摘要:
The invention features primers capable of distinguishing between highly toxic and minimally toxic strains of Actinobacillus actinomycetemcomitans, methods of detecting the presence of highly toxic and minimally toxic strains of Actinobacillus actinomycetemcomitans in samples obtained from a patient and kits for detection of the presence of highly toxic and minimally toxic strains of Actinobacillus actinomycetemcomitans in samples obtained from a patient.
摘要:
The invention features primers capable of distinguishing between highly toxic and minimally toxic strains of Actinobacillus actinomycetemcomitans, methods of detecting the presence of highly toxic and minimally toxic strains of Actinobacillus actinomycetemcomitans in samples obtained from a patient and kits for detection of the presence of highly toxic and minimally toxic strains of Actinobacillus actinomycetemcomitans in samples obtained from a patient.
摘要:
The present invention provides non-peptide compounds of formula (I) wherein: X is —(C1-C8)allcyl-, aryl or -aryl(C1-C8)alkyl-; Y is —(C1-C8)alkyl- or absent; W is heteroaryl, (C3-C7)carbocycle or aryl, wherein any heteroaryl, (C3-C7)carbocycle or, aryl of W is optionally substituted with one or more (e.g. 1, 2, 3, 4 or 5) Z1 groups; R1 is (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl or aryl, wherein aryl is optionally substituted with one or more (e.g. 1, 2, 3, 4 or 5) groups selected from (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C3-C7)carbocycle, halo(C1-C3)alkyl, —CN, NO2, halogen, —ORa, —SRa, —S(O)2NRbRc, —NRbRc, —NRaCORd, —C(O)Ra, —C(O)ORa, and —C(O)NRbRc; R2 is (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)Jalkynyl or aryl, wherein aryl is optionally substituted with one or more (e.g. 1, 2, 3, 4 or 5) groups selected from (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C3-C7)carbocycle, halo(C1-C3)alkyl, —CN, NO2, halogen, —ORe, —SRe, —S(O)2NRfRg, —NRfRg—NReCORh, —C(O)Re, —C(O)ORe and —C(O)NRfRg; I that mimic the streptococcal; SspB Adherence Region (BAR) and function as inhibitors of P. gingivalis adherence to streptococci. The invention also provides methods of making and using the inhibitors.
摘要翻译:本发明提供了式(I)的非肽化合物,其中:X是 - (C1-C8)环烷基,芳基或 - 芳基(C1-C8)烷基 - ; Y是 - (C1-C8)烷基 - 或不存在; W是杂芳基,(C 3 -C 7)碳环或芳基,其中任何杂芳基,(C 3 -C 7)碳环或W的芳基任选被一个或多个(例如1,2,3,4或5个)Z1基团取代; R 1是(C 1 -C 8)烷基,(C 2 -C 8)烯基,(C 2 -C 8)炔基或芳基,其中芳基任选地被一个或多个(例如,1,2,3,4或5) C1-C8)烷基,(C2-C8)烯基,(C2-C8)炔基,(C3-C7)碳环,卤代(C1-C3)烷基,-CN,NO2,卤素,-ORa,-SRa,-S (O)2 NR b R c,-NR b R c,-NR a COR d,-C(O)R a,-C(O)OR a和-C(O)NR b R c; R 2是(C 1 -C 8)烷基,(C 2 -C 8)烯基,(C 2 -C 8)炔基或芳基,其中芳基任选地被一个或多个(例如,1,2,3,4或5) C1-C8)烷基,(C2-C8)烯基,(C2-C8)炔基,(C3-C7)碳环,卤代(C1-C3)烷基,-CN,NO2,卤素,-ORe,-SRe,-S (O)2 NR f R g,-NR f R g -NrCORh,-C(O)Re,-C(O)OR e和-C(O)NR f R g; 模仿链球菌的我; SspB粘附区(BAR)并且作为牙龈卟啉单胞菌粘附于链球菌的抑制剂。 本发明还提供了制备和使用抑制剂的方法。
摘要:
The present invention provides non-peptide compounds of formula (I) wherein: X is —(C1-C8)allcyl-, aryl or -aryl(C1-C8)alkyl-; Y is —(C1-C8)alkyl- or absent; W is heteroaryl, (C3-C7)carbocycle or aryl, wherein any heteroaryl, (C3-C7)carbocycle or, aryl of W is optionally substituted with one or more (e.g. 1, 2, 3, 4 or 5) Z1 groups; R1 is (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl or aryl, wherein aryl is optionally substituted with one or more (e.g. 1, 2, 3, 4 or 5) groups selected from (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C3-C7)carbocycle, halo(C1-C3)alkyl, —CN, NO2, halogen, —ORa, —SRa, —S(O)2NRbRc, —NRbRc, —NRaCORd, —C(O)Ra, —C(O)ORa, and —C(O)NRbRc; R2 is (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)Jalkynyl or aryl, wherein aryl is optionally substituted with one or more (e.g. 1, 2, 3, 4 or 5) groups selected from (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C3-C7)carbocycle, halo(C1-C3)alkyl, —CN, NO2, halogen, —ORe, —SRe, —S(O)2NRfRg, —NRfRg—NReCORh, —C(O)Re, —C(O)ORe and —C(O)NRfRg; I that mimic the streptococcal; SspB Adherence Region (BAR) and function as inhibitors of P. gingivalis adherence to streptococci. The invention also provides methods of making and using the inhibitors.
摘要翻译:本发明提供了式(I)的非肽化合物,其中:X是 - (C1-C8)环烷基,芳基或 - 芳基(C1-C8)烷基 - ; Y是 - (C1-C8)烷基 - 或不存在; W是杂芳基,(C 3 -C 7)碳环或芳基,其中任何杂芳基,(C 3 -C 7)碳环或W的芳基任选被一个或多个(例如1,2,3,4或5个)Z1基团取代; R 1是(C 1 -C 8)烷基,(C 2 -C 8)烯基,(C 2 -C 8)炔基或芳基,其中芳基任选地被一个或多个(例如,1,2,3,4或5) C1-C8)烷基,(C2-C8)烯基,(C2-C8)炔基,(C3-C7)碳环,卤代(C1-C3)烷基,-CN,NO2,卤素,-ORa,-SRa,-S (O)2 NR b R c,-NR b R c,-NR a COR d,-C(O)R a,-C(O)OR a和-C(O)NR b R c; R 2是(C 1 -C 8)烷基,(C 2 -C 8)烯基,(C 2 -C 8)炔基或芳基,其中芳基任选地被一个或多个(例如,1,2,3,4或5) C1-C8)烷基,(C2-C8)烯基,(C2-C8)炔基,(C3-C7)碳环,卤代(C1-C3)烷基,-CN,NO2,卤素,-ORe,-SRe,-S (O)2 NR f R g,-NR f R g -NrCORh,-C(O)Re,-C(O)OR e和-C(O)NR f R g; 模仿链球菌的我; SspB粘附区(BAR)并且作为牙龈卟啉单胞菌粘附于链球菌的抑制剂。 本发明还提供了制备和使用抑制剂的方法。
摘要:
The present invention provides streptococcal SspB Adherence Region (BAR) peptides consisting of Formula I: R18-R1- R2-Val-R3-R4-Leu-Leu-R5-R6-R7-Ile-R8-R9-Lys-R10-R19 , wherein R2, is 1-3 Lys residues; R3 is any amino acid residue except a Pro residue; R4 is any amino acid residue except a Pro residue; R5 is 1-3 Lys residues; R6 is 1-10 amino acid residues; R7 is any amino acid residue except Asp, Glu, Gly or Pro; R8 is any amino acid residue except Ala, Asp, Gly, His, Ile, Pro, Trp or Tyr; R9 is a Val, Ile, Phe, or Trp residue; R10 is 0-1 Cys residue; R18 is 0 amino acids or R12-R11-Pro-, wherein R11 is 0-3 amino acids, wherein the amino acid residues are not Gly or Pro; and R12 is 0-1 Cys residues; and R19 is R13-R14-R15-R16-R17, wherein R13 is 0-1 is Gly residue; R14 is 0-1 Ala residue; R15 is 0-1 Phe residue; R16 is 0-1 Gln residue; R17 is 0-1 Cys residue; and wherein R1 is an ornithine residue; or wherein both R1 and R10 are both Cys and R1 and R10 are covalently linked to form a circular peptide; or wherein R1 is 0-1 Cys or an ornithine residue and R12 and R17, are both Cys and R12 and R17 are covalently linked to form a circular peptide. Embodiments of the present invention further provide devices coated with the BAR peptides.
摘要:
The present invention provides streptococcal SspB Adherence Region (BAR) peptides, nucleic acids encoding the BAR peptides, and methods of using the BAR peptides, and methods of screening BAR peptide mimetics.