An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics

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...

Lead optimization of a pyrazole sulfonamide series of trypanosoma brucei N -myristoyltransferase inhibitors:Identification and evaluation of CNS penetrant compounds as potential treatments for stage 2 human african trypanosomiasis

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...

Synthesis and antitrypanosomal activities of novel pyridylchalcones.

Bhambra, AS
Ruparelia, KC
Tan, HL
Tasdemir, D
Burrell-Saward, H
Yardley, V
Beresford, KJ
Arroo, RR

January 2017

: A library of novel pyridylchalcones were synthesised and screened against Trypanosoma brucei rhode...

An evaluation of minor groove binders as anti-Trypanosoma brucei brucei therapeutics

Scott, Fraser J.
Khalaf, Abedawn I.
Giordani, Federica
Wong, Pui Ee
Duffy, Sandra
Barrett, Michael
Avery, Vicky M.
Suckling, Colin J.

June 2016

A series of 32 structurally diverse MGBs, derived from the natural product distamycin, was evaluated...

An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics

Scott, Fraser J.
Khalaf, Abedawn I.
Giordani, Federica
Wong, Pui Ee
Duffy, Sandra
Barrett, Michael
Avery, Vicky M.
Suckling, Colin J.

June 2016

AbstractA series of 32 structurally diverse MGBs, derived from the natural product distamycin, was e...

Minor groove binders for DNA as antitypanosomal agents : the veterinary context

Suckling, Colin J.
Scott, Fraser
Khalaf, Abedawn
Gillingwater, Kirsten
Morrison, Liam
de Koning, Harry
Barrett, Michael
Giordani, Federica

November 2017

Animal African trypanosomiasis (or nagana) is a wasting livestock disease found in sub-Saharan Afric...

Novel minor groove binders cure animal African trypanosomiasis in an in vivo mouse model

Giordani, Federica
Khalaf, Abedawn I.
Gillingwater, Kirsten
Munday, Jane C.
De Koning, Harry P.
Suckling, Colin J.
Barrett, Michael P.
Scott, Fraser J.

March 2019

Animal African trypanosomiasis (AAT) is a significant socioeconomic burden for sub-Saharan Africa be...

Novel Minor Groove Binders Cure Animal African Trypanosomiasis in an in Vivo Mouse Model

Federica Giordani (1330542)
Abedawn I. Khalaf (1304649)
Kirsten Gillingwater (349563)
Jane C. Munday (386690)
Harry P. de Koning (370318)
Colin J. Suckling (1268478)
Michael P. Barrett (167748)
Fraser J. Scott (1304628)

March 2019

Animal African trypanosomiasis (AAT) is a significant socioeconomic burden for sub-Saharan Africa be...

An evaluation of Minor Groove Binders as anti- Trypanosoma brucei brucei therapeutics

Scott, Fraser J.
Khalaf, Abedawn I.
Giordani, Federica
Wong, Pui Ee
Duffy, Sandra
Barrett, Michael
Avery, Vicky M.
Suckling, Colin J.

June 2016

A series of 32 structurally diverse MGBs, derived from the natural product distamycin, was evaluated...

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...

Activity of bisnaphthalimidopropyl derivatives against trypanosoma brucei

Loureiro, I
Thoo-Lin, P
Ramos, I
Roura, M
Pruvost, A
Pemberton, I
Loukil, H
MacDougall, J
Tavares, J
Cordeiro-da-Silva, A
Graça, NA
Gaspar, L
Costa, DM

January 2016

Current treatments for African trypanosomiasis are either toxic, costly, difficult to administer, or...

Novel minor groove binders cure animal african trypanosomiasis in an in vivo mouse model

GIordani, F.
Khalaf, A. I.
Gillingwater, K.
Munday, J. C.
De Koning, H. P.
Suckling, C. J.
Barrett, M. P.
Scott, F. J.

January 2019

Animal African trypanosomiasis (AAT) is a significant socioeconomic burden for sub-Saharan Africa be...

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...

Inhibitors of human histone deacetylase with potent activity against the African trypanosome Trypanosoma brucei

Kelly, John M.
Taylor, Martin C.
Horn, David
Loza, Einars
Kalvinsh, Ivars
Björkling, Fredrik

March 2012

AbstractA number of hydroxamic acid derivatives which inhibit human histone deacetylases were invest...

Functional and structural analysis of AT-specific minor groove binders that disrupt DNA-protein interactions and cause disintegration of the Trypanosoma brucei kinetoplast

Millan, Cinthia R.
Acosta-Reyes, Francisco J.
Lagartera, Laura
Ebiloma, Godwin U.
Lemgruber Soares, Leandro
Nué Martinez, J. Jonathan
Saperas, Núria
Dardonville, Christophe
De Koning, Harry P.
Campos, J. Lourdes

August 2017

Trypanosoma brucei, the causative agent of sleeping sickness (Human African Trypanosomiasis, HAT), c...

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...

Lead optimization of a pyrazole sulfonamide series of trypanosoma brucei N -myristoyltransferase inhibitors:Identification and evaluation of CNS penetrant compounds as potential treatments for stage 2 human african trypanosomiasis

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...

Synthesis and antitrypanosomal activities of novel pyridylchalcones.

Bhambra, AS
Ruparelia, KC
Tan, HL
Tasdemir, D
Burrell-Saward, H
Yardley, V
Beresford, KJ
Arroo, RR

January 2017

: A library of novel pyridylchalcones were synthesised and screened against Trypanosoma brucei rhode...

An evaluation of minor groove binders as anti-Trypanosoma brucei brucei therapeutics

Scott, Fraser J.
Khalaf, Abedawn I.
Giordani, Federica
Wong, Pui Ee
Duffy, Sandra
Barrett, Michael
Avery, Vicky M.
Suckling, Colin J.

June 2016

A series of 32 structurally diverse MGBs, derived from the natural product distamycin, was evaluated...

An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics

Scott, Fraser J.
Khalaf, Abedawn I.
Giordani, Federica
Wong, Pui Ee
Duffy, Sandra
Barrett, Michael
Avery, Vicky M.
Suckling, Colin J.

June 2016

AbstractA series of 32 structurally diverse MGBs, derived from the natural product distamycin, was e...

Minor groove binders for DNA as antitypanosomal agents : the veterinary context

Suckling, Colin J.
Scott, Fraser
Khalaf, Abedawn
Gillingwater, Kirsten
Morrison, Liam
de Koning, Harry
Barrett, Michael
Giordani, Federica

November 2017

Animal African trypanosomiasis (or nagana) is a wasting livestock disease found in sub-Saharan Afric...

Novel minor groove binders cure animal African trypanosomiasis in an in vivo mouse model

Giordani, Federica
Khalaf, Abedawn I.
Gillingwater, Kirsten
Munday, Jane C.
De Koning, Harry P.
Suckling, Colin J.
Barrett, Michael P.
Scott, Fraser J.

March 2019

Animal African trypanosomiasis (AAT) is a significant socioeconomic burden for sub-Saharan Africa be...

Novel Minor Groove Binders Cure Animal African Trypanosomiasis in an in Vivo Mouse Model

Federica Giordani (1330542)
Abedawn I. Khalaf (1304649)
Kirsten Gillingwater (349563)
Jane C. Munday (386690)
Harry P. de Koning (370318)
Colin J. Suckling (1268478)
Michael P. Barrett (167748)
Fraser J. Scott (1304628)

March 2019

Animal African trypanosomiasis (AAT) is a significant socioeconomic burden for sub-Saharan Africa be...

An evaluation of Minor Groove Binders as anti- Trypanosoma brucei brucei therapeutics

Scott, Fraser J.
Khalaf, Abedawn I.
Giordani, Federica
Wong, Pui Ee
Duffy, Sandra
Barrett, Michael
Avery, Vicky M.
Suckling, Colin J.

June 2016

A series of 32 structurally diverse MGBs, derived from the natural product distamycin, was evaluated...

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...

Activity of bisnaphthalimidopropyl derivatives against trypanosoma brucei

Loureiro, I
Thoo-Lin, P
Ramos, I
Roura, M
Pruvost, A
Pemberton, I
Loukil, H
MacDougall, J
Tavares, J
Cordeiro-da-Silva, A
Graça, NA
Gaspar, L
Costa, DM

January 2016

Current treatments for African trypanosomiasis are either toxic, costly, difficult to administer, or...

Novel minor groove binders cure animal african trypanosomiasis in an in vivo mouse model

GIordani, F.
Khalaf, A. I.
Gillingwater, K.
Munday, J. C.
De Koning, H. P.
Suckling, C. J.
Barrett, M. P.
Scott, F. J.

January 2019

Animal African trypanosomiasis (AAT) is a significant socioeconomic burden for sub-Saharan Africa be...

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...

Inhibitors of human histone deacetylase with potent activity against the African trypanosome Trypanosoma brucei

Kelly, John M.
Taylor, Martin C.
Horn, David
Loza, Einars
Kalvinsh, Ivars
Björkling, Fredrik

March 2012

AbstractA number of hydroxamic acid derivatives which inhibit human histone deacetylases were invest...

Functional and structural analysis of AT-specific minor groove binders that disrupt DNA-protein interactions and cause disintegration of the Trypanosoma brucei kinetoplast

Millan, Cinthia R.
Acosta-Reyes, Francisco J.
Lagartera, Laura
Ebiloma, Godwin U.
Lemgruber Soares, Leandro
Nué Martinez, J. Jonathan
Saperas, Núria
Dardonville, Christophe
De Koning, Harry P.
Campos, J. Lourdes

August 2017

Trypanosoma brucei, the causative agent of sleeping sickness (Human African Trypanosomiasis, HAT), c...

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...

Lead optimization of a pyrazole sulfonamide series of trypanosoma brucei N -myristoyltransferase inhibitors:Identification and evaluation of CNS penetrant compounds as potential treatments for stage 2 human african trypanosomiasis

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...

Synthesis and antitrypanosomal activities of novel pyridylchalcones.

Bhambra, AS
Ruparelia, KC
Tan, HL
Tasdemir, D
Burrell-Saward, H
Yardley, V
Beresford, KJ
Arroo, RR

January 2017

: A library of novel pyridylchalcones were synthesised and screened against Trypanosoma brucei rhode...

An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics

Abstract

Extracted data

An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics

Abstract

Extracted data

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