Cited by 274Prostate Cancer Treatment and ResearchEstrogen and related hormone effectsSperm and Testicular Function

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Activated Cdc42-associated kinase Ack1 promotes prostate cancer progression via androgen receptor tyrosine phosphorylation.

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Mahajan, Nupam P., Liu, Yuanbo, Majumder, Samarpan, Warren, Maria R., Parker, Carol E., Mohler, James L., Earp, H. Shelton, Whang, Young E.·2007·Proceedings of the National Academy of Sciences

DOI 10.1073/pnas.0700420104PMC PMC1895968

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Abstract

Activation of the androgen receptor (AR) may play a role in androgen-independent progression of prostate cancer. Multiple mechanisms of AR activation, including stimulation by tyrosine kinases, have been postulated. We and others have recently shown involvement of activated Cdc42-associated tyrosine kinase Ack1 in advanced human prostate cancer. Here we provide the molecular basis for interplay between Ack1 and AR in prostate cancer cells. Activated Ack1 promoted androgen-independent growth of LNCaP and LAPC-4 prostate xenograft tumors, AR recruitment to the androgen-responsive enhancer, and androgen-inducible gene expression in the absence of androgen. Heregulin-stimulated HER2 activation induced Ack1 activation and AR tyrosine phosphorylation. Ack1 knockdown inhibited heregulin-dependent AR tyrosine phosphorylation, AR reporter activity, androgen-stimulated gene expression, and AR recruitment. Ack1 was recruited to the androgen-responsive enhancers after androgen and heregulin stimulation. In 8 of 18 primary androgen-independent prostate tumor samples, tyrosine-phosphorylated AR protein was detected and correlated with the detection of tyrosine-phosphorylated Ack1. Neither was elevated in androgen-dependent tumors or benign prostate samples. Activated Ack1 phosphorylated AR protein at Tyr-267 and Tyr-363, both located within the transactivation domain. Mutation of Tyr-267 completely abrogated and mutation of Tyr-363 reduced Ack1-induced AR reporter activation and recruitment of AR to the androgen-responsive enhancer. Expression of AR point mutants inhibited Ack1-driven xenograft tumor growth. Thus, Ack1 activated by surface signals or oncogenic mechanisms may directly enhance AR transcriptional function and promote androgen-independent progression of prostate cancer. Targeting the Ack1 kinase may be a potential therapeutic strategy in prostate cancer.

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Authors: Mahajan, N. P., Liu, Y., Majumder, S., Warren, M. R., Parker, C. E., Mohler, J. L., Earp, H. S., & Whang, Y. E.
Affiliations: University of North Carolina at Chapel Hill (US)
UNC Lineberger Comprehensive Cancer Center (US)
Biochemistry and Biophysics,
Roswell Park Comprehensive Cancer Center (US)
ORCID: Mahajan, Nupam P.
Liu, Yuanbo
Majumder, Samarpan
Mohler, James L.
Earp, H. Shelton
Whang, Young E.
Venue: Proceedings of the National Academy of Sciences
Publisher: National Academy of Sciences
Published: 2007-05-15
Volume: 104
Issue: 20
Pages: 8438-8443
ISSN: 0027-8424 (ISSN-L)
1091-6490
DOI: 10.1073/pnas.0700420104
PMC: PMC1895968
OpenAlex: W2055013229
Cited by: 274
References: 26
Citations by year: 2026: 3 · 2025: 7 · 2024: 9 · 2023: 17 · 2022: 28 · 2021: 9 · 2020: 11 · 2019: 13 · 2018: 11 · 2017: 11 · 2016: 11 · 2015: 15 · 2014: 19 · 2013: 24 · 2012: 21
FWCI: 14.40
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Locations: Proceedings of the National Academy of Sciences (publishedVersion)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
Carolina Digital Repository (University of North Carolina at Chapel Hill) (submittedVersion)
UNC Libraries
Funders: Elsa U. Pardee Foundation
National Institutes of Health (CA77739)
Genentech
University of North Carolina at Chapel Hill
National Cancer Institute (R21CA100700, CA-77739, R01CA112553, P01CA077739, CA 100700, K08CA085772, CA085772, CA112553)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Prostate Cancer Treatment and Research
Life Sciences › Biochemistry, Genetics and Molecular Biology › Endocrinology › Estrogen and related hormone effects
Health Sciences › Medicine › Reproductive Medicine › Sperm and Testicular Function
Keywords: ACK1, androgen receptor, prostate cancer, androgen-independent progression, tyrosine phosphorylation, neuregulin-1, HER2, LNCaP cells, transcriptional activation
MeSH terms: Androgens, Animals, DNA, Neoplasm, Enhancer Elements, Genetic, Enzyme Activation, Humans, Male, Models, Genetic, Mutation, Phosphorylation, Prostatic Neoplasms, Protein Binding, Protein-Tyrosine Kinases, Receptors, Androgen, Transcription, Genetic, Transplantation, Heterologous, Gene Expression Regulation, Neoplastic, Disease Progression, Erb-b2 Receptor Tyrosine Kinases, Phosphotyrosine, Neuregulin-1, Protein Transport, Cell Line, Tumor, Mice

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Activated Cdc42-associated kinase Ack1 promotes prostate cancer progression via androgen receptor tyrosine phosphorylation.

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