levels was also assessed, with some notable modulatory effects observed. This work paves the way for developing more potent dual inhibitors specifically targeting CYP17A1 and AKR1C3.

AB - This study reports on the synthesis and evaluation of novel compounds replacing the nitrogen-containing heterocyclic ring on the chemical backbone structure of cytochrome P450 17α-hydroxylase/12,20-lyase (CYP17A1) inhibitors with a phenyl bearing a sulfur-based substituent. Initial screening revealed compounds with marked inhibition of CYP17A1 activity. The selectivity of compounds was thereafter determined against cytochrome P450 21-hydroxylase, cytochrome P450 3A4, and cytochrome P450 oxidoreductase. Additionally, the compounds showed weak inhibitory activity against aldo-keto reductase 1C3 (AKR1C3). The compounds’ impact on steroid hormone levels was also assessed, with some notable modulatory effects observed. This work paves the way for developing more potent dual inhibitors specifically targeting CYP17A1 and AKR1C3.

KW - AKR1C3

KW - CYP17A1

KW - enzyme inhibition

KW - prostate cancer

U2 - 10.3390/biom13091349

DO - 10.3390/biom13091349

M3 - Journal article

C2 - 37759751

AN - SCOPUS:85172765608

VL - 13

JO - Biomolecules

JF - Biomolecules

SN - 2218-273X

IS - 9

M1 - 1349

ER -

ID: 370476533