Identification and Characterization of FTY720 for the Treatment of Human African Trypanosomiasis

Jones, Amy
Kaiser, Marcel
Avery, Vicky

Open PDF

Open link

Publication date

January 2016

DOI

10.1128/AAC.02116-15

Publisher

American Society for Microbiology

Journal

Antimicrobial Agents and Chemotherapy

Abstract

The screening of a focused library identified FTY720 (Fingolimod; Gilenya) as a potent selective antitrypanosomal compound active against Trypanosoma brucei gambiense and T. brucei rhodesiense, the causative agents of human African trypanosomiasis (HAT). This is the first report of trypanocidal activity for FTY720, an oral drug registered for the treatment of relapsing multiple sclerosis, and the characterization of sphingolipids as a potential new class of compounds for HAT.Griffith Sciences, Griffith Institute for Drug DiscoveryFull Tex

Extracted data

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Identification and Characterization of FTY720 for the Treatment of Human African Trypanosomiasis

Jones, Amy
Kaiser, Marcel
Avery, Vicky

Open PDF

Open link

Publication date

January 2016

DOI

10.1128/AAC.02116-15

Publisher

American Society for Microbiology

Journal

Antimicrobial Agents and Chemotherapy

Abstract

Extracted data

Brand, Stephen
Norcross, Neil R.
Thompson, Stephen
Harrison, Justin R.
Smith, Victoria C.
Robinson, David A.
Torrie, Leah S.
McElroy, Stuart P.
Hallyburton, Irene
Norval, Suzanne
Scullion, Paul
Stojanovski, Laste
Simeons, Frederick R.C.
Van Aalten, Daan
Frearson, Julie A.
Brenk, Ruth
Fairlamb, Alan H.
Ferguson, Michael A.J.
Wyatt, Paul G.
Gilbert, Ian H.
Read, Kevin D.

December 2014

Trypanosoma brucei N-myristoyltransferase (TbNMT) is an attractive therapeutic target for the treatm...

Discovery of a Novel Class of Orally Active Trypanocidal N-Myristoyltransferase Inhibitors

Brand, Stephen
Cleghorn, Laura A. T.
McElroy, Stuart P.
Robinson, David A.
Smith, Victoria C.
Hallyburton, Irene
Harrison, Justin R.
Norcross, Neil R.
Spinks, Daniel
Bayliss, Tracy
Norval, Suzanne
Stojanovski, Laste
Torrie, Leah S.
Frearson, Julie A.
Brenk, Ruth
Fairlamb, Alan H.
Ferguson, Michael A. J.
Read, Kevin D.
Wyatt, Paul G.
Gilbert, Ian H.

January 2012

N-Myristoyltransferase (NMT) represents a promising drug target for human African trypanosomiasis (H...

Identification and characterization of FTY720 for the treatment of human African trypanosomiasis

Jones, Amy J.
Kaiser, Marcel
Avery, Vicky M.

January 2015

The screening of a focused library identified FTY720 (Fingolimod; Gilenya) as a potent selective ant...

Development of Novel Anti-Trypanosomal Compounds via Computational, In Vitro and In Vivo Methods

ADLER, NIKOLETTA

January 2018

Human African Trypanosomiasis is a neglected parasitic disease caused by Trypanosoma brucei, which i...

Development of a 2,4-diaminothiazole series for the treatment of human African trypanosomiasis highlights the importance of static-cidal screening of analogues

Cleghorn, Laura A. T.
Wall, Richard J.
Albrecht, Sébastien
MacGowan, Stuart A.
Norval, Suzanne
De Rycker, Manu
Woodland, Andrew
Spinks, Daniel
Thompson, Stephen
Patterson, Stephen
Corpas Lopez, Victoriano
Dey, Gourav
Collie, Iain T.
Hallyburton, Irene
Kime, Robert
Simeons, Frederick R. C.
Stojanovski, Laste
Frearson, Julie A.
Wyatt, Paul G.
Read, Kevin D.
Gilbert, Ian H.
Wyllie, Susan

July 2023

While treatment options for human African trypanosomiasis (HAT) have improved significantly, there i...

Development of a 2,4-diaminothiazole series for the treatment of human African trypanosomiasis highlights the importance of static-cidal screening of analogues

Cleghorn, Laura A. T.
Wall, Richard J.
Albrecht, Sébastien
MacGowan, Stuart A.
Norval, Suzanne
De Rycker, Manu
Woodland, Andrew
Spinks, Daniel
Thompson, Stephen
Patterson, Stephen
Corpas Lopez, Victoriano
Dey, Gourav
Collie, Iain T.
Hallyburton, Irene
Kime, Robert
Simeons, Frederick R. C.
Stojanovski, Laste
Frearson, Julie A.
Wyatt, Paul G.
Read, Kevin D.
Gilbert, Ian H.
Wyllie, Susan

July 2023

While treatment options for human African trypanosomiasis (HAT) have improved significantly, there i...

Development of a 2,4-diaminothiazole series for the treatment of human African trypanosomiasis highlights the importance of static-cidal screening of analogues

Cleghorn, Laura A. T.
Wall, Richard J.
Albrecht, Sébastien
MacGowan, Stuart A.
Norval, Suzanne
De Rycker, Manu
Woodland, Andrew
Spinks, Daniel
Thompson, Stephen
Patterson, Stephen
Corpas Lopez, Victoriano
Dey, Gourav
Collie, Iain T.
Hallyburton, Irene
Kime, Robert
Simeons, Frederick R. C.
Stojanovski, Laste
Frearson, Julie A.
Wyatt, Paul G.
Read, Kevin D.
Gilbert, Ian H.
Wyllie, Susan

July 2023

While treatment options for human African trypanosomiasis (HAT) have improved significantly, there i...

Identification of compounds with anti-proliferative activity against Trypanosoma brucei brucei strain 427 by a whole cell viability based HTS campaign

Sykes, Melissa L
Baell, Jonathan Bayldon
Kaiser, Marcel
Chatelain, Eric
Moawad, Sarah R
Ganame, Danny
Ioset, Jean Robert
Avery, Vicky M

January 2012

Human African Trypanosomiasis (HAT) is caused by two trypanosome sub-species, Trypanosoma brucei rho...

Lead Optimization of 3,5-Disubstituted-7-Azaindoles for the Treatment of Human African Trypanosomiasis

Klug, DM
Mavrogiannaki, EM
Forbes, KC
Silva, L
Diaz-Gonzalez, R
Pérez-Moreno, G
Ceballos-Pérez, G
Garcia-Hernández, R
Bosch-Navarrete, C
Cordón-Obras, C
Gómez-Liñán, C
Saura, A
Momper, JD
Martinez-Martinez, MS
Manzano, P
Syed, A
El-Sakkary, N
Caffrey, CR
Gamarro, F
Ruiz-Perez, LM
Gonzalez Pacanowska, D
Ferrins, L
Navarro, M
Pollastri, MP

July 2021

Neglected tropical diseases such as human African trypanosomiasis (HAT) are prevalent primarily in t...

Identification of compounds with anti-proliferative activity against Trypanosoma brucei brucei strain 427 by a whole cell viability based HTS campaign

Sykes, Melissa L
Baell, Jonathan Bayldon
Kaiser, Marcel
Chatelain, Eric
Moawad, Sarah R
Ganame, Danny
Ioset, Jean Robert
Avery, Vicky M

January 2012

Human African Trypanosomiasis (HAT) is caused by two trypanosome sub-species, Trypanosoma brucei rho...

Identification of compounds with anti-proliferative activity against Trypanosoma brucei brucei strain 427 by a whole cell viability based HTS campaign. PLoS Neglected Tropical Diseases 6

Melissa L. Sykes
Jonathan B. Baell
Marcel Kaiser
Eric Chatelain
Sarah R. Moawad
Danny Ganame
Jean-robert Ioset
Vicky M. Avery

January 2012

Human African Trypanosomiasis (HAT) is caused by two trypanosome sub-species, Trypanosoma brucei rho...

Discovery of a Novel Class of Orally Active Trypanocidal N-Myristoyltransferase Inhibitors

Brand, Stephen
Cleghorn, Laura A. T.
McElroy, Stuart P.
Robinson, David A.
Smith, Victoria C.
Hallyburton, Irene
Harrison, Justin R.
Norcross, Neil R.
Spinks, Daniel
Bayliss, Tracy
Norval, Suzanne
Stojanovski, Laste
Torrie, Leah S.
Frearson, Julie A.
Brenk, Ruth
Fairlamb, Alan H.
Ferguson, Michael A. J.
Read, Kevin D.
Wyatt, Paul G.
Gilbert, Ian H.

January 2012

N-Myristoyltransferase (NMT) represents a promising drug target for human African trypanosomiasis (H...

Discovery of a Novel Class of Orally Active Trypanocidal N-Myristoyltransferase Inhibitors

Brand, Stephen
Cleghorn, Laura A. T.
McElroy, Stuart P.
Robinson, David A.
Smith, Victoria C.
Hallyburton, Irene
Harrison, Justin R.
Norcross, Neil R.
Spinks, Daniel
Bayliss, Tracy
Norval, Suzanne
Stojanovski, Laste
Torrie, Leah S.
Frearson, Julie A.
Brenk, Ruth
Fairlamb, Alan H.
Ferguson, Michael A. J.
Read, Kevin D.
Wyatt, Paul G.
Gilbert, Ian H.

January 2012

N-Myristoyltransferase (NMT) represents a promising drug target for human African trypanosomiasis (H...

Brand, Stephen
Norcross, Neil R.
Thompson, Stephen
Harrison, Justin R.
Smith, Victoria C.
Robinson, David A.
Torrie, Leah S.
McElroy, Stuart P.
Hallyburton, Irene
Norval, Suzanne
Scullion, Paul
Stojanovski, Laste
Simeons, Frederick R.C.
Van Aalten, Daan
Frearson, Julie A.
Brenk, Ruth
Fairlamb, Alan H.
Ferguson, Michael A.J.
Wyatt, Paul G.
Gilbert, Ian H.
Read, Kevin D.

December 2014

Trypanosoma brucei N-myristoyltransferase (TbNMT) is an attractive therapeutic target for the treatm...

Discovery of a Novel Class of Orally Active Trypanocidal N-Myristoyltransferase Inhibitors

Brand, Stephen
Cleghorn, Laura A. T.
McElroy, Stuart P.
Robinson, David A.
Smith, Victoria C.
Hallyburton, Irene
Harrison, Justin R.
Norcross, Neil R.
Spinks, Daniel
Bayliss, Tracy
Norval, Suzanne
Stojanovski, Laste
Torrie, Leah S.
Frearson, Julie A.
Brenk, Ruth
Fairlamb, Alan H.
Ferguson, Michael A. J.
Read, Kevin D.
Wyatt, Paul G.
Gilbert, Ian H.

January 2012

N-Myristoyltransferase (NMT) represents a promising drug target for human African trypanosomiasis (H...

Development of a 2,4-diaminothiazole series for the treatment of human African trypanosomiasis highlights the importance of static-cidal screening of analogues

Cleghorn, Laura A. T.
Wall, Richard J.
Albrecht, Sébastien
MacGowan, Stuart A.
Norval, Suzanne
De Rycker, Manu
Woodland, Andrew
Spinks, Daniel
Thompson, Stephen
Patterson, Stephen
Corpas Lopez, Victoriano
Dey, Gourav
Collie, Iain T.
Hallyburton, Irene
Kime, Robert
Simeons, Frederick R. C.
Stojanovski, Laste
Frearson, Julie A.
Wyatt, Paul G.
Read, Kevin D.
Gilbert, Ian H.
Wyllie, Susan

July 2023

While treatment options for human African trypanosomiasis (HAT) have improved significantly, there i...

Development of a 2,4-diaminothiazole series for the treatment of human African trypanosomiasis highlights the importance of static-cidal screening of analogues

Cleghorn, Laura A. T.
Wall, Richard J.
Albrecht, Sébastien
MacGowan, Stuart A.
Norval, Suzanne
De Rycker, Manu
Woodland, Andrew
Spinks, Daniel
Thompson, Stephen
Patterson, Stephen
Corpas Lopez, Victoriano
Dey, Gourav
Collie, Iain T.
Hallyburton, Irene
Kime, Robert
Simeons, Frederick R. C.
Stojanovski, Laste
Frearson, Julie A.
Wyatt, Paul G.
Read, Kevin D.
Gilbert, Ian H.
Wyllie, Susan

July 2023

While treatment options for human African trypanosomiasis (HAT) have improved significantly, there i...

Development of a 2,4-diaminothiazole series for the treatment of human African trypanosomiasis highlights the importance of static-cidal screening of analogues

Cleghorn, Laura A. T.
Wall, Richard J.
Albrecht, Sébastien
MacGowan, Stuart A.
Norval, Suzanne
De Rycker, Manu
Woodland, Andrew
Spinks, Daniel
Thompson, Stephen
Patterson, Stephen
Corpas Lopez, Victoriano
Dey, Gourav
Collie, Iain T.
Hallyburton, Irene
Kime, Robert
Simeons, Frederick R. C.
Stojanovski, Laste
Frearson, Julie A.
Wyatt, Paul G.
Read, Kevin D.
Gilbert, Ian H.
Wyllie, Susan

July 2023

While treatment options for human African trypanosomiasis (HAT) have improved significantly, there i...

Identification of compounds with anti-proliferative activity against Trypanosoma brucei brucei strain 427 by a whole cell viability based HTS campaign

Sykes, Melissa L
Baell, Jonathan Bayldon
Kaiser, Marcel
Chatelain, Eric
Moawad, Sarah R
Ganame, Danny
Ioset, Jean Robert
Avery, Vicky M

January 2012

Human African Trypanosomiasis (HAT) is caused by two trypanosome sub-species, Trypanosoma brucei rho...

Lead Optimization of 3,5-Disubstituted-7-Azaindoles for the Treatment of Human African Trypanosomiasis

Klug, DM
Mavrogiannaki, EM
Forbes, KC
Silva, L
Diaz-Gonzalez, R
Pérez-Moreno, G
Ceballos-Pérez, G
Garcia-Hernández, R
Bosch-Navarrete, C
Cordón-Obras, C
Gómez-Liñán, C
Saura, A
Momper, JD
Martinez-Martinez, MS
Manzano, P
Syed, A
El-Sakkary, N
Caffrey, CR
Gamarro, F
Ruiz-Perez, LM
Gonzalez Pacanowska, D
Ferrins, L
Navarro, M
Pollastri, MP

July 2021

Neglected tropical diseases such as human African trypanosomiasis (HAT) are prevalent primarily in t...

Identification of compounds with anti-proliferative activity against Trypanosoma brucei brucei strain 427 by a whole cell viability based HTS campaign

Sykes, Melissa L
Baell, Jonathan Bayldon
Kaiser, Marcel
Chatelain, Eric
Moawad, Sarah R
Ganame, Danny
Ioset, Jean Robert
Avery, Vicky M

January 2012

Human African Trypanosomiasis (HAT) is caused by two trypanosome sub-species, Trypanosoma brucei rho...

Identification of compounds with anti-proliferative activity against Trypanosoma brucei brucei strain 427 by a whole cell viability based HTS campaign. PLoS Neglected Tropical Diseases 6

Melissa L. Sykes
Jonathan B. Baell
Marcel Kaiser
Eric Chatelain
Sarah R. Moawad
Danny Ganame
Jean-robert Ioset
Vicky M. Avery

January 2012

Human African Trypanosomiasis (HAT) is caused by two trypanosome sub-species, Trypanosoma brucei rho...

Discovery of a Novel Class of Orally Active Trypanocidal N-Myristoyltransferase Inhibitors

Brand, Stephen
Cleghorn, Laura A. T.
McElroy, Stuart P.
Robinson, David A.
Smith, Victoria C.
Hallyburton, Irene
Harrison, Justin R.
Norcross, Neil R.
Spinks, Daniel
Bayliss, Tracy
Norval, Suzanne
Stojanovski, Laste
Torrie, Leah S.
Frearson, Julie A.
Brenk, Ruth
Fairlamb, Alan H.
Ferguson, Michael A. J.
Read, Kevin D.
Wyatt, Paul G.
Gilbert, Ian H.

January 2012

N-Myristoyltransferase (NMT) represents a promising drug target for human African trypanosomiasis (H...

Discovery of a Novel Class of Orally Active Trypanocidal N-Myristoyltransferase Inhibitors

Brand, Stephen
Cleghorn, Laura A. T.
McElroy, Stuart P.
Robinson, David A.
Smith, Victoria C.
Hallyburton, Irene
Harrison, Justin R.
Norcross, Neil R.
Spinks, Daniel
Bayliss, Tracy
Norval, Suzanne
Stojanovski, Laste
Torrie, Leah S.
Frearson, Julie A.
Brenk, Ruth
Fairlamb, Alan H.
Ferguson, Michael A. J.
Read, Kevin D.
Wyatt, Paul G.
Gilbert, Ian H.

January 2012

N-Myristoyltransferase (NMT) represents a promising drug target for human African trypanosomiasis (H...

Brand, Stephen
Norcross, Neil R.
Thompson, Stephen
Harrison, Justin R.
Smith, Victoria C.
Robinson, David A.
Torrie, Leah S.
McElroy, Stuart P.
Hallyburton, Irene
Norval, Suzanne
Scullion, Paul
Stojanovski, Laste
Simeons, Frederick R.C.
Van Aalten, Daan
Frearson, Julie A.
Brenk, Ruth
Fairlamb, Alan H.
Ferguson, Michael A.J.
Wyatt, Paul G.
Gilbert, Ian H.
Read, Kevin D.

December 2014

Trypanosoma brucei N-myristoyltransferase (TbNMT) is an attractive therapeutic target for the treatm...

Discovery of a Novel Class of Orally Active Trypanocidal N-Myristoyltransferase Inhibitors

Brand, Stephen
Cleghorn, Laura A. T.
McElroy, Stuart P.
Robinson, David A.
Smith, Victoria C.
Hallyburton, Irene
Harrison, Justin R.
Norcross, Neil R.
Spinks, Daniel
Bayliss, Tracy
Norval, Suzanne
Stojanovski, Laste
Torrie, Leah S.
Frearson, Julie A.
Brenk, Ruth
Fairlamb, Alan H.
Ferguson, Michael A. J.
Read, Kevin D.
Wyatt, Paul G.
Gilbert, Ian H.

January 2012

N-Myristoyltransferase (NMT) represents a promising drug target for human African trypanosomiasis (H...

Identification and Characterization of FTY720 for the Treatment of Human African Trypanosomiasis

Abstract

Extracted data

Identification and Characterization of FTY720 for the Treatment of Human African Trypanosomiasis

Abstract

Extracted data

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