Kinase inhibitors: the road ahead

FM Ferguson, NS Gray - Nature reviews Drug discovery, 2018 - nature.com
Receptor tyrosine kinase signalling pathways have been successfully targeted to inhibit
proliferation and angiogenesis for cancer therapy. However, kinase deregulation has been …

Antimalarial drug resistance and novel targets for antimalarial drug discovery

MA Shibeshi, ZD Kifle, SA Atnafie - Infection and drug resistance, 2020 - Taylor & Francis
Malaria is among the most devastating and widespread tropical parasitic diseases in which
most prevalent in developing countries. Antimalarial drug resistance is the ability of a …

Progress towards a public chemogenomic set for protein kinases and a call for contributions

DH Drewry, CI Wells, DM Andrews, R Angell, H Al-Ali… - PloS one, 2017 - journals.plos.org
Protein kinases are highly tractable targets for drug discovery. However, the biological
function and therapeutic potential of the majority of the 500+ human protein kinases remains …

[HTML][HTML] Drug targets for resistant malaria: historic to future perspectives

S Kumar, TR Bhardwaj, DN Prasad… - Biomedicine & …, 2018 - Elsevier
New antimalarial targets are the prime need for the discovery of potent drug candidates. In
order to fulfill this objective, antimalarial drug researches are focusing on promising targets …

Plasmodium parasite exploits host aquaporin-3 during liver stage malaria infection

D Posfai, K Sylvester, A Reddy, JG Ganley… - PLoS …, 2018 - journals.plos.org
Within the liver a single Plasmodium parasite transforms into thousands of blood-infective
forms to cause malaria. Here, we use RNA-sequencing to identify host genes that are …

Chemical probes for understudied kinases: challenges and opportunities

RAM Serafim, JM Elkins, WJ Zuercher… - Journal of Medicinal …, 2021 - ACS Publications
Over 20 years after the approval of the first-in-class protein kinase inhibitor imatinib, the
biological function of a significant fraction of the human kinome remains poorly understood …

[HTML][HTML] Overcoming fungal echinocandin resistance through inhibition of the non-essential stress kinase Yck2

T Caplan, Á Lorente-Macías, PJ Stogios… - Cell chemical …, 2020 - cell.com
New strategies are urgently needed to counter the threat to human health posed by drug-
resistant fungi. To explore an as-yet unexploited target space for antifungals, we screened a …

Identification of Hsp90 inhibitors with anti-Plasmodium activity

D Posfai, AL Eubanks, AI Keim, KY Lu… - Antimicrobial agents …, 2018 - Am Soc Microbiol
Malaria remains a global health burden partly due to Plasmodium parasite resistance to first-
line therapeutics. The molecular chaperone heat shock protein 90 (Hsp90) has emerged as …

Screening the Global Health Priority Box against Plasmodium berghei liver stage parasites using an inexpensive luciferase detection protocol

GB Nguyen, CA Cooper, O McWhorter, R Sharma… - Malaria Journal, 2024 - Springer
Background Malaria, a disease caused by parasites of the genus Plasmodium, continues to
impact many regions globally. The rise in resistance to artemisinin-based anti-malarial drugs …

Random forest model predictions afford dual-stage antimalarial agents

H Mughal, EC Bell, K Mughal… - ACS infectious …, 2022 - ACS Publications
The need for novel antimalarials is apparent given the continuing disease burden
worldwide, despite significant drug discovery advances from the bench to the bedside. In …