Tracy Bayliss

Identification and Evaluation of Dibasic Piperidines as Cell Wall Inhibitors against Mycobacterium tuberculosis

Claire Naylor, Gareth A. Prosser, Tracy Bayliss, Lila Berle et autres

remains a significant burden. Although effective treatment regimens exist, drug resistance has continued to emerge. This clinical resistance, combined with side effects and protracted treatment times from the current front-line therapies, means that there is a need to identify novel agents to …

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Identification and Evaluation of dibasic piperidines as novel cell wall inhibitors against Mycobacterium tuberculosis

Claire E. Naylor, Gareth A. Prosser, Tracy Bayliss, Lila Berle et autres

remains a significant disease burden. Although effective treatment regimens exist, drug resistance continues to emerge. This clinical resistance, combined with side effects and protracted treatment times from the current front-line therapies, means there is a need to identify novel agents to combat …

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Inhibiting Mycobacterium tuberculosis CoaBC by targeting an allosteric site

V. Mendes, Simon R. Green, Joanna C. Evans, Jeannine Hess et autres

Coenzyme A (CoA) is a fundamental co-factor for all life, involved in numerous metabolic pathways and cellular processes, and its biosynthetic pathway has raised substantial interest as a drug target against multiple pathogens including Mycobacterium tuberculosis. The biosynthesis of CoA is performed …

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Antitubercular 2-Pyrazolylpyrimidinones: Structure–Activity Relationship and Mode-of-Action Studies

Candice Soares de Melo, Vinayak Singh, Alissa Myrick, Sandile B. Simelane et autres

Abstract Phenotypic screening of a Medicines for Malaria Venture compound library against Mycobacterium tuberculosis (Mtb) identified a cluster of pan-active 2-pyrazolylpyrimidinones. The biology triage of these actives using various tool strains of Mtb suggested a novel mechanism of action. The compounds were …

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Inhibiting Mycobacterium tuberculosis CoaBC by targeting a new allosteric site

V. Mendes, Simon R. Green, Joanna C. Evans, Jeannine Hess et autres

Abstract Coenzyme A (CoA) is a fundamental co-factor for all life, involved in numerous metabolic pathways and cellular processes, and its biosynthetic pathway has raised substantial interest as a drug target against multiple pathogens including Mycobacterium tuberculosis . The biosynthesis of CoA …

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BindingDB Entry 50000459: Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors.

BindingDB, Tiqing Liu, Michael Gilson, Tracy Bayliss et autres

Small molecule binding data for protein Peptide N-myristoyltransferase, Uniprot P30419

Inhibition of CorA-Dependent Magnesium Homeostasis Is Cidal in Mycobacterium tuberculosis

Yumi Park, Yong-Mo Ahn, Surendranadha Reddy Jonnala, Sangmi Oh et autres

Mechanisms of magnesium homeostasis in Mycobacterium tuberculosis are poorly understood. Here, we describe the characterization of a pyrimidinetrione amide scaffold that disrupts magnesium homeostasis in the pathogen by direct binding to the CorA Mg 2+ /Co 2+ transporter. Mutations in domains of …

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2-Mercapto-Quinazolinones as Inhibitors of Type II NADH Dehydrogenase and Mycobacterium tuberculosis : Structure–Activity Relationships, Mechanism of Action and Absorption, Distribution, Metabolism, and Excretion Characterization

Dinakaran Murugesan, Peter C. Ray, Tracy Bayliss, Gareth A. Prosser et autres

Mycobacterium tuberculosis ( MTb) possesses two nonproton pumping type II NADH dehydrogenase (NDH-2) enzymes which are predicted to be jointly essential for respiratory metabolism. Furthermore, the structure of a closely related bacterial NDH-2 has been reported recently, allowing for the structure-based design …

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Design and Synthesis of Brain Penetrant Trypanocidal N -Myristoyltransferase Inhibitors

Tracy Bayliss, David Alexander Robinson, Victoria Smith, Stephen L. Brand et autres

N-Myristoyltransferase (NMT) represents a promising drug target within the parasitic protozoa Trypanosoma brucei (T. brucei), the causative agent for human African trypanosomiasis (HAT) or sleeping sickness. We have previously validated T. brucei NMT as a promising druggable target for the treatment of …

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Correction for Arora et al., “Respiratory Flexibility in Response to Inhibition of Cytochrome c Oxidase in Mycobacterium tuberculosis ”

Kriti Arora, Bernardo Ochoa‐Montaño, Patricia Siu‐Yee Tsang, Tom L. Blundell et autres

Volume 58, no. 11, p. 6962–6965, 2014, [https://doi.org/10.1128/AAC.03486-14][1]. Page 6963, left column, second paragraph: the following text in lines 5 to 10 should be deleted. “We deleted this oxidase in H37Rv by replacing a 221-bp MluI fragment in the cydABDC operon with …

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Essential but Not Vulnerable: Indazole Sulfonamides Targeting Inosine Monophosphate Dehydrogenase as Potential Leads againstMycobacterium tuberculosis

Yumi Park, Angela Pacitto, Tracy Bayliss, Laura A. T. Cleghorn et autres

A potent, noncytotoxic indazole sulfonamide was identified by high-throughput screening of >100,000 synthetic compounds for activity against Mycobacterium tuberculosis (Mtb). This noncytotoxic compound did not directly inhibit cell wall biogenesis but triggered a slow lysis of Mtb cells as measured by release …

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Respiratory Flexibility in Response to Inhibition of Cytochrome c Oxidase in Mycobacterium tuberculosis

Kriti Arora, Bernardo Ochoa‐Montaño, Patricia Siu‐Yee Tsang, Tom L. Blundell et autres

We report here a series of five chemically diverse scaffolds that have in vitro activities on replicating and hypoxic nonreplicating bacilli by targeting the respiratory bc1 complex in Mycobacterium tuberculosis in a strain-dependent manner. Deletion of the cytochrome bd oxidase generated a …

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