Matches in SemOpenAlex for { <https://semopenalex.org/work/W4362494568> ?p ?o ?g. }
Showing items 1 to 62 of
62
with 100 items per page.
- W4362494568 abstract "<div>Abstract<p>Clinical management of castration-resistant prostate cancer (CRPC) resulting from androgen deprivation therapy remains challenging. CRPC is driven by aberrant activation of androgen receptor (AR) through mechanisms ranging from its amplification, mutation, post-translational modification, and expression of splice variants (e.g., AR-V7). Herein, we present experimental evidence for therapeutic vulnerability of CRPC to a novel phytochemical, leelamine (LLM), derived from pine tree bark. Exposure of human prostate cancer cell lines LNCaP (an androgen-responsive cell line with mutant AR), C4-2B (an androgen-insensitive variant of LNCaP), and 22Rv1 (a CRPC cell line with expression of AR-Vs), and a murine prostate cancer cell line Myc-CaP to plasma achievable concentrations of LLM resulted in ligand-dependent (LNCaP) and ligand-independent (22Rv1) growth inhibition <i>in vitro</i> that was accompanied by downregulation of mRNA and/or protein levels of full-length AR as well as its splice variants, including AR-V7. LLM treatment resulted in apoptosis induction in the absence and presence of R1881. <i>In silico</i> modeling followed by luciferase reporter assay revealed a critical role for noncovalent interaction of LLM with Y739 in AR activity inhibition. Substitution of the amine group with an isothiocyanate functional moiety abolished AR and cell viability inhibition by LLM. Administration of LLM resulted in 22Rv1 xenograft growth suppression that was statistically insignificant but was associated with a significant decrease in Ki-67 expression, mitotic activity, expression of full-length AR and AR-V7 proteins, and secretion of PSA. This study identifies a novel chemical scaffold for the treatment of CRPC. <i>Mol Cancer Ther; 17(10); 2079–90. ©2018 AACR</i>.</p></div>" @default.
- W4362494568 created "2023-04-05" @default.
- W4362494568 creator A5022304953 @default.
- W4362494568 creator A5069231811 @default.
- W4362494568 creator A5081980683 @default.
- W4362494568 date "2023-04-03" @default.
- W4362494568 modified "2023-09-29" @default.
- W4362494568 title "Data from Therapeutic Potential of Leelamine, a Novel Inhibitor of Androgen Receptor and Castration-Resistant Prostate Cancer" @default.
- W4362494568 doi "https://doi.org/10.1158/1535-7163.c.6537730.v1" @default.
- W4362494568 hasPublicationYear "2023" @default.
- W4362494568 type Work @default.
- W4362494568 citedByCount "0" @default.
- W4362494568 crossrefType "posted-content" @default.
- W4362494568 hasAuthorship W4362494568A5022304953 @default.
- W4362494568 hasAuthorship W4362494568A5069231811 @default.
- W4362494568 hasAuthorship W4362494568A5081980683 @default.
- W4362494568 hasBestOaLocation W43624945682 @default.
- W4362494568 hasConcept C121608353 @default.
- W4362494568 hasConcept C126322002 @default.
- W4362494568 hasConcept C134018914 @default.
- W4362494568 hasConcept C185592680 @default.
- W4362494568 hasConcept C2776551883 @default.
- W4362494568 hasConcept C2777899217 @default.
- W4362494568 hasConcept C2777911890 @default.
- W4362494568 hasConcept C2779723316 @default.
- W4362494568 hasConcept C2780192828 @default.
- W4362494568 hasConcept C502942594 @default.
- W4362494568 hasConcept C61367390 @default.
- W4362494568 hasConcept C71315377 @default.
- W4362494568 hasConcept C71924100 @default.
- W4362494568 hasConcept C86803240 @default.
- W4362494568 hasConceptScore W4362494568C121608353 @default.
- W4362494568 hasConceptScore W4362494568C126322002 @default.
- W4362494568 hasConceptScore W4362494568C134018914 @default.
- W4362494568 hasConceptScore W4362494568C185592680 @default.
- W4362494568 hasConceptScore W4362494568C2776551883 @default.
- W4362494568 hasConceptScore W4362494568C2777899217 @default.
- W4362494568 hasConceptScore W4362494568C2777911890 @default.
- W4362494568 hasConceptScore W4362494568C2779723316 @default.
- W4362494568 hasConceptScore W4362494568C2780192828 @default.
- W4362494568 hasConceptScore W4362494568C502942594 @default.
- W4362494568 hasConceptScore W4362494568C61367390 @default.
- W4362494568 hasConceptScore W4362494568C71315377 @default.
- W4362494568 hasConceptScore W4362494568C71924100 @default.
- W4362494568 hasConceptScore W4362494568C86803240 @default.
- W4362494568 hasLocation W43624945681 @default.
- W4362494568 hasLocation W43624945682 @default.
- W4362494568 hasOpenAccess W4362494568 @default.
- W4362494568 hasPrimaryLocation W43624945681 @default.
- W4362494568 hasRelatedWork W1528618484 @default.
- W4362494568 hasRelatedWork W1970062306 @default.
- W4362494568 hasRelatedWork W2469134207 @default.
- W4362494568 hasRelatedWork W2503901337 @default.
- W4362494568 hasRelatedWork W2740124347 @default.
- W4362494568 hasRelatedWork W2931472946 @default.
- W4362494568 hasRelatedWork W2948523439 @default.
- W4362494568 hasRelatedWork W3198382015 @default.
- W4362494568 hasRelatedWork W4287355568 @default.
- W4362494568 hasRelatedWork W4206870430 @default.
- W4362494568 isParatext "false" @default.
- W4362494568 isRetracted "false" @default.
- W4362494568 workType "article" @default.