Abstract: Provided is a high-throughput coupled enzyme method of screening for a tryptophan-2,3-dioxygenase (TDO) inhibitor compound and/or an indoleamine-2,3-dioxygenase (IDO) inhibitor compound, which method comprises: (a) reacting tryptophan with isolated IDO and/or isolated TDO in the presence of a test compound to form N-formylkynurenine; (b) reacting N-formylkynurenine from step (a) with isolated kynurenine formamidase to form kynurenine; and (c) detecting the kynurenine produced in step (b) and determining whether the test compound is a TDO and/or an IDO inhibitor compound or not from the presence or absence or quantity of the detected kynurenine, wherein step (a) is conducted in the presence of a reducing system suitable for converting IDO and/or TDO from the Fe3+ to the Fe2+ state, and which does not prevent the formation of kynurenine in step (c).

Abstract: Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises formula (I) wherein X1, and X2 may be the same or different and each is independently selected from C, N, O and S; X3, X4, X5, and X6 may be the same or different and each is independently selected from C and N; each bond represented by a dotted line may be present or absent, provided that at least one such bond is present; R1, R2, R3, R4, R5 and R6 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R1, R2, R3, R4, R5 and R6 groups present is such that the respective valencies of X1, X2, X3, X4, X5, and X6 are maintained; and wherein at least one of R5 and R6 comprises a group Y, wherein Y is a group having a formula selected from (II), (III), (IV), (V), (VI), (VII) wherein L may be present or absent, and may be a substituted or unsub

Abstract: Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula (I): wherein X1 is selected from C and N; X3 and X5 may be the same or different and each is independently selected from C, N, O and S; Y is selected from N and O; Z is selected from C, N and O; each bond represented by a dotted line may independently be a double bond or a single bond, provided that valencies at each ring atom are maintained and provided that the ring Q contains at least one double bond and provided that the atom N has a double bond; R3 and R5 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R3 groups present is such that the valency of X3 is maintained, and the number of R5 groups present is such that the valency of X5 is maintained; each R11 and R12 may be present or absent and may be the sam

Abstract: Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the general formula (I) detailed within.

Abstract: Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula: wherein X2, X4, X10, and X11 may be the same or different and each is independently selected from C and N; X1, X3, X5, X6, X7, X8, and X9 may be the same or different and each is independently selected from C, N and O; each bond having a dotted line may independently be a double bond or a single bond, provided that valencies at each atom are maintained; the dotted lines joining X4 with the carbon atoms either side of X2 are single bonds, and are only present when X2 is absent, X3 is absent and X4 is C, and when these bonds are present the ring carbons on each side of X2 are not directly bonded to each other; each R1 may be present or absent and may be the same or different and is selected from H and a substituted or unsubstituted organic group, provided that the number of R1 groups present is such that the valency of X1 is maintaine

Abstract: Provided is a compound for use in medicine for inhibiting tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO), which compound comprises formula (I) wherein X1, X2, and X7, may be the same or different and each is independently selected from C and N; X3, X4, X5, and X6 may be the same or different and each is independently selected from C, N, O and S wherein when X3 is N it has a double bond and wherein when X6 is N it has a double bond; the dotted line is a bond which may be present or absent; R1, R2, R3, R4, R5, R6, and R7 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that at least one of R2, R3, R4 and R6 comprises a group Y; and provided that the number of R1, R2, R3, R4, R5, R6, and R7 groups present is such that the respective valencies of X1, X2, X3, X4, X5, X6, and X7 are maintained; and wherein Y is a group having a formula selected from (II), (III), (IV), (V) wherein

Abstract: Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula (I): wherein X1 is selected from C and N; X3 and X5 may be the same or different and each is independently selected from C, N, O and S; Y is selected from N and O; Z is selected from C, N and O; each bond represented by a dotted line may independently be a double bond or a single bond, provided that valencies at each ring atom are maintained and provided that the ring Q contains at least one double bond and provided that the atom N has a double bond; R3 and R5 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R3 groups present is such that the valency of X3 is maintained, and the number of R5 groups present is such that the valency of X5 is maintained; each R11 and R12 may be present or absent and may be the sam

Abstract: Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula: wherein X1, X2, X3, X4, and X5 may be the same or different and each is independently selected from C, N and O; each atom having a dotted line may independently have a double bond or a single bond, provided that valencies at each atom are maintained; each R1, R2, R3, R4, R5, and R7 may be present or absent and may be the same or different and is selected from H and a substituted or unsubstituted organic group, provided that the number of such R groups present is such that the valencies of X1, X2, X3, X4, and X5 are maintained; one or two R6 groups may be present and are selected from H and a substituted or unsubstituted organic group, provided that the number of R6 groups present is such that the valency of the carbon atom to which they are attached is maintained, and provided that at least one R6 is an organic group comprising an atom

Abstract: Provided is a high-throughput coupled enzyme method of screening for a tryptophan-2,3-dioxygenase (TDO) inhibitor compound and/or an indoleamine-2,3-dioxygenase (IDO) inhibitor compound, which method comprises: (a) reacting tryptophan with isolated IDO and/or isolated TDO in the presence of a test compound to form N-formylkynurenine; (b) reacting N-formylkynurenine from step (a) with isolated kynurenine formamidase to form kynurenine; and (c) detecting the kynurenine produced in step (b) and determining whether the test compound is a TDO and/or an IDO inhibitor compound or not from the presence or absence or quantity of the detected kynurenine, wherein step (a) is conducted in the presence of a reducing system suitable for converting IDO and/or TDO from the Fe3+ to the Fe2+ state, and which does not prevent the formation of kynurenine in step (c).

Abstract: Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula: wherein X2, X4, X10, and X11 may be the same or different and each is independently selected from C and N; X1, X3, X5, X6, X7, X8, and X9 may be the same or different and each is independently selected from C, N and O; each bond having a dotted line may independently be a double bond or a single bond, provided that valencies at each atom are maintained; the dotted lines joining X4 with the carbon atoms either side of X2 are single bonds, and are only present when X2 is absent, X3 is absent and X4 is C, and when these bonds are present the ring carbons on each side of X2 are not directly bonded to each other; each R1 may be present or absent and may be the same or different and is selected from H and a substituted or unsubstituted organic group, provided that the number of R1 groups present is such that the valency of X1 is maintaine

Abstract: Provided is a SLC2A class I transporter inhibitor compound for use in medicine, which compound comprises the following formula: wherein A and Z may be the same or different and are each independently selected from C, N, O and S; each X may be the same or different and is independently selected from C, N, O and S; R1 and R5 may be present or absent and may be the same or different and are each selected from H and a substituted or unsubstituted organic group; Z completes a ring with each X, each ring comprising from 3 to 8 ring atoms including the X, A, and Z, each ring atom being independently selected from C, N, O and S, and each ring atom being unsubstituted or independently substituted with H or a substituted or unsubstituted organic group; and wherein the bonds between all of the atoms in the rings including the X, A, and Z may independently be single bonds or double bonds, provided that when X or a ring atom is O or S the bonds to X are single bonds.

Abstract: The present invention relates to the novel GABAB receptor subtypes GABAB-R1c and GABAB-R2 as well as to a novel, functional GABAB receptor which comprises a heterodimer of GABAB-R1 and GABAB-R2 receptor subunits. The present invention also relates to variants of the receptors, nucleotide sequences encoding the receptors and variants thereof and novel vectors, stable cell lines, antibodies, screening methods, methods of treatment and methods of receptor production.

Abstract: A method of treating HM74A and/or HM74 mediated disease in an individual which comprises administering to the individual a therapeutic amount of a modulator of HM74A and/or HM74 activity.

Abstract: The present invention relates to the modification of the CC chemokine receptor 3 to stabilise or enhance surface expression, for example, to reduce internalization and/or kinase-mediated phosphorylation. The invention also relates to assays for CCR3 receptor activity in which internalization and/or kinase mediated phosphorylation of the receptor is reduced.

Abstract: A method for identification of an agent that modulates activity of G-protein coupled receptor 55 (GPR 55), which method comprises: (i) contacting a test agent with GPR 55 or a variant thereof which is capable of coupling to a G-protein; and (ii) monitoring for GPR 55 activity in the presence of a G-protein; thereby determining whether the test agent modulates GPR 55 activity.

Abstract: This invention relates to a method for identification of an agent that modulates activity of G-protein coupled receptor 41 (GPR 41), or G-protein coupled receptor 42 (GPR 42) which method comprises: (i) contacting a test agent with GPR 41, GPR42 or a variant of either thereof which is capable of coupling to a G-protein; and (ii) monitoring for GPR 41 or GPR 42 activity in the presence of a G-protein; thereby determining whether the test agent modulates GPR 41 or GPR 42 activity. An agent identifiable by this method is provided for use in the treatment of dyslipidaemia, coronary heart disease, atheroselerosis, thrombosis or obesity, angina, chronic renal failure, peripheral vascular disease, stroke, type II diabetes or metabolic syndrome (syndrome X).

Abstract: The present invention relates to the novel GABAB receptor subtypes GABAB-R1c and GABAB-R2 as well as to a novel, functional GABAB receptor which comprises a heterodimer of GABAB-R1 and GABAB-R2 receptor subunits. The present invention also relates to variants of the receptors, nucleotide sequences encoding the receptors and variants thereof and novel vectors, stable cell lines, antibodies, screening methods, methods of treatment and methods of receptor production.

Abstract: The present invention relates to the novel GABAB receptor subtypes GABAB-R1c and GABAB-R2 as well as to a novel, functional GABAB receptor which comprises a heterodimer of GABAB-R1 and GABAB-R2 receptor subunits. The present invention also relates to variants of the receptors, nucleotide sequences encoding the receptors and variants thereof and novel vectors, stable cell lines, antibodies, screening methods, methods of treatment and methods of receptor production.