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Reviving Ras Joanne Kotz doi:10.1038/scibx.2012.536 Genentech and Vanderbilt teams have independently used fragment-based drug discovery to identify a new small molecule binding site that blocks activation of Ras, a highly prevalent oncoprotein that has previously been considered undruggable. The results could reinvigorate drug discovery efforts against the target. Full Text | PDF
Cooling down AD Lev Osherovich doi:10.1038/scibx.2012.537 A Johns Hopkins University team has clinical proof-of-concept data for slowing the progression of Alzheimer's disease by reducing activity in the hippocampus with antiepileptic drugs. AgeneBio has licensed the IP and is planning a Phase II trial of an antiepileptic to prevent AD. Full Text | PDF
Getting around peripartum cardiomyopathy Michael J. Haas doi:10.1038/scibx.2012.538 A Harvard Medical School–led team has shown that a soluble form of FLT1 causes about one-third of peripartum cardiomyopathy cases—those associated with pre-eclampsia. Ongoing studies are seeking to identify small molecule inhibitors of the protein and determine whether the mechanism also underlies the other two-thirds of cases. Full Text | PDF
Getting selective for γ Tim Fulmer doi:10.1038/scibx.2012.539 Cellzome and Exelixis have independently designed the first highly selective inhibitors of the γ-isoform of PI3K. Exelixis hopes to out-license its inhibitors, whereas the recent acquisition of Cellzome by GlaxoSmithKline gives the pharma a new class of compounds for inflammatory and autoimmune diseases. Full Text | PDF
BRAF; cyclin dependent kinase inhibitor 2A (CDKN2A; INK4a; ARF; p16INK4a); cyclin dependent kinase 4 (CDK4); CDK6 doi:10.1038/scibx.2012.540 Mouse studies suggest a BRAF inhibitor plus a CDK4 and CDK6 inhibitor could help treat pediatric astrocytomas that carry the BRAF V600E mutation and have a CDKN2A deficiency. Full Text | PDF
DNA doi:10.1038/scibx.2012.541 Mouse and cell culture studies identified mithramycin analogs that could help treat cancer. Full Text | PDF
K-Ras; son of sevenless homolog 1 (SOS1) doi:10.1038/scibx.2012.542 Two independent in vitro studies identified a previously unknown binding site on K-Ras that could be targeted with small molecules to treat cancer. Full Text | PDF
P glycoprotein (MDR1; ABCB1; P-gp; CD243) doi:10.1038/scibx.2012.543 Cell culture studies identified ecdysteroid compounds that could help treat multidrug-resistant (MDR) cancers. Full Text | PDF
p21 Protein (Cdc42 Rac)-activated kinase 4 (PAK4) doi:10.1038/scibx.2012.544 In vitro and rodent studies identified a pyrroloaminopyrazole series of PAK4 inhibitors that could help treat cancers. Full Text | PDF
Sirtuin 7 (SIRT7) doi:10.1038/scibx.2012.545 In vitro and mouse studies suggest inhibiting SIRT7 could help treat cancer. Full Text | PDF
Topoisomerase I (TOP1); tyrosyl-DNA phosphodiesterase 1 (TDP1) doi:10.1038/scibx.2012.546 In vitro studies identified a bis(indenoisoquinoline)-based inhibitor of TOP1 and TDP1 that could help treat cancer. Full Text | PDF
Phosphatidylinositol-3,4,5-triphosphate-dependent Rac exchange factor 2 (PREX2) doi:10.1038/scibx.2012.547 Genomic and mouse studies identified PREX2 mutants in melanomas that could be inhibited to help treat the cancer. Full Text | PDF
Tyrosine kinase non-receptor 2 (Tnk2; ACK1) doi:10.1038/scibx.2012.548 Mouse and cell culture studies suggest inhibiting ACK1 could help reverse resistance to radiotherapy in castration-resistant prostate cancer (CRPC). Full Text | PDF
Survivin (BIRC5) doi:10.1038/scibx.2012.549 Mouse studies suggest survivin inhibitors could help treat Merkel cell carcinoma, a form of skin cancer caused by the Merkel cell polyomavirus. Full Text | PDF
NAD(P)H dehydrogenase quinine 1 (NQO1; QR1) doi:10.1038/scibx.2012.550 In vitro and mouse studies identified deoxynyboquinone (DNQ) as a new NQO1 substrate that could help treat solid tumors. Full Text | PDF
Protein disulfide isomerase (PDI) doi:10.1038/scibx.2012.551 In vitro and mouse studies identified a PDI inhibitor that could help prevent thrombosis. Full Text | PDF
Aldehyde dehydrogenase 1 family member A1 (ALDH1A1) doi:10.1038/scibx.2012.552 Mice and human tissue studies suggest antagonizing ALDH1A1 could help treat obesity and type 2 diabetes. Full Text | PDF
Family with sequence similarity 20 member C (FAM20C) doi:10.1038/scibx.2012.553 In vitro studies identified FAM20C as a protein kinase that phosphorylates extracellular proteins and that could be targeted to treat Raine syndrome, a rare congenital disorder characterized by lethal bone dysplasias. Full Text | PDF
β-Amyloid 42 (Aβ42) doi:10.1038/scibx.2012.554 In vitro and mouse studies suggest inhibiting a pyroglutamylated form of Aβ42 could help treat AD. Full Text | PDF
Not applicable doi:10.1038/scibx.2012.555 A clinical study suggests epilepsy drugs could be useful for treating or preventing AD. Full Text | PDF
Metabotropic glutamate receptor subtype 5 (mGluR5; GRM5) doi:10.1038/scibx.2012.556 Studies in mice suggest antagonizing mGluR5 could help treat autism. Full Text | PDF
Methylglyoxal; NaV1.8 (PN3; SCN10A) doi:10.1038/scibx.2012.557 Human and mouse studies suggest inhibiting the metabolite methylglyoxal could help treat hyperalgesia in diabetic neuropathy. Full Text | PDF
UbiA prenyltransferase domain containing 1 (UBIAD1) doi:10.1038/scibx.2012.558 Drosophila studies suggest improving vitamin K2 production could help treat diseases involving mitochondrial dysfunction, including PD. Full Text | PDF
Transglutaminase 1 (TGM1; TG1); TGM2 (TG2) doi:10.1038/scibx.2012.559 Studies in mice and in cultured neurons suggest inhibiting TGM1 and TGM2 could be neuroprotective after stroke. Full Text | PDF
High throughput screening of T cell receptor (TCR) to detect minimal residual disease (MRD) in T cell acute lymphoblastic leukemia (T-ALL) doi:10.1038/scibx.2012.560 High throughput screening of lymphoid receptor genes could help guide diagnosis and prognosis in T-ALL. Full Text | PDF
Proteomic method for developing rational combinations of kinase inhibitors doi:10.1038/scibx.2012.561 A proteomic method could aid the development of rational combinations of kinase inhibitors to treat cancer. Full Text | PDF
Synthesis of biologically active meroterpenoids doi:10.1038/scibx.2012.562 A method of synthesizing meroterpenoids could generate new compounds to treat cancer and infectious diseases. Full Text | PDF
Protocol for augmenting β cell regeneration and reversing late-stage type 1 diabetes doi:10.1038/scibx.2012.563 A protocol using an antibody and a cell transplant conditioning regimen plus delivery of gastrin and epidermal growth factor (EGF) could help treat late-stage type 1 diabetes. Full Text | PDF
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