The quest for the holy grail: new antitubercular chemical entities, targets and strategies

被引:50
作者
Huszar, Stanislav [1 ]
Chibale, Kelly [1 ,2 ,3 ]
Singh, Vinayak [1 ,2 ,3 ]
机构
[1] Univ Cape Town, Drug Discovery & Dev Ctr H3D, ZA-7701 Rondebosch, South Africa
[2] Univ Cape Town, South African Med Res Council, Drug Discovery & Dev Res Unit, Dept Chem, ZA-7701 Rondebosch, South Africa
[3] Univ Cape Town, Inst Infect Dis & Mol Med, ZA-7701 Rondebosch, South Africa
基金
英国医学研究理事会;
关键词
KILL MYCOBACTERIUM-TUBERCULOSIS; CELL-WALL CORE; DRUG TARGET; INHIBITION; BIOSYNTHESIS; ETHIONAMIDE; THERAPY; IDENTIFICATION; SPECTINAMIDES; ACTIVATION;
D O I
10.1016/j.drudis.2020.02.003
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Tuberculosis (TB) remains the leading cause of death from an infectious disease worldwide. TB therapy is complicated by the protracted treatment regimens, development of resistance coupled with toxicity and insufficient sterilizing capacity of current drugs. Although considerable progress has been made on establishing a TB drug pipeline, the high attrition rate reinforces the need to continually replenish the pipeline with high-quality leads that act through inhibition of novel targets. In this review, we highlight some of the key advances that have assisted TB drug discovery with novel chemical matter, targets and strategies - to fuel the TB drug pipeline.
引用
收藏
页码:772 / 780
页数:9
相关论文
共 65 条
[1]   Identification of KasA as the cellular target of an anti-tubercular scaffold [J].
Abrahams, Katherine A. ;
Chung, Chun-wa ;
Ghidelli-Disse, Sonja ;
Rullas, Joaquin ;
Jose Rebollo-Lopez, Maria ;
Gurcha, Sudagar S. ;
Cox, Jonathan A. G. ;
Mendoza, Alfonso ;
Jimenez-Navarro, Elena ;
Santos Martinez-Martinez, Maria ;
Neu, Margarete ;
Shillings, Anthony ;
Homes, Paul ;
Argyrou, Argyrides ;
Casanueva, Ruth ;
Loman, Nicholas J. ;
Moynihan, Patrick J. ;
Lelievre, Joel ;
Selenski, Carolyn ;
Axtman, Matthew ;
Kremer, Laurent ;
Bantscheff, Marcus ;
Angulo-Barturen, Inigo ;
Cacho Izquierdo, Monica ;
Cammack, Nicholas C. ;
Drewes, Gerard ;
Ballell, Lluis ;
Barros, David ;
Besra, Gurdyal S. ;
Bates, Robert H. .
NATURE COMMUNICATIONS, 2016, 7
[2]   Development of a Novel Lead that Targets M. tuberculosis Polyketide Synthase 13 [J].
Aggarwal, Anup ;
Parai, Maloy K. ;
Shetty, Nishant ;
Wallis, Deeann ;
Woolhiser, Lisa ;
Hastings, Courtney ;
Dutta, Noton K. ;
Galaviz, Stacy ;
Dhakal, Ramesh C. ;
Shrestha, Rupesh ;
Wakabayashi, Shoko ;
Walpole, Chris ;
Matthews, David ;
Floyd, David ;
Scullion, Paul ;
Riley, Jennifer ;
Epemolu, Ola ;
Norval, Suzanne ;
Snavely, Thomas ;
Robertson, Gregory T. ;
Rubin, Eric J. ;
Ioerger, Thomas R. ;
Sirgel, Frik A. ;
van der Merwe, Ruben ;
van Helden, Paul D. ;
Keller, Peter ;
Bottger, Erik C. ;
Karakousis, Petros C. ;
Lenaerts, Anne J. ;
Sacchettini, James C. .
CELL, 2017, 170 (02) :249-+
[3]  
[Anonymous], SCIENCE
[4]   Opposing reactions in coenzyme A metabolism sensitize Mycobacterium tuberculosis to enzyme inhibition [J].
Ballinger, Elaine ;
Mosior, John ;
Hartman, Travis ;
Burns-Huang, Kristin ;
Gold, Ben ;
Morris, Roxanne ;
Goullieux, Laurent ;
Blanc, Isabelle ;
Vaubourgeix, Julien ;
Lagrange, Sophie ;
Fraisse, Laurent ;
Sans, Stephanie ;
Couturier, Cedric ;
Bacque, Eric ;
Rhee, Kyu ;
Scarry, Sarah M. ;
Aube, Jeffrey ;
Yang, Guangbin ;
Ouerfelli, Ouathek ;
Schnappinger, Dirk ;
Ioerger, Thomas R. ;
Engelhart, Curtis A. ;
McConnell, Jennifer A. ;
McAulay, Kathrine ;
Fay, Allison ;
Roubert, Christine ;
Sacchettini, James ;
Nathan, Carl .
SCIENCE, 2019, 363 (6426) :498-+
[5]   INHA, A GENE ENCODING A TARGET FOR ISONIAZID AND ETHIONAMIDE IN MYCOBACTERIUM-TUBERCULOSIS [J].
BANERJEE, A ;
DUBNAU, E ;
QUEMARD, A ;
BALASUBRAMANIAN, V ;
UM, KS ;
WILSON, T ;
COLLINS, D ;
DELISLE, G ;
JACOBS, WR .
SCIENCE, 1994, 263 (5144) :227-230
[6]  
Baulard AR, 2000, J BIOL CHEM, V275, P28326
[7]   Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420 [J].
Blondiaux, Nicolas ;
Moune, Martin ;
Desroses, Matthieu ;
Frita, Rosangela ;
Flipo, Marion ;
Mathys, Vanessa ;
Soetaert, Karine ;
Kiass, Mehdi ;
Delorme, Vincent ;
Djaout, Kamel ;
Trebosc, Vincent ;
Kemmer, Christian ;
Wintjens, Rene ;
Wohlkonig, Alexandre ;
Antoine, Rudy ;
Huot, Ludovic ;
Hot, David ;
Coscolla, Mireia ;
Feldmann, Julia ;
Gagneux, Sebastien ;
Locht, Camille ;
Brodin, Priscille ;
Gitzinger, Marc ;
Deprez, Benoit ;
Willand, Nicolas ;
Baulard, Alain R. .
SCIENCE, 2017, 355 (6330) :1206-1211
[8]   DprE1 Is a Vulnerable Tuberculosis Drug Target Due to Its Cell Wall Localization [J].
Brecik, Miroslav ;
Centarova, Ivana ;
Mukherjee, Raju ;
Kolly, Gaelle S. ;
Huszar, Stanislav ;
Bobovska, Adela ;
Kilacskova, Emoeke ;
Mokosova, Veronika ;
Svetlikova, Zuzana ;
Sarkan, Michal ;
Neres, Joao ;
Kordulakova, Jana ;
Cole, Stewart T. ;
Mikusova, Katarina .
ACS CHEMICAL BIOLOGY, 2015, 10 (07) :1631-1636
[9]  
Choules MP, 2019, ANTIMICROB AGENTS CH, V63, DOI [10.1128/aac.02204-18, 10.1128/AAC.02204-18]
[10]   Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB [J].
Cleghorn, Laura A. T. ;
Ray, Peter C. ;
Odingo, Joshua ;
Kumar, Anuradha ;
Wescott, Heather ;
Korkegian, Aaron ;
Masquelin, Thierry ;
Moure, Abraham Lopez ;
Wilson, Caroline ;
Davis, Susan ;
Hugtgett, Margaret ;
Turner, Penelope ;
Smith, Alasdair ;
Epemolu, Ola ;
Zuccotto, Fabio ;
Riley, Jennifer ;
Scullion, Paul ;
Shishikura, Yoko ;
Ferguson, Liam ;
Rullas, Joaquin ;
Guijarro, Laura ;
Read, Kevin D. ;
Green, Simon R. ;
Hipskind, Phil ;
Parish, Tanya ;
Wyatt, Paul G. .
JOURNAL OF MEDICINAL CHEMISTRY, 2018, 61 (15) :6592-6608