Cederlund A, Nylén F, Miraglia E, Bergman P, Gudmundsson GH, Agerberth B
Journal of Innate Immunity 365-376 (2013)
Ding Z, German P, Bai S, Feng Z, Gao M, Si W, Sobieski MM, Stephan CC, Mills GB, Jonasch E
Journal of biomolecular screening - vol. 17 572-580 (2012)
Von Hippel-Lindau (VHL) disease is an autosomal dominant disorder that affects multiple organs. Treatment is mainly surgical, and effective systemic therapies are needed. We developed a cell-based screening tool to identify compounds that stabilize or upregulate full-length, point-mutated VHL protein. The 786-0 cell line was infected with full-length W117A-mutated VHL linked to a C-terminal Venus […]
Villalta-Romero F, Gortat A, Herrera AE, Arguedas R, Quesada J, De Melo RL, Calvete JJ, Montero M, Murillo R, Rucavado A, Gutiérrez JM, Pérez-Payá E
ACS Medicinal Chemistry Letters - vol. 3 540-543 (2012)
The majority of snakebite envenomations in Central America are caused by the viperid species Bothrops asper, whose venom contains a high proportion of zinc-dependent metalloproteinases that play a relevant role in the pathogenesis of hemorrhage characteristic of these envenomations. Broad metalloproteinase inhibitors, such as the peptidomimetic hydroxamate Batimastat, have been shown to inhibit snake venom […]
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 […]
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 […]
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 […]
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 […]
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 […]
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 […]
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 […]
