Literature DB >> 32463235

Overview of AKR1C3: Inhibitor Achievements and Disease Insights.

Yang Liu1, Siyu He2, Ying Chen3, Yijun Liu1, Feng Feng4,3, Wenyuan Liu1, Qinglong Guo2, Li Zhao2, Haopeng Sun1.   

Abstract

Human aldo-keto reductase family 1 member C3 (AKR1C3) is known as a hormone activity regulator and prostaglandin F (PGF) synthase that regulates the occupancy of hormone receptors and cell proliferation. Because of the overexpression in metabolic diseases and various hormone-dependent and -independent carcinomas, as well as the emergence of clinical drug resistance, an increasing number of studies have investigated AKR1C3 inhibitors. Here, we briefly review the physiological and pathological function of AKR1C3 and then summarize the recent development of selective AKR1C3 inhibitors. We propose our viewpoints on the current problems associated with AKR1C3 inhibitors with the aim of providing a reference for future drug discovery and potential therapeutic perspectives on novel, potent, selective AKR1C3 inhibitors.

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Year:  2020        PMID: 32463235     DOI: 10.1021/acs.jmedchem.9b02138

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  7 in total

1.  The ADAM9/UBN2/AKR1C3 axis promotes resistance to androgen-deprivation in prostate cancer.

Authors:  Trang Thi-Huynh Le; Chia-Ling Hsieh; I-Hsuan Lin; Cheng-Ying Chu; Anh Duy Do; Seu-Hwa Chen; Katsumi Shigemura; Koichi Kitagawa; Masato Fujisawa; Ming-Che Liu; Kuan-Chou Chen; Shian-Ying Sung
Journal:  Am J Cancer Res       Date:  2022-01-15       Impact factor: 6.166

2.  Discovery of Novel Aldo-Keto Reductase 1C3 Inhibitors as Chemotherapeutic Potentiators for Cancer Drug Resistance.

Authors:  Siyu He; Yang Liu; Xianglin Chu; Qi Li; Weiping Lyu; Yijun Liu; Shuaishuai Xing; Feng Feng; Wenyuan Liu; Qinglong Guo; Li Zhao; Haopeng Sun
Journal:  ACS Med Chem Lett       Date:  2022-07-08       Impact factor: 4.632

3.  Isocitrate dehydrogenase 2 inhibitor enasidenib synergizes daunorubicin cytotoxicity by targeting aldo-keto reductase 1C3 and ATP-binding cassette transporters.

Authors:  Anselm Morell; Youssif Budagaga; Dimitrios Vagiannis; Yu Zhang; Lenka Laštovičková; Eva Novotná; Andrew Haddad; Melodie Haddad; Ramon Portillo; Jakub Hofman; Vladimír Wsól
Journal:  Arch Toxicol       Date:  2022-08-16       Impact factor: 6.168

4.  Bruton's Tyrosine Kinase Inhibitors Ibrutinib and Acalabrutinib Counteract Anthracycline Resistance in Cancer Cells Expressing AKR1C3.

Authors:  Anselm Morell; Lucie Čermáková; Eva Novotná; Lenka Laštovičková; Melodie Haddad; Andrew Haddad; Ramon Portillo; Vladimír Wsól
Journal:  Cancers (Basel)       Date:  2020-12-11       Impact factor: 6.639

5.  Analogues of Natural Chalcones as Efficient Inhibitors of AKR1C3.

Authors:  Gabriele Möller; Veronika Temml; Antonio Cala Peralta; Océane Gruet; Pascal Richomme; Denis Séraphin; Guillaume Viault; Luisa Kraus; Petra Huber-Cantonati; Elisabeth Schopfhauser; Johanna Pachmayr; Janina Tokarz; Daniela Schuster; Jean-Jacques Helesbeux; Kenneth Allen Dyar
Journal:  Metabolites       Date:  2022-01-21

6.  Unraveling the differential impact of PAHs and dioxin-like compounds on AKR1C3 reveals the EGFR extracellular domain as a critical determinant of the AHR response.

Authors:  Christian Vogeley; Natalie C Sondermann; Selina Woeste; Afaque A Momin; Viola Gilardino; Frederick Hartung; Markus Heinen; Sophia K Maaß; Melina Mescher; Marius Pollet; Katharina M Rolfes; Christoph F A Vogel; Andrea Rossi; Dieter Lang; Stefan T Arold; Motoki Nakamura; Thomas Haarmann-Stemmann
Journal:  Environ Int       Date:  2021-11-20       Impact factor: 9.621

7.  Knockdown of AKR1C3 Promoted Sorafenib Sensitivity Through Inhibiting the Phosphorylation of AKT in Hepatocellular Carcinoma.

Authors:  Jia Zheng; Zhihong Yang; Yanlei Li; Li Yang; Ruili Yao
Journal:  Front Oncol       Date:  2022-03-11       Impact factor: 6.244

  7 in total

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