CONJUGATE-BASED ANTIFUNGAL AND ANTIBACTERIAL PRODRUGS
申请人:Bapat Abhijit S.
公开号:US20140364595A1
公开(公告)日:2014-12-11
The invention provides conjugate-based antifungal or antibacterial prodrugs formed by coupling at least one anti-fungal agent or antibacterial agent with at least one linker and/or carrier. The prodrugs are of formula: (i) (AFA)
m
-X-(L)
n
; (ii) [(AFA)
m′
-X]
p
-L; (iii) AFA-[X-(L)
n′
]
q
; or (iv) (AFA)
m″
-X, wherein: AFA is an antifungal agent or an antibacterial agent; L is a carrier; X is a linker; m ranges from 1 to 10; n ranges from 2 to 10; m′ is 1 to 10; p is 1 to 10; n′ is 1 to 10; and q is 1 to 10, provided that q′ and n are not both 1; and m″ is 1 to 10. The invention also provides nanoparticles comprising the conjugate-based prodrugs. Additionally, the invention also provides non-conjugated antifungal and antibacterial agents in the form of nanoparticles.
该发明提供了由至少一种抗真菌剂或抗菌剂与至少一种连接剂和/或载体偶联形成的基于共轭的抗真菌或抗菌前药。这些前药的公式为:(i) (AFA)
m
-X-(L)
n
; (ii) [(AFA)
m′
-X]
p
-L; (iii) AFA-[X-(L)
n′
]
q
; 或 (iv) (AFA)
m″
-X,其中:AFA是抗真菌剂或抗菌剂;L是载体;X是连接剂;m范围从1到10;n范围从2到10;m′为1到10;p为1到10;n′为1到10;q为1到10,前提是q'和n不同时为1;m″为1到10。该发明还提供了包含基于共轭的前药的纳米粒子。此外,该发明还提供了以纳米粒子形式的非共轭抗真菌和抗菌剂。
GRAMICIDIN A MUTANTS THAT FUNCTION AS ANTIBIOTICS WITH IMPROVED SOLUBILITY AND REDUCED TOXICITY
申请人:Trustees of boston College
公开号:US20150239936A1
公开(公告)日:2015-08-27
Described herein are antimicrobial peptides for use in pharmaceutical antibiotic compositions and methods of use thereof. These antimicrobial peptides are Gramicidin A (gA) peptide analogs that, in addition to having potent anti-microbial activity, have greatly increased solubility and significantly reduced toxicity in comparison to the wild-type Gramicidin A peptide.
Lin28/let-7 crystal structures, purification protocols, and molecular probes suitable for screening assays and therapeutics
申请人:PRESIDENT AND FELLOWS OF HARVARD COLLEGE
公开号:US10000756B2
公开(公告)日:2018-06-19
The invention provides compositions and methods for regulating microRNA (miRNA) biogenesis. The invention also relates to compositions and methods for treating or preventing cancer in a subject in need thereof.
Modified integrin polypeptides, modified integrin polypeptide dimers, and uses thereof
申请人:THE CHILDREN'S MEDICAL CENTER CORPORATION
公开号:US10273283B2
公开(公告)日:2019-04-30
Described herein are modified integrin α and/or β headpiece polypeptides, and crystallizable integrin polypeptide dimers comprising a modified integrin α and/or β headpiece polypeptide and a disulfide bond linking the two integrin headpiece polypeptide subunits. Methods for using the modified integrin α and/or β headpiece polypeptides and the integrin polypeptide dimers are also provided herein. For example, methods for characterizing integrin-ligand interaction and identifying integrin ligands are also provided herein. In some embodiments, the identified integrin ligands can be used as inhibitors of integrins.
Novel amino acid and peptide inhibitors of Staphylococcus virulence
申请人:——
公开号:US20030050248A1
公开(公告)日:2003-03-13
Isolated synthetic modified amino acids and peptides, which inhibit of the production of virulence factors in bacteria, particularly Staphylococcus, are described. The amino acids and peptides can be used in a method for treatment or prevention of Staphylococcal infections or can be integrated into a medical device to inhibit the development of infection associated with the use of such devices.