Medical Biochemistry Commons^™

Farnesyl Pyrophosphate Analogs, Hans Peter Spielmann, Douglas A. Andres, Kareem A.H. Chehade

Molecular and Cellular Biochemistry Faculty Patents

The post-translational addition of a farnesyl moiety to the Ras oncoprotein is essential for its membrane localization and is required for both its biological activity and ability to induce malignant transformation. The present invention describes design and synthesis of a farnesylpyrophosphate (FPP) analog, 8-anilinogeranyl pyrophosphate (AGPP) that is transferred to Ras by farnesyltransferase (FTase), in which the ω-terminal isoprene unit of the farnesyl group has been replaced with an aniline functionality. AGPP potently inhibited FTase activity in vitro (IC₅₀=0.6 μM) and is highly selective showing little inhibitory activity against either geranylgeranyl-protein transferase type I (GGTase I) (IC_{50 …}

Tetrafluoroazidoaniline And Method Of Making And Using The Same, Hans Peter Spielmann, Kareem A.H. Chehade

Molecular and Cellular Biochemistry Faculty Patents

The invention is directed to a novel compounds comprising 4-azidotetrafluoroaniline and the alkyl, acyl and sulfonamide derivatives thereof and to methods of making and using the same. The novel compounds are useful as a photoaffinity probe to study protein structure and function. Two methods for preparing 4-azidotetrafluoroaniline are disclosed, each employing a stable carbamate intermediate from which the 4-azidotetrafluoroaniline is derived.

Fungal Ipc Synthase Assay, Jeffery Radding, Robert C. Dickson, Robert L. Lester

Molecular and Cellular Biochemistry Faculty Patents

The presently-disclosed IPC synthase-inhibitor assays comprise the steps of: (1) expression of the IPC1 gene in a cell; (2) introducing labeled starting substrates for ceramide conversion as well as potential inhibitor(s) of such conversion to the expressed gene product in an environment which allows time and conditions for conversion, and (3) identifying those potential inhibitors which actually inhibit conversion. The present invention also provides methods to determine the ability of a test compound to inhibit fungal growth, comprising the steps of (1) presenting active inositolphosophotidylceramide synthase in a manner such that synthesis of inositolphosphotidylceramide can occur; (2) introducing ceramide and …

Technique For Specifying The Fatty Acid At The Sn2 Position Of Acylglycerol Lipids, Robert C. Dickson, Robert L. Lester, M. Marek Nagiec

Molecular and Cellular Biochemistry Faculty Patents

A method for specifying a fatty acid at the sn2 position of acylglycerol lipids including (a) transfecting a vector including the SLC1 gene or a variant thereof into embryonic biological material, and (b) allowing the SLC1 gene to specify the type of fatty acid at the sn2 position of acylglycerol lipids. Also provided for is an isolated SLC1 gene and a probe for its detection.

Hybrid Vector And Method Resulting In Protein Overproduction By Eukaryotic Cells, Robert E. Rhoads, Arrico De Benedetti

Molecular and Cellular Biochemistry Faculty Patents

A hybrid vector carrying a first and second DNA segments operationally linked thereto, the first DNA segment encoding a protein capable of cross-linking to the cap structure of mRNA and mediating ribosome-binding, and the second DNA segment encoding a polypeptide or protein, the vector being capable of replication, transcription and translation to express the factor and the polypeptide or protein upon transformation of a eukaryotic host, and the polypeptide or protein being expressed at a level higher than the level of expression thereof in the absence of the first DNA segment. A eukaryotic host is transformed with this hybrid vector. …

Method For Obtaining Antifungal And Herbicidal Compounds That Target The First Committed Step In Shingolipid Long-Chain Base Biosynthesis, Robert C. Dickson, Robert L. Lester

Molecular and Cellular Biochemistry Faculty Patents

The invention provides the LCB1 and LCB2 genes of the yeast Saccharomyces cerevisiae that encode subunits of the enzyme serine palmitoyltransferase (SPT), the first enzyme leading to synthesis of the long-base component of the sphingolipids. The present specification describes the isolation of the LCB1 and LCB2 genes. The invention further relates to methods of using these genes to either inhibit SPT activity or to inhibit synthesis of the enzyme. Furthermore, the invention relates to methods for constructing strains of S. cerevisiae or other organisms that can be used to select and to test for compounds that either inhibit SPT activity …

Lac+ Saccharomyces Cerevisiae, Robert C. Dickson, Kotikanyadanam K. Sreekrishna

Molecular and Cellular Biochemistry Faculty Patents

The invention relates to novel, transformed strains of Lac⁺ Saccharomyces cerevisiae, capable of utilizing lactose as a sole carbon source, produced by inserting into the Saccharomyces cerevisiae a plasmid containing a lactose permease and a beta-galactosidase gene derived from Kluyveromyces lactis yeast.

Inhibitors Of Bacterial Collagenase, Richard E. Galardy, Damian Grobelny

Molecular and Cellular Biochemistry Faculty Patents

This invention relates to amino acid derivatives that are useful as inhibitors of bacterial collagenase. . .

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