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Review
. 2014 Nov 26;114(22):11280-304.
doi: 10.1021/cr500197d. Epub 2014 Oct 7.

Kinases as druggable targets in trypanosomatid protozoan parasites

Christopher Merritt  1 , Lisseth E Silva  2 , Angela L Tanner  2 , Kenneth Stuart  1 , Michael P Pollastri  2
Affiliations
Review

Kinases as druggable targets in trypanosomatid protozoan parasites

Christopher Merritt et al. Chem Rev. .
No abstract available

PubMed Disclaimer

Figures

Figure 1
Figure 1
Protein kinase inhibitors screened against TbGSK and BSF T. brucei
Figure 2
Figure 2
Human GSK inhibitors screened against TbGSK-3s.
Figure 3
Figure 3
Known mammalian kinase inhibitors profiled against the T. brucei kinome using kinobead technology.
Figure 4
Figure 4
Inhibitors of TbGSK3.
Figure 5
Figure 5
2,5-Anhydro-d-mannitol analogues screened against TbPFK.
Figure 6
Figure 6
Alkaloids screened against T. brucei PFK.
Figure 7
Figure 7
Amidosulfonamide derivatives tested against TbPFK.
Figure 8
Figure 8
Adenosine derivatives tested against TbPGK and T. brucei.
Figure 9
Figure 9
Glucose-6-phosphate derivatives tested against T. brucei hexokinase.
Figure 10
Figure 10
General protein kinase inhibitors in T. cruzi.
Figure 11
Figure 11
Inhibitors of arginine kinase in T. cruzi.
Figure 12
Figure 12
Inhibitors of T. cruzi PFK.
Figure 13
Figure 13
Indirubins screened against L. donovani.
Figure 14
Figure 14
2,5-Anhydro-d-mannitol derivatives tested against L. mexicanan PyK.
Figure 15
Figure 15
(A) Saccharin derivatives screened against L. mexicana PyK. (B) Overlaid X-ray structures of LmPyK and HsM2PyK with covalently bound inhibitor. Reprinted with permission from ref (114). Copyright 2012 The Biochemical Society.
Figure 16
Figure 16
Compound from the bark of the Entada abyssinica plant tested against LmPyK.
Figure 17
Figure 17
CK inhibitors purvalanol B, and pyrrole and imidazopyridine derivatives screened against Leishmania.
Figure 18
Figure 18
Compounds shown to inhibit L. donovani PKC.
Figure 19
Figure 19
Compounds screened against L. donovani amastigotes and L. mexicana promastigotes.
Figure 20
Figure 20
Compounds screened against Leishmania CRK3:CYC6, human CDK2:CycA, and L. major promastigote and amastigote cells.
Figure 21
Figure 21
Compounds screened against Leishmania CRK3:CYC6 and human CDK2:CycA.
Figure 22
Figure 22
Human aurora kinase inhibitors.
Figure 23
Figure 23
SAR exploration of the hesperadin chemotype.
Figure 24
Figure 24
Repurposed human aurora inhibitors 1 and 2, and a new analogue with improved T. brucei selectivity.
Figure 25
Figure 25
NVP-BEZ235 and derivatives are potent trypanosomatid growth inhibitors. Tbb = T. brucei brucei; Tbr = T. brucei rhodesiense.
Figure 26
Figure 26
Lapatinib and derivatives that show potent and selective T. brucei activity.
See this image and copyright information in PMC

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