Adenosine receptor agonists, partial agonists, and antagonists (U.S. Patent Number 13/479,973)
NIDDK announces the availability of a highly selective A1 adenosine receptor (AR) agonist. This receptor is neuroprotective in ischemic and epileptic models. The A1AR-selective full agonist MRS5474 displayed anticonvulsant activity in vivo in a model of minimal clonic seizures, without toxicity characteristic of other A1AR agonists. Nucleoside docking to a homology model based on recently reported agonist-bound AR structures characterized the interaction of cycloalkylrelated constituents with a small hydrophobic subpocket in the A1AR. Recent advances in specificity to the A1AR encourage development of these agonists for CN...
Source: NIDDK Research Resources - August 17, 2018 Category: Endocrinology Source Type: research
A3 Adenosine receptor allosteric modulators (U.S. Patent Number 20090054476 A1)
The present invention relates to allosteric modulation of A3 adenosine receptor (A3AR) and provides for the use of an A3 adenosine receptor modulator (A3RM), for the preparation of pharmaceutical compositions for modulating the A3AR in a subject, as well as pharmaceutical compositions comprising the same and therapeutic methods comprising administering to a subject an amount of an A3RM, the amount being effective to modulate A3AR activity. The A3RM according to the invention are 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives. The invention also provides some of such novel 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives. (So...
Source: NIDDK Research Resources - August 17, 2018 Category: Endocrinology Source Type: research
A3 Adenosine Receptor Antagonists and Partial Agonists (U.S. Patent Application Number 13/056,997)
Disclosed are A3 adenosine receptor antagonists and/or partial agonists of formula (I): wherein R1 to R5 are as described herein, as well as pharmaceutical compositions thereof and methods of use thereof. The antagonists or partial agonists find use in treating a number of diseases including cancer, glaucoma, inflammatory diseases, asthma, stroke, myocardial infarction, allergic reactions, rhinitis, poison ivy induced responses, urticaria, scleroderma, arthritis, brain arteriole diameter constriction, bronchoconstriction, and myocardial ischemia, as well as in preventing cardiac ischemia. Also disclosed are radiolabeled co...
Source: NIDDK Research Resources - August 16, 2018 Category: Endocrinology Source Type: research
M ÍOS: Better Animal Care for Better Research
Millions of rodents are used in HHS research labs each year to both understand mechanisms of disease and develop new therapies. Monitoring the health of these animals is essential not only to ensure their general welfare but also to ensure that research studies produce quality and reproducible data.Currently, trained specialists monitor the health of these animals with daily checks of each cage, a time consuming and expensive process. Additionally, frequent human interaction and environment changes are stress inducing factors for the rodents, potentially introducing variability into experimental designs. To address th...
Source: NIDDK Research Resources - February 27, 2018 Category: Endocrinology Source Type: research
M & #205;OS: Better Animal Care for Better Research
Millions of rodents are used in HHS research labs each year to both understand mechanisms of disease and develop new therapies. Monitoring the health of these animals is essential not only to ensure their general welfare but also to ensure that research studies produce quality and reproducible data.Currently, trained specialists monitor the health of these animals with daily checks of each cage, a time consuming and expensive process. Additionally, frequent human interaction and environment changes are stress inducing factors for the rodents, potentially introducing variability into experimental designs. To address th...
Source: NIDDK Research Resources - September 8, 2017 Category: Endocrinology Source Type: research
M & #205;OS Better Animal Care for Better Research
Millions of rodents are used in HHS research labs each year to both understand mechanisms of disease and develop new therapies. Monitoring the health of these animals is essential not only to ensure their general welfare but also to ensure that research studies produce quality and reproducible data.Currently, trained specialists monitor the health of these animals with daily checks of each cage, a time consuming and expensive process. Additionally, frequent human interaction and environment changes are stress inducing factors for the rodents, potentially introducing variability into experimental designs. To address th...
Source: NIDDK Research Resources - September 5, 2017 Category: Endocrinology Source Type: research
Method for over-expression of rapid purification of biosynthetic proteins (U.S. Patent Number 6,077,694)
The subject invention relates to a method of producing and purifying large quantities of a biosynthetic protein. The gene which codes for the protease is placed between the binding domain of a gene which codes for a binding protein and a gene coding for the target protein of interest. The fused gene construct is inserted in an expression vector which is then introduced into a host cell. (Source: NIDDK Research Resources)
Source: NIDDK Research Resources - June 9, 2017 Category: Endocrinology Source Type: research
Detection of nucleic acid sequence variations using phase Mu transposase (U.S. Patent Number 7,316,903)
The present invention relates, e.g., to a method of detecting a mismatch in a double stranded nucleic acid target, comprising (a) contacting the target with (i) a Mu-end nucleic acid, and (ii) a phage Mu transposase, under conditions effective for the Mu-end nucleic acid to transpose into the target at about the site of a mismatch, if the target comprises a mismatch, and (b) detecting transposition of the Mu-end DNA into the target, wherein transposition of the Mu-end nucleic acid into the target at a predominant site indicates the presence of a mismatch at that site. (Source: NIDDK Research Resources)
Source: NIDDK Research Resources - June 9, 2017 Category: Endocrinology Source Type: research
MEN1, the gene associated with multiple endocrine neoplasia type 1, menin polypeptides and uses thereof (U.S. Patent Number 7,358,347)
The invention relates to the discovery of a novel tumor suppressor gene which is associated with multiple endocrine neoplasia type 1. The gene has been designated MEN1 and the gene product is menin. The absence of this protein and associated mutations in the corresponding gene have been identified in individuals suffering from multiple endocrine neoplasia type 1. The identification of this marker for multiple endocrine neoplasia type 1 has diagnostic uses as well as for gene therapy. (Source: NIDDK Research Resources)
Source: NIDDK Research Resources - June 9, 2017 Category: Endocrinology Source Type: research
HIV protease gene and method for its expression (U.S. Patent Number 5,637,488)
The invention is a synthetic DNA sequence for encoding a specific enzyme or protease. The protease is essential for the completion (replication) of an infective human immunodeficiency virus (HIV). The invented gene is desirable for the expression of the protease by recombinant methodology in prokaryotic and/or eukaryotic cells and the production of a commercially desirable amount of the protease for biochemical and physical characterization, necessary to find effective inhibitor of the protease, and thereby to block the production of infectious human immunodeficiency virus (HIVs). (Source: NIDDK Research Resources)
Source: NIDDK Research Resources - June 9, 2017 Category: Endocrinology Source Type: research
hGC-1, a gene encoding a member of the olfactomedin-related protein family (U.S. Patent Number 7,557,196)
An isolated acid having the sequence of a) SEQ ID NO: 1; b) the sequence of SEQ ID NO: 2; c) the sequence of SEQ ID NO: 3; d) a sequence complementary to any of a), b), or c); or e) a sequence of at least 10 contiguous nucleotides specific for any of a)-d). The invention relates to the identification and characterization of a hitherto unidentified human gene, hGC-1. The protein encoded by hGC-1 appears to be a member of the olfactomedin-related proteins. The invention relates generally to the gene (hGC-1), nucleic acids, cDNA, vectors, polypeptides, protein, antibodies, cells, transgenic animal, and other compositions rela...
Source: NIDDK Research Resources - June 9, 2017 Category: Endocrinology Source Type: research
Dihydropyridine-, pyridine-, Benzopyran-4-one- and Triazoloquinazoline Derivative, Their Preparation, and Their Use as Adenosine Receptor Antagonists (U.S. Patent Number 6,066,642)
The present invention provides a method of identifying CFTR-binding compounds for treating cells having a reduced apical Cl.sup.- conductance, such as cystic fibrosis cells. This identification method involves the use of polypeptide I.alpha., which constitutes a portion of the CFTR protein. The present invention also provides a method of treating CF cells by contacting cells having a reduced apical Cl.sup.- conductance with a therapeutically effective quantity of a compound selected by the present inventive identification method. Preferred compounds for such treatment have little or no affinity for adenosine cell receptors...
Source: NIDDK Research Resources - June 9, 2017 Category: Endocrinology Source Type: research
Detection and treatment of polycystic kidney disease (U.S. Patent Number 7,553,644)
Compositions useful for examining the PKD1 gene are provided. In addition, methods for detecting mutations of the PKD1 gene, which can be associated with autosomal dominant polycystic kidney disease in humans, are provided. Methods for diagnosing a mutant PKD1 gene sequence in a subject also are provided, as are methods of treating a subject having a PKD1-associated disorder. For more information please contactJohns Hopkins University's Technology Ventures office. (Source: NIDDK Research Resources)
Source: NIDDK Research Resources - June 9, 2017 Category: Endocrinology Source Type: research
Linking compounds useful for coupling carbohydrates to amine-containing carriers (U.S. Patent Number 5,952,454)
The present invention provides a method to couple a glycosyl donor to an amine-containing carrier or substrate material using as a spacer a compound of the general formula I: ##STR1## in which n and m are each independently an integer of from 1 to 12, R.sub.1 and R.sub.2 are each independently H, lower alkyl, a hydroxyl group, or a substituent which does not interfere with the linking reactions, R.sub.4 and R.sub.5 are each independently H, lower alkyl, a hydroxyl group, or a substituent which does not interfere with the linking reactions, R.sub.3 and R'.sub.3 are each independently an optionally substituted lower alkyl or...
Source: NIDDK Research Resources - June 9, 2017 Category: Endocrinology Source Type: research
A3 Adenosine Receptor Antagonists (U.S. Patent Number 6,376,521)
This invention relates to a method of decreasing intraocular pressure by administrating an A3 subtype adenosine receptor antagonist, a calmodulin antagonist or an antiestrogen such as tamoxifen. (Source: NIDDK Research Resources)
Source: NIDDK Research Resources - June 9, 2017 Category: Endocrinology Source Type: research
