Abstract: Disclosed are thyclotides, which are oligomers, each comprising (a) from about 8 to about 25 monomer units of formula (I) and (b) from 0 to about 24 monomer units of formula (II): wherein B is a nucleobase, which can be the same or different at each occurrence, or a pharmaceutically acceptable salt thereof. The thyclotides are soluble in water, bind strongly to complementary DNA and RNA, and are cell permeable. The thyclotides are useful as reagents for antisense and antigene applications, and as probes in molecular diagnostics and microarrays.

Abstract: Disclosed is a compound of formula (I): for treating or preventing a human immunodeficiency virus (HIV) infection in a mammal, for inhibiting or preventing maturation of an immature human immunodeficiency virus (HIV) to a mature HIV, and for preventing or inhibiting a human immunodeficiency virus (HIV) infection in a mammal having at least one HIV viral particle on a surface thereof.

Abstract: The invention concerns methods for detecting a nucleic acid of interest in a solution comprising (a) contacting a solution suspected of containing the nucleic acid of interest with a PNA capture probe and a PNA reporter probe; wherein (i) the PNA capture probe comprises at least two trans-cyclopentanes; (ii) the PNA reporter probe comprises at least six biotin groups; (iii) the PNA capture probe bound to a surface; and (iv) the PNA capture probe and the PNA reporter probe each comprise a nucleobase sequence that is complementary to different non-overlapping portions of the nucleic acid of interest; (b) detecting the presence of the PNA capture probe and the PNA reporter probe bound to the surface; wherein the nucleic acid of interest is detected when 1-1000 molecules of the nucleic acid of interest are present in the solution being tested.

Abstract: Described herein are compositions composed of peptide nucleic acid strands. In some aspects the peptide nucleic acid strands are complementary to at least a portion of another peptide nucleic acid strand that may have one or more gamma substituents, where the ratio of PNA strands is least 1:1. Certain gamma substituents are capable of effecting attachment of a PNA strand to a cell. The disclosure also concerns construction of nanostructure platforms and vaccines and use of the inventive compositions in inhibiting disease states in mammals.

Abstract: Disclosed is a method for lowering the detection limit in a method of detecting a nucleic acid comprising (i) contacting a solution comprising a first PNA with a substrate having a second PNA affixed thereto, the second PNA comprising at least one trans-cyclopentane residue, wherein the first PNA has two linker-attached biotins attached thereto and the first and second PNAs being complementary to different portions of a target DNA; (ii) contacting a sample suspected of containing the nucleic acid with the first and second PNAs; and (iii) determining the presence of the reporter molecule on the substrate. Also disclosed are a detection assay and a kit for detecting a target nucleic acid.

Abstract: The invention concerns methods for detecting a nucleic acid of interest in a solution comprising (a) contacting a solution suspected of containing the nucleic acid of interest with a PNA capture probe and a PNA reporter probe; wherein (i) the PNA capture probe comprises at least two trans-cyclopentanes; (ii) the PNA reporter probe comprises at least six biotin groups; (iii) the PNA capture probe bound to a surface; and (iv) the PNA capture probe and the PNA reporter probe each comprise a nucleobase sequence that is complementary to different non-overlapping portions of the nucleic acid of interest; (b) detecting the presence of the PNA capture probe and the PNA reporter probe bound to the surface; wherein the nucleic acid of interest is detected when 1-1000 molecules of the nucleic acid of interest are present in the solution being tested.

Abstract: Disclosed are ?-amino acid monomers containing cylcoalkyl, cycloalkenyl, and heterocylic substituents which encompass the ? and ? carbons of the peptide backbone and ?-polypeptides made from such monomers. Method of generating combinatorial libraries of polypeptides containing the ?-peptide residues and libraries formed thereby are disclosed.

Abstract: The invention concerns compositions comprising strands of polynucleotide and strands of PNA, each PNA strand comprising: (i) from 2 to 50 nucleobase subunits and (ii) one or more gamma substituents. The PNA strands are complementary to at least a portion of at least some of the polynucleotide strands, and the molar ratio of PNA strands to polynucleotide strands being at least 1:1. Certain gamma substituents are capable of effecting attachment of a PNA strand to a cell. The invention also concerns construction of nanostructure platforms and vaccines and use of the inventive compositions in inhibiting disease states in mammals.

Abstract: Disclosed are ?-amino acid monomers containing cylcoalkyl, cycloalkenyl, and heterocylic substituents which encompass the ? and ? carbons of the peptide backbone and ?-polypeptides made from such monomers. Method of generating combinatorial libraries of polypeptides containing the ?-peptide residues and libraries formed thereby are disclosed.

Abstract: The present invention concerns methods for detecting a nucleic acid comprising (i) contacting a solution comprising a first PNA having a first cross-reactive functional group with a substrate having a second PNA affixed thereto, the second PNA having a second first cross-reactive functional group, wherein the first PNA has a reporter molecule attached thereto and the first and second PNAs being complementary to different portions of a target DNA; (ii) contacting a sample suspected of containing the nucleic acid with the first and second PNAs; and (iii) determining the presence of the reporter molecule on the substrate.

Abstract: The present invention concerns methods for detecting a nucleic acid comprising (i) contacting a solution comprising a first PNA having a first cross-reactive functional group with a substrate having a second PNA affixed thereto, the second PNA having a second first cross-reactive functional group, wherein the first PNA has a reporter molecule attached thereto and the first and second PNAs being complementary to different portions of a target DNA; (ii) contacting a sample suspected of containing the nucleic acid with the first and second PNAs; and (iii) determining the presence of the reporter molecule on the substrate.

Abstract: Ketoamine compounds and related methods for reactivation of tumor suppressor protein p53.

Abstract: The present invention concerns methods of synthesis of trans-tert-butyl-2-aminocylcopentylcarbamate comprising contacting 6-tosyl-6-azabicyclo[3.1.0]hexane with TMSN3 and TBAF to produce 2-azido-N-tosylcyclopentananiine; reducing the 2-azido-N-tosylcyclopentanamine to produce 2-amino-N-tosylcyclopentanamine; contacting the 2-amino-N-tosylcyclopentanamine with di-tert/-butyl dicarbonate to produce tert-butyl-2-(tosylamino)cyclopentylcarbamate; and detosylation of tert-butyl O(tosylamino) cyclopentylcarbamate to produce trans-tert-butyl-2-aminocyclopentylcarbamate. The invention also concerns PNAs comprising residues of the monomers of the invention in the backbone and uses of such PNAs. The PNAs of the invention can be used to detect DNAs of infectious agents or to suppress expression of protein associated with cancer.

Abstract: Ketoamine compounds and related methods for reactivation of tumor suppressor protein p53.

Abstract: Ketoamine compounds and related methods for reactivation of tumor suppressor protein p53.

Abstract: One aspect of the present invention relates to methods for the transition-metal-catalyzed asymmetric 1,4-addition of a nucleophile, e.g., hydride, to cyclic and acyclic enoates and enones. In certain embodiments of the methods of the present invention, the transition metal catalyst consists essentially of copper and an asymmetric bidentate bisphosphine ligand.

Abstract: Disclosed are &bgr;-peptides containing cylcoalkyl, cycloalkenyl, and heterocylic substituents which encompass the &agr; and &bgr; carbons of the peptide backbone. The &bgr;-peptides adopt stable helical and sheet structures in both the solid state and in solution. Method of generating combinatorial libraries of peptides containing &bgr;-peptide residues and the libraries formed thereby are disclosed.

Abstract: One aspect of the present invention relates to methods for the transition-metal-catalyzed asymmetric 1,4-addition of a nucleophile, e.g., hydride, to cyclic and acyclic enoates and enones. In certain embodiments of the methods of the present invention, the transition metal catalyst consists essentially of copper and an asymmetric bidentate bisphosphine ligand.

Abstract: One aspect of the present invention relates to methods for the transition-metal-catalyzed asymmetric 1,4-addition of a nucleophile, e.g., hydride, to cyclic and acyclic enoates and enones. In certain embodiments of the methods of the present invention, the transition metal catalyst consists essentially of copper and an asymmetric bidentate bisphosphine ligand.

Abstract: Disclosed are &bgr;-amino acid monomers containing cylcoalkyl, cycloalkenyl, and heterocylic substituents which encompass the &agr; and &bgr; carbons of the peptide backbone and &bgr;-polypeptides made from such monomers. Method of generating combinatorial libraries of polypeptides containing the &bgr;-peptide residues and libraries formed thereby are disclosed.