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NOT Open Access | Synthesis, structure-activity relationship and antimalarial efficacy of 6-chloro-2-arylvinylquinolines

September 23, 2020 - 09:30 -- NOT Open Access
Huang G, Murillo Solano C, Yuan Y, et al.
J Med Chem. 2020 Sep 22

There is an urgent need to develop new efficacious antimalarials to address the emerging drug-resistant clinical cases. Our previous phenotypic screening identified styrylquinoline UCF501 as a promising antimalarial compound.

NOT Open Access | Structure activity studies of truncated latrunculin analogues with anti-malarial activity

September 16, 2020 - 13:05 -- NOT Open Access
Varghese S, Rahmani R, Drew DR, Beeson JG, Baum J, Smith BJ, Baell J
ChemMedChem. 2020 Sep 14

Malarial parasites employ actin dynamics for motility, and any disruption to these dynamics renders the parasites unable to effectively establish infection. Therefore, actin presents a potential target for malarial drug discovery, and naturally occurring actin inhibitors such as latrunculins are a promising starting point.

A Nonpeptidyl Molecule Modulates Apoptosis-like Cell Death by Inhibiting P.falciparum Metacapase-2

March 24, 2020 - 12:31 -- Open Access
Kumari V, Sankar S, Prasad KM, Kashif M, Kalia I, Rai R, Singh AP, Pandey KC
Biochem J. 2020 Mar 23. pii: BCJ20200050

Metacaspases are novel cysteine proteases found in apicomplexan whose function is poorly understood. Our earlier studies on Plasmodium falciparum metacaspase-2 (PfMCA-2) revealed that the caspase inhibitor, Z-FA-FMK efficiently inhibited PfMCA-2 activity and, expression, and significantly blocked in vitro progression of the parasite developmental cycle via apoptosis-like parasite death.

The contribution of non-malarial febrile illness co-infections to Plasmodium falciparum case counts in health facilities in sub-Saharan Africa

June 11, 2019 - 14:52 -- Open Access
Ursula Dalrymple, Ewan Cameron, Peter W. Gething, et al.
Malaria Journal 2019 18:195, 11 June 2019

The disease burden of Plasmodium falciparum malaria illness is generally estimated using one of two distinct approaches: either by transforming P. falciparum infection prevalence estimates into incidence estimates using conversion formulae; or through adjustment of counts of recorded P. falciparum-positive fever cases from clinics. Whilst both ostensibly seek to evaluate P. falciparum disease burden, there is an implicit and problematic difference in the metric being estimated. The first enumerates only symptomatic malaria cases, while the second enumerates all febrile episodes coincident with a P. falciparum infection, regardless of the fever’s underlying cause.

New adenovirus-based vaccine vectors targeting Pfs25 elicit antibodies that inhibit Plasmodium falciparum transmission

June 15, 2017 - 15:44 -- Open Access
Kathleen A. McGuire, Kazutoyo Miura, Christopher M. Wiethoff and Kim C. Williamson
Malaria Journal 2017 16:254, 15 June 2017

The data suggest that focusing the immune response against defined epitopes displayed on the viral capsid is an effective strategy for transmission-blocking vaccine development.

Fixed dose artesunate amodiaquine - a phase IIb, randomized comparative trial with non-fixed artesunate amodiaquine

December 22, 2014 - 09:56 -- Open Access
Ogutu B, Juma E, Obonyo C, Jullien V, Carn G, Vaillant M, Taylor WR, Kiechel J
Malaria Journal 2014, 13 :498 (16 December 2014)

Tolerability of both formulations was good. For QTcB, a parameter for ECG modifications, increases were modest and due to rising DAQ concentrations and falling heart rates as malaria resolved.

Export of virulence proteins by malaria-infected erythrocytes involves remodeling of host actin cytoskeleton

December 16, 2014 - 15:16 -- Open Access
Melanie Rug, Marek Cyrklaff, Alan F. Cowman, et al.
Blood: 124 (23), November 27, 2014

Following invasion of human red blood cells (RBCs) by the malaria parasite, Plasmodium falciparum, a remarkable process of remodeling occurs in the host cell mediated by trafficking of several hundred effector proteins to the RBC compartment.

Antiplasmodial activity of chloroquine analogs against chloroquine-resistant parasites, docking studies and mechanisms of drug action

December 12, 2014 - 06:43 -- Open Access
Nicolli B de Souza, Arturene ML Carmo, Adilson D da Silva, Tanos CC França, Antoniana U Krettli
Malaria Journal 2014, 13:469 (2 December 2014)

The presence of an alkyne group and the size of the side chain affected anti-P. falciparum activity in vitro.

Medical Treatment: 

Glomerular changes and alterations of zonula occludens-1 in the kidneys of Plasmodium falciparum malaria patients

May 20, 2014 - 09:45 -- Open Access
Wichapoon B, Punsawad C, Chaisri U, Viriyavejakul P
Malaria Journal 2014, 13 :176 (9 May 2014)

In P. falciparum malaria with AKI, the decrease in glomerular area, despite glomerular cell proliferation, could be due to the collapse of cellular structures secondary to damaged tight junction-associated protein, ZO-1.


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