Publications

Jak-Stat

 Walker SR, Frank DA
 Jak-Stat - vol. 1 292-299 (2012)

STAT transcription factors are regulators of critical cellular processes such as proliferation, survival, and self-renewal. While the activity of these proteins is tightly regulated under physiological conditions, they can become constitutively activated in a broad range of human cancers. This inappropriate STAT activation leads to enhanced transcription of genes that can directly lead to the […]

Analytical Biochemistry

 Zeder-Lutz G, Choulier L, Besse M, Cousido-Siah A, Figueras FXR, Didier B, Jung ML, Podjarny A, Altschuh D
 Analytical Biochemistry - vol. 421 417-427 (2012)

We investigated the suitability of surface plasmon resonance (SPR) for providing quantitative binding information from direct screening of a chemical library on protein tyrosine phosphatase 1b (PTP1B). The experimental design was established from simulations to detect binding with K D < 10 -4 M. The 1120 compounds (cpds) were injected sequentially at concentrations [C(cpd)] of […]

Chemistry and Biology

 Wang Y, Davidow L, Arvanites AC, Blanchard J, Lam K, Xu K, Oza V, Yoo JW, Ng JMY, Curran T, Rubin LL, McMahon AP
 Chemistry and Biology - vol. 19 972-982 (2012)

The Hedgehog signaling pathway is linked to a variety of diseases, notably a range of cancers. The first generation of drug screens identified Smoothened (Smo), a membrane protein essential for signaling, as an attractive drug target. Smo localizes to the primary cilium upon pathway activation, and this transition is critical for the response to Hedgehog […]

Tuberculosis

 Reynolds RC, Ananthan S, Faaleolea E, Hobrath JV, Kwong CD, Maddox C, Rasmussen L, Sosa MI, Thammasuvimol E, White EL, Zhang W, Secrist JA
 Tuberculosis - vol. 92 72-83 (2012)

Kinase targets are being pursued in a variety of diseases beyond cancer, including immune and metabolic as well as viral, parasitic, fungal and bacterial. In particular, there is a relatively recent interest in kinase and ATP-binding targets in Mycobacterium tuberculosis in order to identify inhibitors and potential drugs for essential proteins that are not targeted […]

PLoS ONE

 Polireddy K, Khan MMT, Chavan H, Young S, Ma X, Waller A, Garcia M, Perez D, Chavez S, Strouse JJ, Haynes MK, Bologa CG, Oprea TI, Tegos GP, Sklar LA, Krishnamurthy P
 PLoS ONE - vol. 7 1-14 (2012)

ABCB6 is a member of the adenosine triphosphate (ATP)-binding cassette family of transporter proteins that is increasingly recognized as a relevant physiological and therapeutic target. Evaluation of modulators of ABCB6 activity would pave the way toward a more complete understanding of the significance of this transport process in tumor cell growth, proliferation and therapy-related drug […]

Blood cancer journal

 Li Y, Zhao X, Vecchiarelli-Federico LM, Li Y, Datti A, Cheng Y, Ben-David Y
 Blood cancer journal - vol. 2 1-9 (2012)

The Ets transcription factor, Fli-1 is activated in murine erythroleukemia and overexpressed in various human malignancies including Ewing’s sarcoma, induced by the oncogenic fusion protein EWS/Fli-1. Recent studies by our group and others have demonstrated that Fli-1 plays a key role in tumorigenesis, and disrupting its oncogenic function may serve as a potential treatment option […]

The AAPS Journal

 Oprea TI, Mestres J
 The AAPS Journal - vol. 14 759-763 (2012)

Repurposing drugs requires finding novel therapeutic indications compared to the ones for which they were already approved. This is an increasingly utilized strategy for finding novel medicines, one that capitalizes on previous investments while derisking clinical activities. This approach is of interest primarily because we continue to face significant gaps in the drug-target interactions matrix […]

Matrix Biology

 Tomasini-Johansson BR, Johnson IA, Hoffmann FM, Mosher DF
 Matrix Biology - vol. 31 360-367 (2012)

Fibronectin (FN) is a plasma glycoprotein that circulates in the near micromolar concentration range and is deposited along with locally produced FN in the extracellular matrices of many tissues. The control of FN deposition is tightly controlled by cells. Agents that modulate FN assembly may be useful therapeutically in conditions characterized by excessive FN deposition, […]

Neuroscience Letters

 Shin JH, Park SJ, Jo YK, Kim ES, Kang H, Park JH, Lee EH, Cho DH
 Neuroscience Letters - vol. 515 162-167 (2012)

Mefloquine is an effective treatment drug for malaria. However, it can cause several adverse side effects, and the precise mechanism associated with the adverse neurological effects of Mefloquine is not clearly understood. In this study, we investigated the effect of Mefloquine on autophagy in neuroblastoma cells. Mefloquine treatment highly induced the formation of autophagosomes and […]

Cell

 Sachlos E, Risueño RM, Laronde S, Shapovalova Z, Lee JH, Russell J, Malig M, McNicol JD, Fiebig-Comyn A, Graham M, Levadoux-Martin M, Lee JB, Giacomelli AO, Hassell JA, Fischer-Russell D, Trus MR, Foley R, Leber B, Xenocostas A, Brown ED, Collins TJ, Bhatia M
 Cell - vol. 149 1284-1297 (2012)

Selective targeting of cancer stem cells (CSCs) offers promise for a new generation of therapeutics. However, assays for both human CSCs and normal stem cells that are amenable to robust biological screens are limited. Using a discovery platform that reveals differences between neoplastic and normal human pluripotent stem cells (hPSC), we identify small molecules from […]

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