Inhibition of Aurora kinase B is important for biologic activity of the dual inhibitors of BCR-ABL and Aurora kinases R763/AS703569 and PHA-739358 in BCR-ABL transformed cells.

Autor: Anna L Illert, Anna K Seitz, Christoph Rummelt, Stefanie Kreutmair, Richard A Engh, Samantha Goodstal, Christian Peschel, Justus Duyster, Nikolas von Bubnoff

Publikováno v: PLoS ONE, Vol 9, Iss 11, p e112318 (2014)

ABL tyrosine kinase inhibitors (TKI) like Imatinib, Dasatinib and Nilotinib are the gold standard in conventional treatment of CML. However, the emergence of resistance remains a major problem. Alternative therapeutic strategies of ABL TKI-resistant

Externí odkaz: https://doaj.org/article/7cbc95d55e134a64a7319d29adfb3a40

Data from Inhibiting Aurora Kinases Reduces Tumor Growth and Suppresses Tumor Recurrence after Chemotherapy in Patient-Derived Triple-Negative Breast Cancer Xenografts

Autor: Elisabetta Marangoni, Didier Decaudin, Ivan Bièche, Patricia de Cremoux, Samantha Goodstal, Edward Spooner, Xiaohong Liu, Jean-Jacques Fontaine, Jean-Luc Servely, Marie-France Poupon, Sophie Chateau-Joubert, Franck Assayag, Anderson Clark, Angela Romanelli

Triple-negative breast cancers (TNBC) have an aggressive phenotype with a relatively high rate of recurrence and poor overall survival. To date, there is no approved targeted therapy for TNBCs. Aurora kinases act as regulators of mammalian cell divis

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e89dbad1fbc6867b442b41ae31e13342
https://doi.org/10.1158/1535-7163.c.6536178

Data from The MEK1/2 Inhibitor Pimasertib Enhances Gemcitabine Efficacy in Pancreatic Cancer Models by Altering Ribonucleotide Reductase Subunit-1 (RRM1)

Autor: Daniel Hochhauser, John A. Hartley, Thorsten Hagemann, Samantha Goodstal, Manuel Rodriguez-Justo, Eleonora Li Causi, Francesca Vena

Purpose: Gemcitabine, a nucleoside analogue, is an important treatment for locally advanced and metastatic pancreatic ductal adenocarcinoma (PDAC) but provides only modest survival benefit. Targeting downstream effectors of the RAS/ERK signaling path

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78495784fc176fc85661efca19295c32
https://doi.org/10.1158/1078-0432.c.6524828.v1

Selective Oral MEK1/2 Inhibitor Pimasertib in Metastatic Melanoma: Antitumor Activity in a Phase I, Dose-Escalation Trial

Autor: Carlos Gomez-Roca, Sylvie Rottey, Thierry Lesimple, Céleste Lebbé, Ahmad Awada, Celine Pages, Antoine Italiano, Philippe Aftimos, Richard F. Kefford, Armin Schueler, Jean Pierre Delord, Vibeke Kruse, Samantha Goodstal, Nadine Houede, Monica Dinulescu, Suzanne Leijen, Jan H.M. Schellens, Sandrine Faivre, Giorgio Massimini, Eric Raymond

Publikováno v: Targeted Oncology. 16:47-57

Pimasertib is a selective, potent mitogen-activated protein kinase kinase (MEK) 1/2 inhibitor. The aim of this study was to describe the efficacy, safety, and pharmacodynamics of pimasertib at pharmacologically active doses in a cohort of patients wi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c4b54bf40f4ad1adca2f6b4e80520370
https://doi.org/10.1007/s11523-020-00767-1

Pharmacological Perturbation of the Immunoproteasome in Hematologic Neoplasias: Therapeutic Implications

Autor: Richard W.J. Groen, Michael Sanderson, Manja Friese-Hamim, Megan Bariteau, Ricardo De Matos Simoes, Sondra L. Downey-Kopyscinski, Constantine S. Mitsiades, Gina Walter, Samantha Goodstal, Sam Bender, Jennifer Roth, Minasri Borah, Janaka Foneska

Publikováno v: Blood, 134. American Society of Hematology
Downey-Kopyscinski, S L, Simoes, R D M, Bariteau, M, Borah, M L, Bender, S, Foneska, J, Roth, J, Groen, R, Walter, G, Friese-Hamim, M, Goodstal, S M, Sanderson, M & Mitsiades, C S 2019, ' Pharmacological Perturbation of the Immunoproteasome in Hematologic Neoplasias: Therapeutic Implications ', Blood, vol. 134 . https://doi.org/10.1182/blood-2019-130356

Pharmacological inhibition of the canonical proteasome by inhibitors targeting its beta5 (PSMB5) subunit represent a cornerstone of the therapeutic management of plasma cell neoplasias. However, proteasome inhibitors have limited clinical application

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ac8e68f58cf3cbecabfe15f084ed115b
https://doi.org/10.1182/blood-2019-130356