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Open-source discovery of chemical leads for next-generation chemoprotective antimalarials

ScienceNOW Daily News Feed - Jue, 12/06/2018 - 12:38

To discover leads for next-generation chemoprotective antimalarial drugs, we tested more than 500,000 compounds for their ability to inhibit liver-stage development of luciferase-expressing Plasmodium spp. parasites (681 compounds showed a half-maximal inhibitory concentration of less than 1 micromolar). Cluster analysis identified potent and previously unreported scaffold families as well as other series previously associated with chemoprophylaxis. Further testing through multiple phenotypic assays that predict stage-specific and multispecies antimalarial activity distinguished compound classes that are likely to provide symptomatic relief by reducing asexual blood-stage parasitemia from those which are likely to only prevent malaria. Target identification by using functional assays, in vitro evolution, or metabolic profiling revealed 58 mitochondrial inhibitors but also many chemotypes possibly with previously unidentified mechanisms of action.

News at a glance

ScienceNOW Daily News Feed - Jue, 12/06/2018 - 12:38

Taking aim

ScienceNOW Daily News Feed - Jue, 12/06/2018 - 12:38

At arm's length

ScienceNOW Daily News Feed - Jue, 12/06/2018 - 12:38

Two-dimensional materials skip the energy barrier by growing one row at a time

EurekAlert! - Mié, 12/05/2018 - 23:00
A new study published in the journal Science, could provide engineers new design rules for creating microelectronics, membranes, and tissues, and open up better production methods for new materials. At the same time, the research helps uphold a scientific theory that has remained unproven for over a century.

Developing new materials for the fusion reactor

EurekAlert! - Mié, 12/05/2018 - 23:00
At National Institute for Fusion Science (NIFS) we have newly developed vanadium alloys that is strong at high temperatures and is appropriate for manufacturing and welding. From this, we have shown for the first time in the world the possibility of producing a blanket which will be installed in a future fusion reactor and will be an important equipment for generating electricity.

Targeted cognitive training benefits patients with severe schizophrenia

EurekAlert! - Mié, 12/05/2018 - 23:00
Researchers find that patients with severe, refractory schizophrenia benefit from targeted cognitive therapy, improving auditory and verbal outcomes and the way they process information.

Eliminating the latent reservoir of HIV

EurekAlert! - Mié, 12/05/2018 - 23:00
A new study suggests that a genetic switch that causes latent HIV inside cells to begin to replicate can be manipulated to completely eradicate the virus from the human body. Cells harboring latent HIV are 'invisible' to the natural defenses of the immune system.The findings, which suggest a cure for HIV may be possible, are reported in the journal Proceedings of the National Academy of Sciences.

Black women have worse breast cancer outcomes despite receiving similar treatment as white women

EurekAlert! - Mié, 12/05/2018 - 23:00
Even with equivalent treatments in women with hormone receptor-positive, HER2-negative breast cancer, black women had significantly higher breast cancer recurrence and increased overall mortality compared to white women in a large phase III clinical trial, TAILORx, according to data presented at the 2018 San Antonio Breast Cancer Symposium.

Houston Methodist launches real-time flu tracker website

EurekAlert! - Mié, 12/05/2018 - 23:00
Pathologists at Houston Methodist developed a real-time website to track flu cases, just in time to assist physicians, the CDC and patients for the fall 2018 flu season.

WSU researchers create 3D-printed glucose biosensors

EurekAlert! - Mié, 12/05/2018 - 23:00
A 3D-printed glucose biosensor for use in wearable monitors has been created by Washington State University researchers. The work could lead to improved glucose monitors for millions of people who suffer from diabetes.

Unknown treasure trove of planets found hiding in dust

EurekAlert! - Mié, 12/05/2018 - 23:00
The first unbiased survey of protoplanetary disks surrounding young stars in the Taurus star-forming region turned up a higher-than-expected number of disks with features suggesting nascent planets, according to a study by an international team of astronomers involving researchers at the University of Arizona's Steward Observatory and Lunar and Planetary Laboratory.

New traffic rules in 'Graphene City'

EurekAlert! - Mié, 12/05/2018 - 23:00
In the drive to find new ways to extend electronics beyond the use of silicon, physicists are experimenting with other properties of electrons, beyond charge. In work published today (Dec 7) in the journal Science, a team led by Penn State professor of physics Jun Zhu describes a way to manipulate electrons based on their energy in relation to momentum -- called 'valley degree of freedom.'

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