摘要:
The present invention provides a protein regulating the sensitivity of fungus to an antimycotic aureobasidin, a gene coding for this protein, the use thereof, an antibody for the protein and the use thereof. The invention is useful in the diagnosis and treatment for diseases including mycoses. The invention also provides a novel chromosome integration vector capable of imparting a novel selective marker of a drug resistance to a fungal transformant, a transformant transformed with this vector and a process for producing the same. In particular, it provides a protein capable of imparting the resistance to aureobasidin and acting as a selective marker and a DNA coding for the same.
摘要:
The present invention has its object to provide a noble antifungal substance which is use of as clinical medicine in the therapy of fungal infectious diseases. The present invention is related to an antibiotic TKR459 having the following chemical formula (1) or its pharmacologically acceptable salt.
摘要:
The object of the present invention is to provide a novel bioactive substance of value as a therapeutic agent for mycosis, and the like.This invention relates to the bioactive substance TKR1785 of the following general formula (A): ##STR1## (wherein R represents --CH(CH.sub.3).sub.2 or --CH(CH.sub.3)C.sub.2 H.sub.5).
摘要:
A gene associated with sensitivity to the antimycotic agent, aureobasidin A, has been isolated. The gene can be detected in a variety of cell types, and variant forms of the gene have been identified in mutant yeast strains. The proteins encoded by these genes are useful in diagnosing and treating mycoses.
摘要:
This invention relates to Aureobasidins useful as an antifungal agent having broader spectrum. The compound according to this invention includes a cyclic depsipeptide consisting of one hydroxy acid residue having A.sup.1, 3 amino acid residues having C.sup.1, F.sup.1 and H.sup.1, respectively, 4 N-methylamino acid residues having B.sup.1, D.sup.1, G.sup.1 and I.sup.1, respectively, and 1 cyclic amino acid residue having E.sup.1. The typical compound includes one wherein A.sup.1 is CH.sub.3 CH.sub.2 CH(CH.sub.3)--, B.sup.1 is (CH.sub.3).sub.2 CH--, C.sup.1 is benzyl, cyclohexylmethyl, p-fluorobenzyl, benzyloxymethyl, benzyloxybenzyl, methoxybenzyl, cyclohexylmethyloxybenzyl or the like, D.sup.1 is methyl, benzyl, hydroxymethyl or the like, E.sup.1 is --(CH.sub.2).sub.3 --, F.sup.1 is CH.sub.3 CH.sub.2 CH(CH.sub.3)--, G.sup.1 is (CH.sub.3).sub.2 CH--, H.sup.1 is (CH.sub.3).sub.2 CHCH.sub.2 -- and I.sup.1 is (CH.sub.3).sub.2 C(OH)--. The compound according to this invention has an excellent activity against not only Candida but also Cryptococcus and Aspergillus.
摘要:
An antibiotic R106 represented by the general formula I): ##STR1## wherein: R is methyl or ethyl;X.sub.1 is MePhe, .beta.-HOMePhe or Phe;X.sub.2 is allo-Ile, Val or Leu;X.sub.3 is MeVal or Val;X.sub.4 is .beta.-HOMeVal, .gamma.-HOMeVal, MeVal, Val, N,.beta.-MeAsp, .beta.-HOMePhe, MePhe, MeDH.sub.2,3 Val or MeDH.sub.3,4 Valis produced by a process which comprises culturing a strain of the genus Aureobasidium that is capable of producing the said antibiotic R106 and collecting the said antibiotic from the fermentation broth. The antibiotic R106 compounds are useful in the treatment of fungal infection.
摘要:
An antibiotic R106 represented by the general formula (I): ##STR1## wherein: R is methyl or ethyl;X.sub.1 is MePhe, .beta.-HOMePhe or Phe;X.sub.2 is allo-Ile, Val or Leu;X.sub.3 is MeVal or Val;X.sub.4 is .beta.-HOMeVal, .gamma.-HOMeVal, MeVal, Val, N,.beta.-MeAsp, .beta.-HOMePhe, MePhe, MeDH.sub.2,3 Val or MeDH.sub.3,4 Valis produced by a process which comprises culturing a strain of the genus Aureobasidium that is capable of producing the said antibiotic R106 and collecting the said antibiotic from the fermentation broth. The antibiotic R106 compounds are useful in the treatment of fungal infection.
摘要:
There are provided R106 compounds represented by the following general formula (I): ##STR1## wherein: A.sub.1 is Phe, o-FPhe, m-FPhe, or Tyr;A.sub.2 is MePhe, o-FMePhe, m-FMePhe, MeTyr, Sar, MeSery, or .beta.-oxoMePhe;A.sub.3 is Pro, 4Hyp, or SPro;A.sub.4 is allo-Ile or Nle;A.sub.5 is Leu or Nva;A.sub.6 is .beta.-HOMeVal or Sar;excluding those wherein A.sub.1 is Phe and A.sub.2 is MePhe and A.sub.3 is Pro and A.sub.4 is allo-Ile and A.sub.5 is Leu and A.sub.6 is .beta.-HOMeVal (SEQ ID No. 4), which are useful as therapeutic agents for fungal infection.
摘要:
The feature of the present invention is a process for preparing compounds represented by general formula (Ia) described below: ##STR1## wherein X.sub.1, X.sub.2, X.sub.3, R.sub.1, R.sub.2, R.sub.3 and R.sub.7 are as defined in formula (I) and R.sub.10 represents a lower alkyl group, or acid salts thereof, which process is characterized by using the guanidylfungins (II) as raw materials, reacting these guanidylfungins with alcohols (III) in the presence of an acid catalyst, and then hydrolyzing the malonic acid monoester (IV).
摘要:
An antibiotic R106 represented by the general formula (I): ##STR1## wherein: R is methyl or ethyl;X.sub.1 is MePhe, .beta.-HOMePhe or Phe;X.sub.2 is allo-Ile, Val or Leu;X.sub.3 is MeVal or Val;X.sub.4 is .beta.-HOMeVal, .gamma.HOMeVal, MeVal, Val, N,.beta.-MeAsp, .beta.-HOMePhe, MePhe, MeDH.sub.2,3 Val or MeDH.sub.3,4 Valis produced by a process which comprises culturing a strain of the genus Aureobasidium that is capable of producing the said antibiotic R106 and collecting the said antibiotic from the fermentation broth. The antibiotic R106 compounds are useful in the treatment of fungal infection.