Now showing items 1-8 of 8

    • Binding to an Unusual Inactive Kinase Conformation by Highly Selective Inhibitors of Inositol-Requiring Enzyme 1α Kinase-Endoribonuclease. 

      Colombano, G; Caldwell, JJ; Matthews, TP; Bhatia, C; Joshi, A; McHardy, T; Mok, NY; Newbatt, Y; Pickard, L; Strover, J; Hedayat, S; Walton, MI; Myers, SM; Jones, AM; Saville, H; McAndrew, C; Burke, R; Eccles, SA; Davies, FE; Bayliss, R; Collins, I (2019-03-14)
      A series of imidazo[1,2- b]pyridazin-8-amine kinase inhibitors were discovered to allosterically inhibit the endoribonuclease function of the dual kinase-endoribonuclease inositol-requiring enzyme 1α (IRE1α), a key component ...
    • Functional imaging and circulating biomarkers of response to regorafenib in treatment-refractory metastatic colorectal cancer patients in a prospective phase II study. 

      Khan, K; Rata, M; Cunningham, D; Koh, D-M; Tunariu, N; Hahne, JC; Vlachogiannis, G; Hedayat, S; Marchetti, S; Lampis, A; Damavandi, MD; Lote, H; Rana, I; Williams, A; Eccles, SA; Fontana, E; Collins, D; Eltahir, Z; Rao, S; Watkins, D; Starling, N; Thomas, J; Kalaitzaki, E; Fotiadis, N; Begum, R; Bali, M; Rugge, M; Temple, E; Fassan, M; Chau, I; Braconi, C; Valeri, N (2018-08)
      OBJECTIVE: Regorafenib demonstrated efficacy in patients with metastatic colorectal cancer (mCRC). Lack of predictive biomarkers, potential toxicities and cost-effectiveness concerns highlight the unmet need for better ...
    • HSF1 Is Essential for Myeloma Cell Survival and A Promising Therapeutic Target. 

      Fok, JHL; Hedayat, S; Zhang, L; Aronson, LI; Mirabella, F; Pawlyn, C; Bright, MD; Wardell, CP; Keats, JJ; De Billy, E; Rye, CS; Chessum, NEA; Jones, K; Morgan, GJ; Eccles, SA; Workman, P; Davies, FE (2018-05-15)
      Purpose: Myeloma is a plasma cell malignancy characterized by the overproduction of immunoglobulin, and is therefore susceptible to therapies targeting protein homeostasis. We hypothesized that heat shock factor 1 (HSF1) ...
    • Longitudinal Liquid Biopsy and Mathematical Modeling of Clonal Evolution Forecast Time to Treatment Failure in the PROSPECT-C Phase II Colorectal Cancer Clinical Trial. 

      Khan, KH; Cunningham, D; Werner, B; Vlachogiannis, G; Spiteri, I; Heide, T; Mateos, JF; Vatsiou, A; Lampis, A; Damavandi, MD; Lote, H; Huntingford, IS; Hedayat, S; Chau, I; Tunariu, N; Mentrasti, G; Trevisani, F; Rao, S; Anandappa, G; Watkins, D; Starling, N; Thomas, J; Peckitt, C; Khan, N; Rugge, M; Begum, R; Hezelova, B; Bryant, A; Jones, T; Proszek, P; Fassan, M; Hahne, JC; Hubank, M; Braconi, C; Sottoriva, A; Valeri, N (2018-10)
      Sequential profiling of plasma cell-free DNA (cfDNA) holds immense promise for early detection of patient progression. However, how to exploit the predictive power of cfDNA as a liquid biopsy in the clinic remains unclear. ...
    • miR-31-3p Expression and Benefit from Anti-EGFR Inhibitors in Metastatic Colorectal Cancer Patients Enrolled in the Prospective Phase II PROSPECT-C Trial. 

      Anandappa, G; Lampis, A; Cunningham, D; Khan, KH; Kouvelakis, K; Vlachogiannis, G; Hedayat, S; Tunariu, N; Rao, S; Watkins, D; Starling, N; Braconi, C; Darvish-Damavandi, M; Lote, H; Thomas, J; Peckitt, C; Kalaitzaki, R; Khan, N; Fotiadis, N; Rugge, M; Begum, R; Rana, I; Bryant, A; Hahne, JC; Chau, I; Fassan, M; Valeri, N (2019-07-01)
      PURPOSE: Anti-EGFR mAbs are effective in the treatment of metastatic colorectal cancer (mCRC) patients. RAS status and tumor location (sidedness) are predictive markers of patients' response to anti-EGFR mAbs. Recently, ...
    • MIR21 Drives Resistance to Heat Shock Protein 90 Inhibition in Cholangiocarcinoma. 

      Lampis, A; Carotenuto, P; Vlachogiannis, G; Cascione, L; Hedayat, S; Burke, R; Clarke, P; Bosma, E; Simbolo, M; Scarpa, A; Yu, S; Cole, R; Smyth, E; Mateos, JF; Begum, R; Hezelova, B; Eltahir, Z; Wotherspoon, A; Fotiadis, N; Bali, MA; Nepal, C; Khan, K; Stubbs, M; Hahne, JC; Gasparini, P; Guzzardo, V; Croce, CM; Eccles, S; Fassan, M; Cunningham, D; Andersen, JB; Workman, P; Valeri, N; Braconi, C (2018-03)
      BACKGROUND & AIMS: Cholangiocarcinomas (CCA) are resistant to chemotherapy, so new therapeutic agents are needed. We performed a screen to identify small-molecule compounds that are active against CCAs. Levels of microRNA ...
    • Patient-derived organoids model treatment response of metastatic gastrointestinal cancers. 

      Vlachogiannis, G; Hedayat, S; Vatsiou, A; Jamin, Y; Fernández-Mateos, J; Khan, K; Lampis, A; Eason, K; Huntingford, I; Burke, R; Rata, M; Koh, D-M; Tunariu, N; Collins, D; Hulkki-Wilson, S; Ragulan, C; Spiteri, I; Moorcraft, SY; Chau, I; Rao, S; Watkins, D; Fotiadis, N; Bali, M; Darvish-Damavandi, M; Lote, H; Eltahir, Z; Smyth, EC; Begum, R; Clarke, PA; Hahne, JC; Dowsett, M; de Bono, J; Workman, P; Sadanandam, A; Fassan, M; Sansom, OJ; Eccles, S; Starling, N; Braconi, C; Sottoriva, A; Robinson, SP; Cunningham, D; Valeri, N (2018-02-23)
      Patient-derived organoids (PDOs) have recently emerged as robust preclinical models; however, their potential to predict clinical outcomes in patients has remained unclear. We report on a living biobank of PDOs from ...
    • Second-Generation HSP90 Inhibitor Onalespib Blocks mRNA Splicing of Androgen Receptor Variant 7 in Prostate Cancer Cells. 

      Ferraldeschi, R; Welti, J; Powers, MV; Yuan, W; Smyth, T; Seed, G; Riisnaes, R; Hedayat, S; Wang, H; Crespo, M; Nava Rodrigues, D; Figueiredo, I; Miranda, S; Carreira, S; Lyons, JF; Sharp, S; Plymate, SR; Attard, G; Wallis, N; Workman, P; de Bono, JS (2016-05)
      Resistance to available hormone therapies in prostate cancer has been associated with alternative splicing of androgen receptor (AR) and specifically, the expression of truncated and constitutively active AR variant 7 ...