Publications

Journal of biomolecular screening

 Ahmad S, Hughes MA, Johnson GL, Scott JE
 Journal of biomolecular screening - vol. 18 388-399 (2013)

The kinase MEKK2 (MAP3K2) has recently been implicated in tumor growth and metastasis. Thus, selective inhibition of MEKK2 may be a novel strategy for cancer therapy. To identify inhibitors of MEKK2 kinase activity, we have developed a novel activity assay for MEKK2 based on the discovery that recombinant purified MEKK2 has intrinsic ATPase activity. This […]

Analytical Chemistry

 Choulier L, Nominé Y, Zeder-Lutz G, Charbonnier S, Didier B, Jung ML, Altschuh D
 Analytical Chemistry - vol. 85 8787-8795 (2013)

We have developed a surface plasmon resonance (SPR)-based inhibition in solution assay (ISA) to search for inhibitors of the medium affinity (KD = 0.8 μM) interaction between an E6-derived peptide (E6peptide) immobilized on the sensor and a PDZ domain (MAGI-1 PDZ1) in the mobile phase. DZ domains are widespread protein-protein interaction modules that recognize the […]

Tuberculosis

 Goldman RC
 Tuberculosis - vol. 93 569-588 (2013)

High through put screening (HTS) was extensively used in attempts to discover new TB drugs from libraries of pure small molecule compounds many of which complied with the rule of five. Coupled with new methods for determining the target of lead compounds by resistance selection followed by genome sequencing, screening for growth inhibitors led to […]

The open microbiology journal

 Kourtesi C, Ball AR, Huang Y, Jachak SM, Vera DMA, Khondkar P, Gibbons S, Hamblin MR, Tegos GP
 The open microbiology journal - vol. 7 34-52 (2013)

Conventional antimicrobials are increasingly ineffective due to the emergence of multidrug-resistance among pathogenic microorganisms. The need to overcome these deficiencies has triggered exploration for novel and unconventional approaches to controlling microbial infections. Multidrug efflux systems (MES) have been a profound obstacle in the successful deployment of antimicrobials. The discovery of small molecule efflux system blockers […]

PLoS ONE

 Jiang X, Sun L, Qiu JJ, Sun X, Li S, Wang X, So CWE, Dong S
 PLoS ONE - vol. 8 1-9 (2013)

Acute myeloid leukemia (AML) is the most common malignant myeloid disorder of progenitor cells in myeloid hematopoiesis and exemplifies a genetically heterogeneous disease. The patients with AML also show a heterogeneous response to therapy. Although all-trans retinoic acid (ATRA) has been successfully introduced to treat acute promyelocytic leukemia (APL), it is rather ineffective in non-APL […]

Drug Discovery Today

 Blatt J, Corey SJ
 Drug Discovery Today - vol. 18 4-10 (2013)

Drug ‘repurposing’, that is, using old drugs for new indications, has been proposed as a more efficient strategy for drug development than the current standard of beginning with novel agents. In this review, we explore the scope of drug repurposing in pediatric hematology oncology and in pediatrics in general. Drugs commonly used in children were […]

Journal of biomolecular screening

 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 […]

ACS Medicinal Chemistry Letters

 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 […]

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