Search Results - patrick+woster

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N-aroylanthranilic acids and derivatives as inhibitors of bacterial class B transpeptidases
Technology: MUSC inventors identified a new chemical scaffold (N-aroylanthranilic acids and derivatives) as inhibitors of various class B penicillin-binding proteins (PBPs). The novel molecules showed high potency of PBP inhibition. Antimicrobial assays against antibiotic-resistant gonorrhea strain FA19 and H041 showed significant growth inhibition...
Published: 11/9/2020   |   Inventor(s): Jonathan Turner, Christopher Davies, Patrick Woster, Joy Kirkpatrick
Keywords(s):  
Category(s): Therapeutic
Inhibition of the Histone Demethylase KDM4B Leads to Activation of KDM1A, Attenuates Bacterial-Induced Pro-Inflammatory Cytokine Release and Reduces Osteoclastogenesis
Technology: Researchers at MUSC have discovered a series of novel small molecules that contain potent immunosuppressive activity and can be used as the new treatment for periodontal disease (PD). PD is caused by bacteria infection in dental plaque, which leads to the inflammation response in the area of gums, periodontal ligament or alveolar bone....
Published: 8/13/2019   |   Inventor(s): Patrick Woster, Joy Kirkpatrick
Keywords(s):  
Category(s): Therapeutic
LSD1 Protein Inhibitors as Fetal Hemoglobin Inducers for Sickle Cell Disease
Technology: Researchers at MUSC have identified several potential inhibitors of lysine-specific demethylase 1 (LSD1) utilizing a virtual screen and found compounds that fit the LSD1 active site in silico. Next, they synthesized these molecules and evaluated them as highly selective LSD1 inhibitors. The series of compounds are new chemical entities being...
Published: 4/4/2017   |   Inventor(s): Patrick Woster, Craig Kutz
Keywords(s):  
Category(s): Therapeutic
Non-Aniline Histone Deacetylase Inhibitors
Technology: Inventors at MUSC have discovered a 2-(oxazol-2-yl)phenol moiety containing a novel zinc binding group (ZBG) that can be used to produce compounds that are potent histone deacetylase (HDAC) inhibitors. A series of 15 analogues with the novel ZBG have been synthesized, and exhibit selective inhibition against HDAC1 as well as HDAC 6 &...
Published: 3/24/2015   |   Inventor(s): Patrick Woster, Youxuan Li
Keywords(s):  
Category(s): Therapeutic
LSD1 Protein Inhibitors as Cancer Therapeutics
Technology: Researchers at MUSC have identified several potential inhibitors of lysine-specific demethylase 1 (LSD1) utilizing a virtual screen and found compounds that fit the LSD1 active site in silico. LSD1 is overexposed in a number of human cancers (neuroblastoma, retinoblastoma, prostate, cancer, lung, and bladder), and has emerged as an important...
Published: 5/13/2014   |   Inventor(s): Patrick Woster, Craig Kutz
Keywords(s):  
Category(s): Therapeutic
Cyclic Peptide Inhibitors of Lysine-Specific Demethylase 1 (LSD1)
Technology: Researchers at MUSC have used a ligand-based approach to design and synthesize a series of cyclic peptides that are effective inhibitors of LSD1, and have greater stability to proteolytic degradation than their linear homologues. Cyclic peptide 9 inhibits LSD1 in vitro with a Ki value of 385 nM, and has antitumor activity in MCF-7 and Calu-6...
Published: 5/13/2014   |   Inventor(s): Patrick Woster, Isuru Kumarasinghe
Keywords(s): cancer
Category(s): Therapeutic
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