Browsing by author "Pancholi, Sunil"
Now showing items 1-11 of 11
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ABC-transporter upregulation mediates resistance to the CDK7 inhibitors THZ1 and ICEC0942.
Sava, GP; Fan, H; Fisher, RA; Lusvarghi, S; Pancholi, S; et al. (NATURE PUBLISHING GROUP, 2020-01-01)The CDK7 inhibitors (CDK7i) ICEC0942 and THZ1, are promising new cancer therapeutics. Resistance to targeted drugs frequently compromises cancer treatment. We sought to identify mechanisms by which cancer cells may become ... -
Abiraterone shows alternate activity in models of endocrine resistant and sensitive disease.
Simigdala, N; Pancholi, S; Ribas, R; Folkerd, E; Liccardi, G; et al. (SPRINGERNATURE, 2018-08-01)BACKGROUND: Resistance to endocrine therapy remains a major clinical problem in the treatment of oestrogen-receptor positive (ER+) breast cancer. Studies show androgen-receptor (AR) remains present in 80-90% of metastatic ... -
Cholesterol biosynthesis pathway as a novel mechanism of resistance to estrogen deprivation in estrogen receptor-positive breast cancer.
Simigdala, N; Gao, Q; Pancholi, S; Roberg-Larsen, H; Zvelebil, M; et al. (BMC, 2016-06-01)BACKGROUND: Therapies targeting estrogenic stimulation in estrogen receptor-positive (ER+) breast cancer (BC) reduce mortality, but resistance remains a major clinical problem. Molecular studies have shown few high-frequency ... -
Combination of mTORC1/2 inhibitor vistusertib plus fulvestrant in vitro and in vivo targets oestrogen receptor-positive endocrine-resistant breast cancer.
Pancholi, S; Leal, MF; Ribas, R; Simigdala, N; Schuster, E; et al. (BMC, 2019-12-04)BACKGROUND: Endocrine therapies are still the main strategy for the treatment of oestrogen receptor-positive (ER+) breast cancers (BC), but resistance remains problematic. Cross-talk between ER and PI3K/AKT/mTORC has been ... -
Discovery of naturally occurring ESR1 mutations in breast cancer cell lines modelling endocrine resistance.
Martin, L-A; Ribas, R; Simigdala, N; Schuster, E; Pancholi, S; et al. (NATURE PORTFOLIO, 2017-11-30)Resistance to endocrine therapy remains a major clinical problem in breast cancer. Genetic studies highlight the potential role of estrogen receptor-α (ESR1) mutations, which show increased prevalence in the metastatic, ... -
Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ERαWT and ERαMUT Breast Cancer.
Puyang, X; Furman, C; Zheng, GZ; Wu, ZJ; Banka, D; et al. (AMER ASSOC CANCER RESEARCH, 2018-09-01)Mutations in estrogen receptor alpha (ERα) that confer resistance to existing classes of endocrine therapies are detected in up to 30% of patients who have relapsed during endocrine treatments. Because a significant ... -
GDNF-RET signaling in ER-positive breast cancers is a key determinant of response and resistance to aromatase inhibitors.
Morandi, A; Martin, L-A; Gao, Q; Pancholi, S; Mackay, A; et al. (AMER ASSOC CANCER RESEARCH, 2013-06-15)Most breast cancers at diagnosis are estrogen receptor-positive (ER(+)) and depend on estrogen for growth and survival. Blocking estrogen biosynthesis by aromatase inhibitors has therefore become a first-line endocrine ... -
Src Is a Potential Therapeutic Target in Endocrine-Resistant Breast Cancer Exhibiting Low Estrogen Receptor-Mediated Transactivation.
Guest, SK; Ribas, R; Pancholi, S; Nikitorowicz-Buniak, J; Simigdala, N; et al. (PUBLIC LIBRARY SCIENCE, 2016-06-16)Despite the effectiveness of endocrine therapies in estrogen receptor positive (ER+) breast cancer, approximately 40% of patients relapse. Previously, we identified the Focal-adhesion kinase canonical pathway as a major ... -
Targeting tumour re-wiring by triple blockade of mTORC1, epidermal growth factor, and oestrogen receptor signalling pathways in endocrine-resistant breast cancer.
Ribas, R; Pancholi, S; Rani, A; Schuster, E; Guest, SK; et al. (BIOMED CENTRAL LTD, 2018-06-08)BACKGROUND: Endocrine therapies are the mainstay of treatment for oestrogen receptor (ER)-positive (ER+) breast cancer (BC). However, resistance remains problematic largely due to enhanced cross-talk between ER and growth ... -
The Lineage Determining Factor GRHL2 Collaborates with FOXA1 to Establish a Targetable Pathway in Endocrine Therapy-Resistant Breast Cancer.
Cocce, KJ; Jasper, JS; Desautels, TK; Everett, L; Wardell, S; et al. (CELL PRESS, 2019-10-22)Notwithstanding the positive clinical impact of endocrine therapies in estrogen receptor-alpha (ERα)-positive breast cancer, de novo and acquired resistance limits the therapeutic lifespan of existing drugs. Taking the ... -
Tumour kinome re-wiring governs resistance to palbociclib in oestrogen receptor positive breast cancers, highlighting new therapeutic modalities.
Pancholi, S; Ribas, R; Simigdala, N; Schuster, E; Nikitorowicz-Buniak, J; et al. (SPRINGERNATURE, 2020-06-18)Combination of CDK4/6 inhibitors and endocrine therapy improves clinical outcome in advanced oestrogen receptor (ER)-positive breast cancer, however relapse is inevitable. Here, we show in model systems that other than ...