Diversity-Oriented Synthesis for Novel, Selective and Drug-like Inhibitors for a Phosphatase from Mycobacterium Tuberculosis

Simple item page
dc.contributor.authorHe, Rongjun
dc.contributor.authorBai, Yunpeng
dc.contributor.authorYu, Zhi-Hong
dc.contributor.authorWu, Li
dc.contributor.authorGunawan, Andrea Michelle
dc.contributor.authorZhang, Zhong-Yin
dc.contributor.departmentDepartment of Biochemistry & Molecular Biology, IU School of Medicineen_US
dc.date.accessioned2016-08-23T12:57:27Z
dc.date.available2016-08-23T12:57:27Z
dc.date.issued2014-10
dc.description.abstractMycobacterium protein tyrosine phosphatase B (mPTPB) is a potential drug target of Tuberculosis (TB). Small molecule inhibitors of mPTPB could be a treatment to overcome emerging TB drug resistance. Using a Diversity-Oriented Synthesis (DOS) strategy, we successfully developed a salicylic acid based and drug-like mPTPB inhibitor with an IC50 of 2 μM and >20-fold specificity over many human PTPs, making it an excellent lead molecule for anti-TB drug discovery. In addition, DOS generated bicyclic salicylic acids are also promising starting points for acquiring inhibitors targeting other PTPs.en_US
dc.eprint.versionAuthor's manuscripten_US
dc.identifier.citationHe, R., Bai, Y., Yu, Z.-H., Wu, L., Gunawan, A. M., & Zhang, Z.-Y. (2014). Diversity-Oriented Synthesis for Novel, Selective and Drug-like Inhibitors for a Phosphatase from Mycobacterium Tuberculosis. MedChemComm, 5(10), 1496–1499. http://doi.org/10.1039/C4MD00099Den_US
dc.identifier.urihttps://hdl.handle.net/1805/10754
dc.language.isoen_USen_US
dc.publisherRoyal Society of Chemistryen_US
dc.relation.isversionof10.1039/C4MD00099Den_US
dc.relation.journalMedChemCommen_US
dc.rightsPublisher Policyen_US
dc.sourcePMCen_US
dc.subjectMycobacterium protein tyrosine phosphatase Ben_US
dc.subjectTuberculosisen_US
dc.subjectTB drug resistanceen_US
dc.titleDiversity-Oriented Synthesis for Novel, Selective and Drug-like Inhibitors for a Phosphatase from Mycobacterium Tuberculosisen_US
dc.typeArticleen_US
Files
Original bundle
Now showing 1 - 1 of 1
Thumbnail Image
Name:
nihms-619488.pdf
Size:
307.53 KB
Format:
Adobe Portable Document Format
Description:
Main Article
Download
License bundle
Now showing 1 - 1 of 1
No Thumbnail Available
Name:
license.txt
Size:
1.88 KB
Format:
Item-specific license agreed upon to submission
Description:
Download
Collections
Open Access Policy Articles
Department of Biochemistry and Molecular Biology Works