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CYP17 inhibitors for prostate cancer therapyNovel retinoic acid metabolism blocking agents have potent inhibitory activities on human breast cancer cells and tumour growth.17alpha-Hydroxylase/17,20 lyase inhibitor VN/124-1 inhibits growth of androgen-independent prostate cancer cells via induction of the endoplasmic reticulum stress response.VN/14-1 induces ER stress and autophagy in HP-LTLC human breast cancer cells and has excellent oral pharmacokinetic profile in female Sprague Dawley ratsTargeting drug-metabolizing enzymes for effective chemoprevention and chemotherapy.Prolonging hormone sensitivity in prostate cancer xenografts through dual inhibition of AR and mTOR.The Coffey Lecture: steroidogenic enzyme inhibitors and hormone dependent cancerStructure-Based Screen Identifies a Potent Small Molecule Inhibitor of Stat5a/b with Therapeutic Potential for Prostate Cancer and Chronic Myeloid Leukemia.First chemical feature-based pharmacophore modeling of potent retinoidal retinoic acid metabolism blocking agents (RAMBAs): identification of novel RAMBA scaffolds.First pharmacophore-based identification of androgen receptor down-regulating agents: discovery of potent anti-prostate cancer agents.Galeterone and VNPT55 induce proteasomal degradation of AR/AR-V7, induce significant apoptosis via cytochrome c release and suppress growth of castration resistant prostate cancer xenografts in vivo.Retinoic acid metabolism blocking agents (RAMBAs) for treatment of cancer and dermatological diseases.The combination of the histone deacetylase inhibitor vorinostat and synthetic triterpenoids reduces tumorigenesis in mouse models of cancerRetinoids in clinical use.MS-275 synergistically enhances the growth inhibitory effects of RAMBA VN/66-1 in hormone-insensitive PC-3 prostate cancer cells and tumours.Inhibitory effects of retinoic acid metabolism blocking agents (RAMBAs) on the growth of human prostate cancer cells and LNCaP prostate tumour xenografts in SCID mice.Androgen receptor inactivation contributes to antitumor efficacy of 17{alpha}-hydroxylase/17,20-lyase inhibitor 3beta-hydroxy-17-(1H-benzimidazole-1-yl)androsta-5,16-diene in prostate cancer.CYP17 inhibitors for prostate cancer treatment--an update.Murine toxicology and pharmacokinetics evaluation of retinoic acid metabolism blocking agent (RAMBA), VN/12-1.A new simple and high-yield synthesis of 5α-dihydrotestosterone (DHT), a potent androgen receptor agonist.Autophagy inhibition synergistically enhances anticancer efficacy of RAMBA, VN/12-1 in SKBR-3 cells, and tumor xenograftsFirst MNKs degrading agents block phosphorylation of eIF4E, induce apoptosis, inhibit cell growth, migration and invasion in triple negative and Her2-overexpressing breast cancer cell lines.Novel, potent anti-androgens of therapeutic potential: recent advances and promising developments.New insights into the androgen-targeted therapies and epigenetic therapies in prostate cancer.Galeterone and VNPT55 disrupt Mnk-eIF4E to inhibit prostate cancer cell migration and invasion.Dissecting major signaling pathways in prostate cancer development and progression: Mechanisms and novel therapeutic targets.Simultaneous targeting of androgen receptor (AR) and MAPK-interacting kinases (MNKs) by novel retinamides inhibits growth of human prostate cancer cell lines.Targeting of protein translation as a new treatment paradigm for prostate cancer.Design, synthesis, and evaluation of novel mutual prodrugs (hybrid drugs) of all-trans-retinoic acid and histone deacetylase inhibitors with enhanced anticancer activities in breast and prostate cancer cells in vitro.Potent anti-prostate cancer agents derived from a novel androgen receptor down-regulating agent.Synergistic effect of a novel antiandrogen, VN/124-1, and signal transduction inhibitors in prostate cancer progression to hormone independence in vitro.Effects of novel retinoic acid metabolism blocking agent (VN/14-1) on letrozole-insensitive breast cancer cells.Regulation of androgen receptor activity by tyrosine phosphorylation.Pregnenolone stimulates LNCaP prostate cancer cell growth via the mutated androgen receptor.Novel 17-azolyl steroids, potent inhibitors of human cytochrome 17 alpha-hydroxylase-C17,20-lyase (P450(17) alpha): potential agents for the treatment of prostate cancer.Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer.Galeterone and its analogs inhibit Mnk-eIF4E axis, synergize with gemcitabine, impede pancreatic cancer cell migration, invasion and proliferation and inhibit tumor growth in miceIdentification of Novel Steroidal Androgen Receptor Degrading Agents Inspired by Galeterone 3β-Imidazole CarbamateBiotransformation of progesterone to 14 alpha-hydroxypregna-1,4-diene-3,20-dione, a novel fungal metabolite, by Colletotrichum antirrhini.Pharmacokinetic profile of 3beta-hydroxy-17-(1H-1,2,3-triazol-1-yl)androsta-5,16-diene (VN/87-1), a potent androgen synthesis inhibitor, in mice.
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onderzoeker
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researcher
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հետազոտող
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Vincent C Njar
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Vincent C Njar
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Vincent C Njar
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Vincent C Njar
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Vincent C Njar
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Vincent C Njar
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Vincent C Njar
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Vincent C Njar
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Vincent C Njar
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Vincent C Njar
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Vincent C Njar
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Vincent C Njar
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P106
P31
P496
0000-0003-2630-8479