BIOMARKERS

Molecular Biopsy of Human Tumors

- a resource for Precision Medicine *

209 related articles for article (PubMed ID: 24981575)

  • 1. In vitro and in vivo characterisation of ASP9521: a novel, selective, orally bioavailable inhibitor of 17β-hydroxysteroid dehydrogenase type 5 (17βHSD5; AKR1C3).
    Kikuchi A; Furutani T; Azami H; Watanabe K; Niimi T; Kamiyama Y; Kuromitsu S; Baskin-Bey E; Heeringa M; Ouatas T; Enjo K
    Invest New Drugs; 2014 Oct; 32(5):860-70. PubMed ID: 24981575
    [TBL] [Abstract][Full Text] [Related]  

  • 2. Discovery of 2-methyl-1-{1-[(5-methyl-1H-indol-2-yl)carbonyl]piperidin-4-yl}propan-2-ol: a novel, potent and selective type 5 17β-hydroxysteroid dehydrogenase inhibitor.
    Watanabe K; Kakefuda A; Yasuda M; Enjo K; Kikuchi A; Furutani T; Naritomi Y; Otsuka Y; Okada M; Ohta M
    Bioorg Med Chem; 2013 Sep; 21(17):5261-70. PubMed ID: 23845281
    [TBL] [Abstract][Full Text] [Related]  

  • 3. Safety, tolerability and anti-tumour activity of the androgen biosynthesis inhibitor ASP9521 in patients with metastatic castration-resistant prostate cancer: multi-centre phase I/II study.
    Loriot Y; Fizazi K; Jones RJ; Van den Brande J; Molife RL; Omlin A; James ND; Baskin-Bey E; Heeringa M; Baron B; Holtkamp GM; Ouatas T; De Bono JS
    Invest New Drugs; 2014 Oct; 32(5):995-1004. PubMed ID: 24771350
    [TBL] [Abstract][Full Text] [Related]  

  • 4. Overexpression of aldo-keto reductase 1C3 (AKR1C3) in LNCaP cells diverts androgen metabolism towards testosterone resulting in resistance to the 5α-reductase inhibitor finasteride.
    Byrns MC; Mindnich R; Duan L; Penning TM
    J Steroid Biochem Mol Biol; 2012 May; 130(1-2):7-15. PubMed ID: 22265960
    [TBL] [Abstract][Full Text] [Related]  

  • 5. 11-Oxygenated androgen precursors are the preferred substrates for aldo-keto reductase 1C3 (AKR1C3): Implications for castration resistant prostate cancer.
    Barnard M; Quanson JL; Mostaghel E; Pretorius E; Snoep JL; Storbeck KH
    J Steroid Biochem Mol Biol; 2018 Oct; 183():192-201. PubMed ID: 29936123
    [TBL] [Abstract][Full Text] [Related]  

  • 6. Steroidogenic enzyme AKR1C3 is a novel androgen receptor-selective coactivator that promotes prostate cancer growth.
    Yepuru M; Wu Z; Kulkarni A; Yin F; Barrett CM; Kim J; Steiner MS; Miller DD; Dalton JT; Narayanan R
    Clin Cancer Res; 2013 Oct; 19(20):5613-25. PubMed ID: 23995860
    [TBL] [Abstract][Full Text] [Related]  

  • 7. A 3-(4-nitronaphthen-1-yl) amino-benzoate analog as a bifunctional AKR1C3 inhibitor and AR antagonist: Head to head comparison with other advanced AKR1C3 targeted therapeutics.
    Wangtrakuldee P; Adeniji AO; Zang T; Duan L; Khatri B; Twenter BM; Estrada MA; Higgins TF; Winkler JD; Penning TM
    J Steroid Biochem Mol Biol; 2019 Sep; 192():105283. PubMed ID: 30641225
    [TBL] [Abstract][Full Text] [Related]  

  • 8. A Mansonone Derivative Coupled with Monoclonal Antibody 4D5-Modified Chitosan Inhibit AKR1C3 to Treat Castration-Resistant Prostate Cancer.
    Zhou M; Wang X; Xia J; Cheng Y; Xiao L; Bei Y; Tang J; Huang Y; Xiang Q; Huang S
    Int J Nanomedicine; 2020; 15():3087-3098. PubMed ID: 32431503
    [TBL] [Abstract][Full Text] [Related]  

  • 9. Development of potent and selective inhibitors of aldo-keto reductase 1C3 (type 5 17β-hydroxysteroid dehydrogenase) based on N-phenyl-aminobenzoates and their structure-activity relationships.
    Adeniji AO; Twenter BM; Byrns MC; Jin Y; Chen M; Winkler JD; Penning TM
    J Med Chem; 2012 Mar; 55(5):2311-23. PubMed ID: 22263837
    [TBL] [Abstract][Full Text] [Related]  

  • 10. Screening baccharin analogs as selective inhibitors against type 5 17β-hydroxysteroid dehydrogenase (AKR1C3).
    Zang T; Verma K; Chen M; Jin Y; Trippier PC; Penning TM
    Chem Biol Interact; 2015 Jun; 234():339-48. PubMed ID: 25555457
    [TBL] [Abstract][Full Text] [Related]  

  • 11. An indomethacin analogue, N-(4-chlorobenzoyl)-melatonin, is a selective inhibitor of aldo-keto reductase 1C3 (type 2 3alpha-HSD, type 5 17beta-HSD, and prostaglandin F synthase), a potential target for the treatment of hormone dependent and hormone independent malignancies.
    Byrns MC; Steckelbroeck S; Penning TM
    Biochem Pharmacol; 2008 Jan; 75(2):484-93. PubMed ID: 17950253
    [TBL] [Abstract][Full Text] [Related]  

  • 12. Hydroxytriazole derivatives as potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors discovered by bioisosteric scaffold hopping approach.
    Pippione AC; Giraudo A; Bonanni D; Carnovale IM; Marini E; Cena C; Costale A; Zonari D; Pors K; Sadiq M; Boschi D; Oliaro-Bosso S; Lolli ML
    Eur J Med Chem; 2017 Oct; 139():936-946. PubMed ID: 28881288
    [TBL] [Abstract][Full Text] [Related]  

  • 13. Potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors based on the benzoisoxazole moiety: application of a bioisosteric scaffold hopping approach to flufenamic acid.
    Pippione AC; Carnovale IM; Bonanni D; Sini M; Goyal P; Marini E; Pors K; Adinolfi S; Zonari D; Festuccia C; Wahlgren WY; Friemann R; Bagnati R; Boschi D; Oliaro-Bosso S; Lolli ML
    Eur J Med Chem; 2018 Apr; 150():930-945. PubMed ID: 29602039
    [TBL] [Abstract][Full Text] [Related]  

  • 14. Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer.
    Liedtke AJ; Adeniji AO; Chen M; Byrns MC; Jin Y; Christianson DW; Marnett LJ; Penning TM
    J Med Chem; 2013 Mar; 56(6):2429-46. PubMed ID: 23432095
    [TBL] [Abstract][Full Text] [Related]  

  • 15. Aldo-keto reductase 1C3 expression in MCF-7 cells reveals roles in steroid hormone and prostaglandin metabolism that may explain its over-expression in breast cancer.
    Byrns MC; Duan L; Lee SH; Blair IA; Penning TM
    J Steroid Biochem Mol Biol; 2010 Feb; 118(3):177-87. PubMed ID: 20036328
    [TBL] [Abstract][Full Text] [Related]  

  • 16. AKR1C3 Inhibitor KV-37 Exhibits Antineoplastic Effects and Potentiates Enzalutamide in Combination Therapy in Prostate Adenocarcinoma Cells.
    Verma K; Gupta N; Zang T; Wangtrakluldee P; Srivastava SK; Penning TM; Trippier PC
    Mol Cancer Ther; 2018 Sep; 17(9):1833-1845. PubMed ID: 29891491
    [TBL] [Abstract][Full Text] [Related]  

  • 17. Aldo-keto reductase family 1 member C3 (AKR1C3) is a biomarker and therapeutic target for castration-resistant prostate cancer.
    Hamid AR; Pfeiffer MJ; Verhaegh GW; Schaafsma E; Brandt A; Sweep FC; Sedelaar JP; Schalken JA
    Mol Med; 2013 Jan; 18(1):1449-55. PubMed ID: 23196782
    [TBL] [Abstract][Full Text] [Related]  

  • 18. Discovery of (R)-2-(6-Methoxynaphthalen-2-yl)butanoic Acid as a Potent and Selective Aldo-keto Reductase 1C3 Inhibitor.
    Adeniji A; Uddin MJ; Zang T; Tamae D; Wangtrakuldee P; Marnett LJ; Penning TM
    J Med Chem; 2016 Aug; 59(16):7431-44. PubMed ID: 27486833
    [TBL] [Abstract][Full Text] [Related]  

  • 19. In Silico and In Vitro Assessment of Carbonyl Reductase 1 Inhibition Using ASP9521-A Potent Aldo-Keto Reductase 1C3 Inhibitor with the Potential to Support Anticancer Therapy Using Anthracycline Antibiotics.
    Jamrozik M; Piska K; Bucki A; Koczurkiewicz-Adamczyk P; Sapa M; Władyka B; Pękala E; Kołaczkowski M
    Molecules; 2023 Apr; 28(9):. PubMed ID: 37175180
    [TBL] [Abstract][Full Text] [Related]  

  • 20. Structure-function aspects and inhibitor design of type 5 17beta-hydroxysteroid dehydrogenase (AKR1C3).
    Penning TM; Burczynski ME; Jez JM; Lin HK; Ma H; Moore M; Ratnam K; Palackal N
    Mol Cell Endocrinol; 2001 Jan; 171(1-2):137-49. PubMed ID: 11165022
    [TBL] [Abstract][Full Text] [Related]  

    [Next]    [New Search]
    of 11.