Blood
Ch’ng J, Moll K, Quintana MDP, Chan S, Moles E, Liu J, Eriksson AB, Wahlgren M
Blood 1-13 (2015)
Ch’ng J, Moll K, Quintana MDP, Chan S, Moles E, Liu J, Eriksson AB, Wahlgren M
Blood 1-13 (2015)
Bharadwaj U. ET, Mancini ADJT
Oncogene - vol. 34 1341-1353 (2015)
Signal transducer and activator of transcription (STAT) 3 regulates many cardinal features of cancer including cancer cell growth, apoptosis resistance, DNA damage response, metastasis, immune escape, tumor angiogenesis, the Warburg effect, and oncogene addiction and has been validated as a drug target for cancer therapy. Several strategies have been employed to identify agents that target […]
Yang YHC, Vilin YY, Roberge M, Kurata HT, Johnson JD
Molecular endocrinology - vol. 28 406-417 (2014)
Pancreatic β-cell death plays a role in both type 1 and type 2 diabetes, but clinical treatments that specifically target β-cell survival have not yet been developed. We have recently developed live-cell imaging-based, high-throughput screening methods capable of identifying factors that modulate pancreatic β-cell death, with the hope of finding drugs that can intervene in […]
Voisset C, Daskalogianni C, Contesse M, Mazars A, Arbach H, Le Cann M, Soubigou F, Apcher S, Fåhraeus R, Blondel M
Disease models & mechanisms - vol. 7 435-444 (2014)
Epstein-Barr virus (EBV) is tightly associated with certain human cancers, but there is as yet no specific treatment against EBV-related diseases. The EBV-encoded EBNA1 protein is essential to maintain viral episomes and for viral persistence. As such, EBNA1 is expressed in all EBV-infected cells, and is highly antigenic. All infected individuals, including individuals with cancer, […]
Röhrig UF, Majjigapu SR, Chambon M, Bron S, Pilotte L, Colau D, Van Den Eynde BJ, Turcatti G, Vogel P, Zoete V, Michielin O
European Journal of Medicinal Chemistry - vol. 84 284-301 (2014)
Indoleamine 2,3-dioxygenase 1 (IDO1) is a key regulator of immune responses and therefore an important therapeutic target for the treatment of diseases that involve pathological immune escape, such as cancer. Here, we describe a robust and sensitive high-throughput screen (HTS) for IDO1 inhibitors using the Prestwick Chemical Library of 1200 FDA-approved drugs and the Maybridge […]
Normand A, Rivi??re E, Renodon-Corni??re A
Biochemical Pharmacology - vol. 91 293-300 (2014)
Homologous Recombination (HR) plays an essential role in cellular proliferation and in maintaining genomic stability by repairing DNA double-stranded breaks that appear during replication. Rad51, a key protein of HR in eukaryotes, can have an elevated expression level in tumor cells, which correlates with their resistance to anticancer therapies. Therefore, targeted inhibition of Rad51 through […]
Liu C, Lou W, Zhu Y, Nadiminty N, Schwartz CT, Evans CP, Gao AC
Clinical Cancer Research - vol. 20 3198-3210 (2014)
PURPOSE: Enzalutamide, a second-generation antiandrogen, was recently approved for the treatment of castration-resistant prostate cancer (CRPC) in patients who no longer respond to docetaxel. Despite these advances that provide temporary respite, resistance to enzalutamide occurs frequently. Androgen receptor (AR) splice variants such as AR-V7 have recently been shown to drive castration-resistant growth and resistance to […]
Mech LD
Chemistry & Biology - vol. 11 907-913 (2014)
Alarge collection of bioactivecompoundswith diverse biological effects can be used as probes to elucidate new biological mechanisms that influence a particular cellular process. Here we analyze the effects of 880 well-known small-molecule bioactives or drugs on the insulin-induced adipogenesis of 3T3-L1 fibroblasts, a cell-culturemodelof fat cell differentiation. Our screen identified 86 compounds as modulators of […]
Baell J, Walters MA
Nature - vol. 513 481-483 (2014)
Naivety about promiscuous, assay-duping molecules is polluting the literature and wasting resources, warn Jonathan Baell and Michael A. Walters
Wang J, Cheng H, Ratia K, Varhegyi E, Hendrickson WG, Li J, Rong L
Journal of Biomolecular Screening - vol. 19 100-107 (2014)
