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Literature DB >> 26787697

The Investigational Fungal Cyp51 Inhibitor VT-1129 Demonstrates Potent In Vitro Activity against Cryptococcus neoformans and Cryptococcus gattii.

Shawn R Lockhart¹, Annette W Fothergill², Naureen Iqbal¹, Carol B Bolden¹, Nina T Grossman¹, Edward P Garvey³, Stephen R Brand³, William J Hoekstra³, Robert J Schotzinger³, Elizabeth Ottinger⁴, Thomas F Patterson⁵, Nathan P Wiederhold⁶.

Abstract

Thein vitroactivities of the novel fungal Cyp51 inhibitor VT-1129 were evaluated against a large panel ofCryptococcus neoformansandCryptococcus gattiiisolates. VT-1129 demonstrated potent activities against bothCryptococcusspecies as demonstrated by low MIC50and MIC90values. ForC. gattii, thein vitropotency was maintained against all genotypes. In addition, significantly lower geometric mean MICs were observed for VT-1129 than for fluconazole againstC. neoformans, including isolates with reduced fluconazole susceptibility.

Entities: Chemical Species

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Year: 2016 PMID： 26787697 PMCID： PMC4808209 DOI： 10.1128/AAC.02770-15

Source DB: PubMed Journal: Antimicrob Agents Chemother ISSN： 0066-4804 Impact factor: 5.191

16 in total

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5. Antifungal susceptibilities among different serotypes of Cryptococcus gattii and Cryptococcus neoformans.

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8. Evaluation of Etest method for determining isavuconazole MICs against Cryptococcus gattii and Cryptococcus neoformans.

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Review 9. Consensus multi-locus sequence typing scheme for Cryptococcus neoformans and Cryptococcus gattii.

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10. The clinical candidate VT-1161 is a highly potent inhibitor of Candida albicans CYP51 but fails to bind the human enzyme.

Authors: A G S Warrilow; C M Hull; J E Parker; E P Garvey; W J Hoekstra; W R Moore; R J Schotzinger; D E Kelly; S L Kelly
Journal: Antimicrob Agents Chemother Date: 2014-09-15 Impact factor: 5.191

25 in total

1. Azole Resistance Reduces Susceptibility to the Tetrazole Antifungal VT-1161.

Authors: Brian C Monk; Mikhail V Keniya; Manya Sabherwal; Rajni K Wilson; Danyon O Graham; Harith F Hassan; Danni Chen; Joel D A Tyndall
Journal: Antimicrob Agents Chemother Date: 2018-12-21 Impact factor: 5.191

2. Successful Aspects of the Coadministration of Sterol 14α-Demethylase Inhibitor VFV and Benznidazole in Experimental Mouse Models of Chagas Disease Caused by the Drug-Resistant Strain of Trypanosoma cruzi.

Authors: Francisca Hildemagna Guedes-da-Silva; Denise da Gama Jaén Batista; Cristiane França Da Silva; Beatriz Philot Pavão; Marcos Meuser Batista; Otacílio Cruz Moreira; Letícia Rocha Quintino Souza; Constança Britto; Girish Rachakonda; Fernando Villalta; Galina I Lepesheva; Maria de Nazaré Correia Soeiro
Journal: ACS Infect Dis Date: 2019-01-23 Impact factor: 5.084

3. The Investigational Drug VT-1129 Is a Highly Potent Inhibitor of Cryptococcus Species CYP51 but Only Weakly Inhibits the Human Enzyme.

Authors: Andrew G S Warrilow; Josie E Parker; Claire L Price; W David Nes; Edward P Garvey; William J Hoekstra; Robert J Schotzinger; Diane E Kelly; Steven L Kelly
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Review 4. The antifungal pipeline: a reality check.

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Review 6. Molecular and genetic basis of azole antifungal resistance in the opportunistic pathogenic fungus Candida albicans.

Authors: Andrew T Nishimoto; Cheshta Sharma; P David Rogers
Journal: J Antimicrob Chemother Date: 2020-02-01 Impact factor: 5.790

7. The Fungal Cyp51 Inhibitor VT-1129 Is Efficacious in an Experimental Model of Cryptococcal Meningitis.

Authors: Nathan P Wiederhold; Laura K Najvar; Edward P Garvey; Stephen R Brand; Xin Xu; Elizabeth A Ottinger; Asaf Alimardanov; Jim Cradock; Mark Behnke; William J Hoekstra; Robert J Schotzinger; Rosie Jaramillo; Marcos Olivo; William R Kirkpatrick; Thomas F Patterson
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8. Heterologous Expression of Full-Length Lanosterol 14α-Demethylases of Prominent Fungal Pathogens Candida albicans and Candida glabrata Provides Tools for Antifungal Discovery.

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9. Crystal Structure of the New Investigational Drug Candidate VT-1598 in Complex with Aspergillus fumigatus Sterol 14α-Demethylase Provides Insights into Its Broad-Spectrum Antifungal Activity.

Authors: Tatiana Y Hargrove; Edward P Garvey; William J Hoekstra; Christopher M Yates; Zdzislaw Wawrzak; Girish Rachakonda; Fernando Villalta; Galina I Lepesheva
Journal: Antimicrob Agents Chemother Date: 2017-06-27 Impact factor: 5.191

10. New Triazole NT-a9 Has Potent Antifungal Efficacy against Cryptococcus neoformans In Vitro and In Vivo.

Authors: Ren-Yi Lu; Ting-Jun-Hong Ni; Jing Wu; Lan Yan; Quan-Zhen Lv; Li-Ping Li; Da-Zhi Zhang; Yuan-Ying Jiang
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