Abstract: The current invention relates to use of oral pyrophosphate wherein said pyrophosphate is selected from the group consisting of monoarginine pyrophosphate, monolysine pyrophosphate, dipotassium pyrophosphate, bisethanolamine pyrophosphate and bisammonium pyrophosphate for preventing and/or reducing tissue calcification, particularly soft tissue calcification, and/or diseases or disorders characterized by low plasma PPi levels, as, e.g.

Abstract: The present invention provides a compound having the structure: wherein X is CR6 or N; R1, R2, R3, R4, and R6 are each independently —H, —F, —Cl, —Br, —I, —NO2, —CN, —CF3, —CF2H, —OCF3, -(alkyl), -(haloalkyl), -(alkenyl), -(alkynyl), -(aryl), -(heteroaryl), -(cycloalkyl), -(cycloalkylalkyl), -(heteroalkyl), heterocycle, heterocycloalkyl, -(alkylheteroalkyl), -(alkylaryl), —OH, —OAc, —O-(alkyl), —O-(alkenyl), —O-(alkynyl), —O-(aryl), —O-(heteroaryl), —SH, —S-(alkyl), —S-(alkenyl), —S-(alkynyl), —S-(aryl), —S-(heteroaryl), —NH2, —NH-(alkyl), —NH-(alkenyl), —NH-(alkynyl), —NH-(aryl), —NH-(heteroaryl), —C(O)R7, —S(O)R7, —SO2R7, —NHSO2R7, —OC(O)R7, —SC(O)R7, —NHC(O)R8 or —NHC(S) R8, wherein R7 is, H, -(alkyl), —OH, —O(alkyl), —NH2, —NH(alkyl) or —N(alkyl)2, and wherein R8 is, -(alkyl), —O-(alkyl), —NH2, —NH(alkyl) or —N(alkyl)2; Y is O, S, N, NH, or a bond; Z is O, S, N, NH, (CH2)o, or a bond; R5 is H, OH, halogen, alkyl, or R5 is (CH2)p and is bound to Y when Y is N to form a ring together with Z; o and

Abstract: The subject invention provides a method for treating a non-alcoholic fatty liver disease (NAFLD) disease in a subject afflicted therewith comprising administering to the subject a pharmaceutical composition comprising an amount of a compound which is a non-retinoid retinol-binding protein 4 (RBP4) antagonist effective to treat the subject, thereby treating the subject. The subject invention provides a method for treating gout in a subject afflicted therewith comprising administering to the subject a pharmaceutical composition comprising an amount of a compound which is a retinol-binding protein 4 (RBP4) antagonist effective to treat the subject, thereby treating the subject.

Abstract: The invention is concerned with use of oral inorganic pyrophosphate for preventing and/or reducing tissue calcification, particularly soft tissue calcification, and/or diseases or disorders characterized by low plasma PPi levels, as, e.g.

Abstract: The current invention relates to use of oral disodium pyrophosphate for preventing and/or reducing tissue calcification, particularly soft tissue calcification, and/or diseases or disorders characterized by low plasma PPi levels, as, e.g.

Abstract: Described herein are compounds of Formulae (I?)-(II?), compounds of Formulae (I)-(II) and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful for modulating opioid receptor activity. The provided compounds may have both agonistic and antagonistic effect on one or more opioid receptors. Methods of using the compounds for treating or managing pain are also described.

Abstract: Described herein are compounds of Formulae (I?)-(II?), compounds of Formulae (I)-(II) and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful for modulating opioid receptor activity. The provided compounds may have both agonistic and antagonistic effect on one or more opioid receptors. Methods of using the compounds for treating or managing pain are also described.

Abstract: The present invention provides a compound having the structure: wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3, C1-C4 alkyl, aryl or heteroaryl; X is N or CR6, wherein R6 is H, OH, or halogen; A is absent or present, and when present is B has the structure: or a pharmaceutically acceptable salt thereof.

Abstract: The invention is concerned with use of oral inorganic pyrophosphate for preventing and/or reducing tissue calcification, particularly soft tissue calcification, and/or diseases or disorders characterized by low plasma PPi levels, as, e.g.

Abstract: Described herein are compounds of Formulae (I?)-(II?), compounds of Formulae (I)-(II) and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful for modulating opioid receptor activity. The provided compounds may have both agonistic and antagonistic effect on one or more opioid receptors. Methods of using the compounds for treating or managing pain are also described.

Abstract: The invention provides for a novel cholesterol loaded insect cell membrane preparation having an increased cholesterol level as compared to physiological cholesterol levels of insect cell membranes or to control insect cell membrane preparations without cholesterol loading, wherein said cholesterol loaded membrane preparation comprises an ABC transporter protein having an increased substrate transport activity due to increased cholesterol level of the membrane. The invention also relates to reagent kits comprising the preparations of the invention. The invention also relates to methods for manufacturing said preparations and methods for measuring any type of activity of the ABC transporters present in the cholesterol loaded membranes as well as studying or testing compounds and interaction of compounds and ABC transporters, in this assay systems. The invention also provides for a test system useful for testing whether ABC transporter proteins can be activated by cholesterol in an insect cell membrane.

Abstract: The invention provides for a novel cholesterol loaded insect cell membrane preparation having an increased cholesterol level as compared to physiological cholesterol levels of insect cell membranes or to control insect cell membrane preparations without cholesterol loading, wherein said cholesterol loaded membrane preparation comprises an ABC transporter protein having an increased substrate transport activity due to increased cholesterol level of the membrane. The invention also relates to reagent kits comprising the preparations of the invention. The invention also relates to methods for manufacturing said preparations and methods for measuring any type of activity of the ABC transporters present in the cholesterol loaded membranes as well as studying or testing compounds and interaction of compounds and ABC transporters, in this assay systems. The invention also provides for a test system useful for testing whether ABC transporter proteins can be activated by cholesterol in an insect cell membrane.

Abstract: The invention relates to methods for screening selective modulators of half transporter proteins of the ABCG family, more closely of ABCG1 and ABCG4. In particular the invention relates to methods for determining whether a substance is a selective activator, an inhibitor or a substrate of an ABCG1 or ABCG4 homodimer or of an ABCG1/ABCG4 heterodimer protein, methods for detection of ABCG1 protein in a biological sample, methods for modulating the function of said proteins, and methods for detecting the presence of and/or quantitating ABCG1/ABCG4 heterodimer activity in a biological sample. Moreover, the invention relates to isolated ABCG1/ABCG4 heterodimer proteins and antibodies selective for ABCG1 or ABCG4. The closely related human ABC half-transporters, ABCG1 and ABCG4, have been suggested to play an important role in cellular lipid/sterol regulation. ABCG1 and ABCG4 and mutants thereof have been expressed and studied by the present inventors in whole cells as well as isolated membrane preparations.

Abstract: The invention relates to an isolated nucleic acid comprising a sequence encoding a half transporter protein of the ABCG-family for use in gene therapy, to the use of the isolated nucleic acid for selecting somatic mammalian cells against at least one drug transportable by the transporter protein, to vectors, cells, pharmaceutical compositions and kits comprising the nucleic acid and methods for protecting and selecting cells against a cytotoxic drug transportable by said transporter protein and for gene therapy methods.

Abstract: The invention relates to a method for testing L0-specific inhibitors of transporter proteins of the MRP-family and for testing inhibitors specific to the predicted amphipatic helical region of the L0 region, the tested inhibitors L0 peptide, mutants thereof, polynucleotides coding the peptides. Vectors and hosts cells comprising the polynucleotides and reagent kits for testing and developing the inhibitors. The invention is especially useful for combatting multidrug resistance in cancer patients and in the field of related research.