Elizabeth A. Winzeler

Identification, Structure–Activity Relationship (SAR), and Biological Evaluation of New Chemical Series as Malaria Parasite Pf GCN5 Bromodomain Inhibitors

Pedro Martín-Acosta, Abbas H. K. Al Temimi, Luma G. Magalhães, Juan Salamanca-Viloria et autres

Abstract Despite considerable progress in prevention, treatment, and eradication efforts, malaria continues to impose a significant public health and socioeconomic burden for many countries around the globe. With the effectiveness of current treatment options partially or totally compromised due to resistance, the …

fr, gb, nl, us (code pays fourni par la source)

Discovery of Sphaeriaurantins as Rapid-Acting Antiplasmodials with Dual Activity in Blood and Liver Stages

Chantal D. Bader, Jennifer E. Collins, Yuelan Li, Edward Kalkreuter et autres

The rapid emergence of resistance in the malaria-causing protozoan Plasmodium falciparum has heightened the demand for treatments with novel modes of action. Having evolved to produce a myriad of structurally diverse natural products (NPs) as defenses against soil-dwelling parasites including protozoa, Actinomycetota …

us, gb (code pays fourni par la source)

VAMP3 vesicles support host protein recruitment and Plasmodium liver stage development

Michael E. Chirgwin, Chelsea Gan, Karla P. Godinez‐Macias, Kaitlyn Choe et autres

ABSTRACT Plasmodium remodels the host liver cell as an obligatory step in malaria infection. Although several host proteins are recruited to the parasitophorous vacuole membrane (PVM) after invasion, the mechanisms underlying this acquisition remain unknown. Here, we validated the upregulation and recruitment …

us, pe (code pays fourni par la source)

Discovery of Sphaeriaurantins as Rapid-Acting Antiplasmodials with Dual Activity in Blood and Liver Stages

Chantal D. Bader, Jennifer E. Collins, Yuelan Li, Edward Kalkreuter et autres

The rapid emergence of resistance in the malaria-causing protozoan Plasmodium falciparum has heightened the demand for treatments with novel modes of action. Having evolved to produce a myriad of structurally diverse natural products (NPs) as defenses against soil-dwelling parasites including protozoa, Actinomycetota …

us, gb, no (code pays fourni par la source)

The Human Chk1 Inhibitor CHIR-124 Shows Multistage Activity against the Human Malaria Parasite Plasmodium falciparum via Polypharmacological Inhibition of Pf Ark1 and Hemozoin Formation

Kathryn J. Wicht, John G. Woodland, Larnelle F. Garnie, Henrico Langeveld et autres

High Resolution Image Download MS PowerPoint Slide The high burden of malaria and growing resistance to frontline antimalarials demand new drug target combinations with reduced propensities for conferring parasite resistance. An attractive approach for circumventing antimalarial drug resistance is target repurposing, in …

Afrique du Sud, ca, Éthiopie, us, de, fr, gb, ch, cz (code pays fourni par la source)

Duplication of superoxide dismutase and a mutation in aquaglyceroporin mediates the sensitivity of Plasmodium falciparum to cryptosporin, a natural product derived from Acaromyces ingoldii

Tiantian Jiang, Jennifer E. Collins, Jin Woo Lee, Sebastian Buss et autres

Abstract Cryptosporin, a fungal metabolite, exhibited potent antimalarial activity against both asexual blood stage Plasmodium falciparum and liver-stage Plasmodium berghei with minimal human HepG2 toxicity. Unlike atovaquone, cryptosporin’s mechanism is independent of mitochondrial electron transport. Minimum inoculum of resistance showed a low …

us, kr, de, gb, br (code pays fourni par la source)

The Human Chk1 Inhibitor CHIR-124 Shows Multistage Activity against the Human Malaria Parasite Plasmodium falciparum via Polypharmacological Inhibition of Pf Ark1 and Hemozoin Formation

Kathryn J. Wicht, John G. Woodland, Larnelle F. Garnie, Henrico Langeveld et autres

The high burden of malaria and growing resistance to frontline antimalarials demand new drug target combinations with reduced propensities for conferring parasite resistance. An attractive approach for circumventing antimalarial drug resistance is target repurposing, in which known drugs that act through protein …

de (code pays fourni par la source)

BindingDB Entry 50010210: Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials.

BindingDB, Tiqing Liu, Michael Gilson, Neil Norcross et autres

Small molecule binding data for protein Cytochrome P450 1A2, Cytochrome P450 2C19, Cytochrome P450 2C9, Cytochrome P450 2D6, and Cytochrome P450 3A4, Uniprot P05177, P08684, P10635, P11712, and P33261

Abstract Book

Robert L. Summers, Manu Vanaerschot, James M. Murithi, Charisse F. Pasaje et autres

Indonesia carries the heaviest burden of soil-transmitted helminth (STH) infection in Southeast Asia with more than 62 million children requiring preventative chemotherapy in 2017 alone. Prevalence data for many parts of the country are out-dated and knowledge of the risk factors involved …

cz (code pays fourni par la source)

CCDC 1045851: Experimental Crystal Structure Determination

Alice Williamson, Paul M. Ylioja, Murray N. Robertson, Yevgeniya Antonova‐Koch et autres

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, …