摘要:
A method of identifying an antifungal agent which targets a PPTB protein of a fungus comprising determining whether a candidate compound binds to or inhibits a PPTB protein, wherein binding or inhibition indicates that the candidate substance is an antifungal agent.
摘要:
A method of identifying an antifungal agent which targets a PPTB protein of a fungus comprising determining whether a candidate compound binds to or inhibits a PPTB protein, wherein binding or inhibition indicates that the candidate sub-stance is an antifungal agent.
摘要:
Method of identifying an anti-fungal agent which targets as an essential protein or gene of a fungus comprising contacting a candidate substance with (i) a protein which comprises the sequence shown by SEQ ID NOS: 3, 6, 9, 12, 15, 18, 21, 24, 27, 30, 33, 36, 39, 42, 45, 48, 50, 53, 56, 59, 61 or 63, or (ii) a protein which has 60% identity with (i), or (iii) a protein comprising a fragment of (i) or (ii) which fragment has a length of at least 50 amino acids, or (iv) a polynucleotide that comprises a sequence which encodes (i), (ii) or (iii), or (v) a polynucleotide comprising a sequence which has at least 70% identity with the coding sequence of (iv), and determining whether the candidate substance binds or modulates (i), (ii), (iii), (iv), or (v), wherein binding or modulation of (i), (ii), (iii), (iv), or (v) indicates that the candidate substance is an anti-fungal agent.
摘要翻译:鉴定靶向作为真菌的必需蛋白质或基因的抗真菌剂的方法,包括使候选物质与(i)包含SEQ ID NO:3,6,9,12,15, 18,21,24,27,30,33,36,39,42,45,48,50,53,56,59,61或63,或(ii)与(i)具有60%同一性的蛋白质, 或(iii)包含(i)或(ii)的片段的蛋白质,所述片段具有至少50个氨基酸的长度,或(iv)包含编码(i),(ii)或( iii)或(v)多核苷酸,其包含与(iv)的编码序列具有至少70%同一性的序列,并确定候选物质是否结合或调节(i),(ii),(iii),( iv)或(v),其中(i),(ii),(iii),(iv)或(v)的结合或调节表明候选物质是抗真菌剂。
摘要:
Method of identifying an anti-fungal agent which targets an essential protein or gene of a fungus comprising contacting a candidate substance with (i) a NADH:flavin oxidoreductase protein which comprises the sequence shown by SEQ ID NO:3, (ii) a NADH:flavin oxidoreductase protein which is a homologue of (i) and which comprises the sequence shown by SEQ ID NO: 8, 12, 14, 19, 24, 42, 44, 83 or 85, (iii) a protein which has 50% identity with (i) or (ii), (iv) a protein comprising a fragment of (i), (ii) or (iii) which fragment has a length of at least 50 amino acids, (v) a polynucleotide that comprises sequence which encodes (i), (ii), (iii) or (iv), (vi) a polynucleotide comprising sequence which has at least 70% identity with the coding sequence of (v), and determining whether the candidate substance binds or modulates (i), (ii), (iii), (iv), (v) or (vi), wherein binding or modulation of (i), (ii), (iii), (iv), (v) or (vi) indicates that the candidate substance is an anti-fungal agent.
摘要翻译:鉴定靶向真菌的必需蛋白质或基因的抗真菌剂的方法,包括使候选物质与(i)包含SEQ ID NO:3所示序列的NADH:黄素氧化还原酶蛋白质接触,(ii)NADH :(i)的同系物的黄素氧化还原酶蛋白,其包含SEQ ID NO:8,12,14,19,24,42,44,83或85所示的序列,(iii)具有50% 与(i)或(ii)的同一性,(iv)包含(i),(ii)或(iii)的片段的蛋白质,该片段长度为至少50个氨基酸,(v)包含序列 其编码(i),(ii),(iii)或(iv),(vi)包含与(v)的编码序列具有至少70%同一性的序列的多核苷酸,并确定候选物质是否结合或调节 (i),(ii),(iii),(iv),(v)或(vi)中的(i),(ii),(iii) vi)表示候选物质是抗真菌剂。
摘要:
A method of identifying an antifungal agent which targets a DHODH protein (alias PyrE, dihydroorotate dehydrogenase, EC: 1.3.99.11) of a fungus comprising contacting a candidate substance with a fungal DHODH protein and determining whether the candidate substance binds or modulates the DHODH protein, wherein binding or modulation indicates that the candidate substance is an antifungal agent. Specific examples concern Aspergillus fumigatus and Candida albicans DHODH proteins. DHODH inhibitors with a Quinazolinone core are also disclosed.
摘要:
A method of identifying an antifungal agent which targets a DHODH protein (alias PyrE, dihydroorotate dehydrogenase, EC: 1.3.99.11) of a fungus comprising contacting a candidate substance with a fungal DHODH protein and determining whether the candidate substance binds or modulates the DHODH protein, wherein binding or modulation indicates that the candidate substance is an antifungal agent. Specific examples concern Aspergillus fumigatus and Candida albicans DHODH proteins. DHODH inhibitors with a Quinazolinone core are also disclosed.
摘要:
The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof; wherein: R1, R2, R3, R4, R5, R6, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
摘要:
The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof; wherein: R1, R2, R3, R4, R5, R6, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
摘要:
The invention provides pharmaceutical combinations comprising a combination of an antifungal indolizine compound of formula (I) or a pharmaceutically acceptable salt thereof and a second antifungal agent: wherein: R1, R2, R3, R4, R5, R6, R7, X and X1 are as defined herein. The invention also provides pharmaceutical compositions comprising an antifungal indolizine compound of formula (I) or a pharmaceutically acceptable salt thereof, a second antifungal agent and a pharmaceutically acceptable diluent or carrier. The combinations and compositions are useful in the prevention or treatment of a fungal disease. A combination of an indolizine compound of formula (I) or agriculturally acceptable salts thereof and a second antifungal agent may also be used as an agricultural fungicide.