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Molecular mechanisms linking geranylgeranyl diphosphate synthase to cell survival and proliferation
TLDR
Recent advances in geranylgeranyl diphosphate synthase expression and inhibitor development are described with a particular focus on the molecular mechanisms that link geranyl Geranylation to cell proliferation via geranylgersanylated small GTPases. Expand
Geranylgeranyl diphosphate synthase inhibition induces apoptosis that is dependent upon GGPP depletion, ERK phosphorylation and caspase activation
TLDR
DGBP is a more potent and selective compound than zoledronate in inducing apoptosis mediated through pathways that include caspases and MEK/ERK and support the further development of GGDPS inhibitors as anticancer therapeutics. Expand
Phosphinophosphonates and Their Tris-pivaloyloxymethyl Prodrugs Reveal a Negatively Cooperative Butyrophilin Activation Mechanism.
TLDR
Together, tris-POM prodrugs enhance the cellular activity of phosphinophosphonates, reveal structure-activity relationships of butyrophilin ligands, and support a negatively cooperative model of cellular butyphilin activation. Expand
Probing the Ligand-Binding Pocket of BTN3A1.
TLDR
The results further define the structure-activity relationships underlying BTN3A1 ligand binding and antigenicity and support further structure-guided drug design. Expand
Toward Broad Spectrum DHFR inhibitors Targeting Trimethoprim Resistant Enzymes Identified in Clinical Isolates of Methicillin-Resistant Staphylococcus aureus.
TLDR
A series of INCA compounds that exhibit low nanomolar enzymatic activity and potent cellular activity with human selectivity against a panel of clinically relevant TMPR MRSA isolates are reported. Expand
Regulation of the Notch-ATM-abl axis by geranylgeranyl diphosphate synthase inhibition
TLDR
The results provide a model by which T-ALL cells use Notch1 to avoid DNA-damage-induced apoptosis, and can be overcome by inhibition of GGDPS through effects on notch1 expression and its subsequent response. Expand
[Mammary hamartoma with atypical stromal cells: a potential diagnostic dilemma].
TLDR
It is reported that a case of breast hamartoma containing numerous atypical mono- or multinucleated stromal cells within the fibro-fatty component raised differential diagnostic problems with pleomorphic lipoma, well-differentiated liposarcoma and malignant phylloid tumour with a lipomatous heterologous component. Expand
Toward Broad Spectrum DHFR inhibitors Targeting Trimethoprim Resistant Enzymes Identified in Clinical Isolates of Methicillin-Resistant Staphylococcus aureus
TLDR
A series of INCA compounds that exhibit low nanomolar enzymatic activity and potent cellular activity with human selectivity against a panel of clinically relevant TMPR MRSA isolates are reported. Expand