User profiles for Madeline R. Luth
Madeline R. Luth, Ph.D.Verified email at ucsd.edu Cited by 935 |
Open-source discovery of chemical leads for next-generation chemoprotective antimalarials
INTRODUCTION Malaria remains a devastating disease, affecting 216 million people annually,
with 445,000 deaths occurring primarily in children under 5 years old. Malaria treatment …
with 445,000 deaths occurring primarily in children under 5 years old. Malaria treatment …
Cytoplasmic isoleucyl tRNA synthetase as an attractive multistage antimalarial drug target
Development of antimalarial compounds into clinical candidates remains costly and arduous
without detailed knowledge of the target. As resistance increases and treatment options at …
without detailed knowledge of the target. As resistance increases and treatment options at …
Reaction hijacking of tyrosine tRNA synthetase as a new whole-of-life-cycle antimalarial strategy
Aminoacyl transfer RNA (tRNA) synthetases (aaRSs) are attractive drug targets, and we
present class I and II aaRSs as previously unrecognized targets for adenosine 5′-…
present class I and II aaRSs as previously unrecognized targets for adenosine 5′-…
[PDF][PDF] Chemogenomics identifies acetyl-coenzyme A synthetase as a target for malaria treatment and prevention
We identify the Plasmodium falciparum acetyl-coenzyme A synthetase (PfAcAS) as a
druggable target, using genetic and chemical validation. In vitro evolution of resistance with two …
druggable target, using genetic and chemical validation. In vitro evolution of resistance with two …
Using in Vitro Evolution and Whole Genome Analysis To Discover Next Generation Targets for Antimalarial Drug Discovery
Although many new anti-infectives have been discovered and developed solely using
phenotypic cellular screening and assay optimization, most researchers recognize that structure-…
phenotypic cellular screening and assay optimization, most researchers recognize that structure-…
The anticancer human mTOR inhibitor sapanisertib potently inhibits multiple Plasmodium kinases and life cycle stages
…, E Erlank, N Venter, N Mittal, MR Luth… - Science translational …, 2022 - science.org
Compounds acting on multiple targets are critical to combating antimalarial drug resistance.
Here, we report that the human “mammalian target of rapamycin” (mTOR) inhibitor …
Here, we report that the human “mammalian target of rapamycin” (mTOR) inhibitor …
[HTML][HTML] Covalent Plasmodium falciparum-selective proteasome inhibitors exhibit a low propensity for generating resistance in vitro and synergize with multiple …
Therapeutics with novel modes of action and a low risk of generating resistance are urgently
needed to combat drug-resistant Plasmodium falciparum malaria. Here, we report that the …
needed to combat drug-resistant Plasmodium falciparum malaria. Here, we report that the …
Target Validation and Identification of Novel Boronate Inhibitors of the Plasmodium falciparum Proteasome
The Plasmodium proteasome represents a potential antimalarial drug target for compounds
with activity against multiple life cycle stages. We screened a library of human proteasome …
with activity against multiple life cycle stages. We screened a library of human proteasome …
Advances in malaria pharmacology and the online guide to MALARIA PHARMACOLOGY: IUPHAR review 38
Antimalarial drug discovery has until recently been driven by high‐throughput phenotypic
cellular screening, allowing millions of compounds to be assayed and delivering clinical drug …
cellular screening, allowing millions of compounds to be assayed and delivering clinical drug …
[HTML][HTML] CYP51 is an essential drug target for the treatment of primary amoebic meningoencephalitis (PAM)
Primary Amoebic Meningoencephalitis (PAM) is caused by Naegleria fowleri, a free-living
amoeba that occasionally infects humans. While considered “rare” (but likely underreported) …
amoeba that occasionally infects humans. While considered “rare” (but likely underreported) …