Sidechain Functionalized S-Acylbenzamides With Anti-HIV Activity

HIV infection remains a major medical problem, with approximately 38 million people worldwide living with HIV. Nipamovir and SAMT-247 are simple and inexpensive small molecules that inactivate HIV virus by interference with final maturation steps of the virus. This mechanism provides a high barrier for HIV to develop resistance. In fact, lab experiments designed to encourage HIV to develop resistance to Nipamovir and SAMT-247 have all failed. In animal tests, Nipamovir and SAMT-247 do not display toxic side effects.

Truncated Methanocarba Adenosine Derivatives as A3 Adenosine Receptor Antagonists

Novel A3 adenosine antagonists available for licensing. A3 receptors are particularly highly expressed in inflammatory cells, making it a potentially desirable target for inflammatory diseases. This technology relates to highly specific antagonists and partial agonists of A3 adenosine receptors, which are negatively coupled to adenylate cyclase and have been broadly implicated in inflammation, cardiovascular disease, endocrine conditions and cancer. Further, A3 adenosine receptors have been implicated in asthma and glaucoma.

New Cholera Vaccine and Method for Conjugating Bacterial Polysaccharides to Proteins

A new conjugate vaccine for cholera has been developed. The invention includes a new method to conjugate the O-specific polysaccharide-core part of the bacterial lipopolysaccharide and protein subcomponents. Conventional technology has entailed chemical treatment of both components to introduce linkers, which made them amenable for covalent linking. The new method simplifies production by utilizing squaric acid chemistry for conjugating the free amine-containing species (e.g. polysaccharides) directly to amine-containing species (e.g.

SMAD3 Reporter Mouse for Assessing TGF-ß/Activin Pathway Activation

The Transforming Growth Factor Beta (TGF-ß) ligands (i.e., TGF-ß1, -ß2, -ß3) are key regulatory proteins in animal physiology. Disruption of normal TGF-ß signaling is associated with many diseases from cancer to fibrosis. In mice and humans, TGF-ß activates TGF-ß receptors (e.g., TGFBR1), which activates SMAD proteins that alter gene expression and contribute to tumorigenesis.  Reliable animal models are essential for the study of TGF-ß signaling.

New Heterocyclic Scaffold-Based Inhibitors of the Polo-Box Domain of Polo-like Kinase 1 for the Treatment of Cancer

Polo-like kinase 1 (Plk1), a member of the Polo-like kinase family, plays a critical role in regulating mitosis and cell cycle progression. Aberrant expression of Plk1 has been observed in a variety of human cancers, and it is known to be associated with tumorigenesis as well as poor prognosis in cancer patients. Unlike normal cells, some cancer cells are dependent on augmented Plk1 levels to remain viable and are killed when Plk1 function is attenuated.

A Specialized Tissue Collection Device for the Preservation and Transportation of Needle Biopsies

The ability to hold and transport tissue, especially needle biopsies in a pre-defined and controlled environment is critical for the preservation of biopsy samples in downstream analytic applications. Currently, tissue specimens are placed in open containers with variable, poorly controlled solutions applied to them, often in less than sterile conditions.  Evaluation of the tissue by examination through a stereoscope or similar approaches to determine adequacy is limited and requires manipulation of the tissue that can further damage the tissue.

Novel Fixative for Improved Biomolecule Quality from Paraffin-Embedded Tissue

Tissues samples collected during medical procedures, such as biopsies, are used to diagnose a wide variety of diseases. Before diagnosis, patient samples are typically processed by fixation and paraffin embedding. This fixation/embedding process is used to preserve tissue morphology and histology for subsequent evaluation. Unfortunately, most fixative agents can damage or destroy nucleic acids (RNA and DNA) and damage proteins during the fixation process, thereby potentially impairing diagnostic assessment of tissue.

Rescue of AAV Production by shRNA Co-transfection

Recombinant adeno-associated virus (rAAV) vectors are proving to be a valid, safe and efficient gene transfer system for clinical applications. As most vectors utilize constitutive promoters, this results in transgene expression in the producer cell. Some of these transgene products can induce proapoptotic, cytostatic or other unknown effects that interfere with producer cell function. Therefore, this reduces the viral vector yield and is a major limitation when trying to characterize poorly described genes.

Prostatic Adenocarcinoma Cells Expressing or Lacking the Tumor Suppressor Gene PTEN

PTEN is a tumor suppressor gene that is frequently deleted or mutated in a variety of human cancers, including prostate, breast, endometrial, lung, and ovarian cancers. In prostate cancer cells, PTEN deletion is the most common event observed. The loss of PTEN is thought to play and important role in tumor cell proliferation and metastasis due to a lack of control of the signaling pathways that mediate cellular processes such as apoptosis and migration.
Subscribe to NIDDK