Antimalarial hemozoin inhibitors (β-hematin formation inhibition): latest updates

JN Cruz, SN Mali - Combinatorial Chemistry & High …, 2022 - ingentaconnect.com
… Thus, drugs targeting hemozoin formation (a unique process by Plasmodium spp. to
detoxify free heme) remain a key and viable target for anti-malarial drugmechanism yet [1]. …

Hemozoin (beta-hematin) Formation inhibitors: Promising target for the development of new antimalarials: Current update and future prospect

SN Mali, A Pandey - Combinatorial Chemistry & High …, 2022 - ingentaconnect.com
… focus on drug inhibiting the β-hematin formation via π-π interactions, ie., by heme-drug
interactions. … Compound 42 f was subjected for mechanistic study, and it was observed that this …

Heme detoxification in the malaria parasite: A target for antimalarial drug development

KA de Villiers, TJ Egan - Accounts of chemical research, 2021 - ACS Publications
… These metrics are regularly updated to reflect usage leading … docking to discover new
hemozoin inhibiting compounds from an … Our work on the mechanism of β-hematin formation has …

A second mechanism employed by artemisinins to suppress Plasmodium falciparum hinges on inhibition of hematin crystallization

W Ma, VA Balta, R West, KN Newlin, OŠ Miljanić… - Journal of Biological …, 2021 - ASBMB
… -class antimalarials inhibit the formation of hemozoin and in … We show that these adducts
inhibit β-hematin crystallization … via parent drug activation. Our findings reveal an irreversible …

The role of the iron protoporphyrins heme and hematin in the antimalarial activity of endoperoxide drugs

HC Quadros, MCB Silva, DRM Moreira - Pharmaceuticals, 2022 - mdpi.com
… biomineralization of hematin into hemozoin crystals, differing … A second mechanism, where
a drug binds by adsorption … –drug adducts to inhibit β-hematin crystal formation and the …

Pyronaridine: An update of its pharmacological activities and mechanisms of action

C Bailly - Biopolymers, 2021 - Wiley Online Library
… in hemozoin. This is also the case of PYR which was found to be equally potent as chloroquine
at inhibiting β-hematin formation in … suppresses β-hematin crystal growth by a mechanism

In Vitro Investigation Unveiling New Insights into the Antimalarial Mechanism of Chloroquine: Role in Perturbing Nucleation Events during Heme to β-Hematin …

R Singh, R Singh, V Srihari, RD Makde - ACS Infectious Diseases, 2023 - ACS Publications
… These metrics are regularly updated to reflect usage leading … To study the role of CQ in
inhibiting heme to β-hematin … of chloroquine on hemozoin formation, and it is well-established that …

Antimalarial Activity of Highly Coordinative Fused Heterocycles Targeting β-Hematin Crystallization

ME Acosta, L Gotopo, N Gamboa, JR Rodrigues… - ACS …, 2022 - ACS Publications
… These metrics are regularly updated to reflect … mechanism within its digestive vacuole
where the heme group is converted into a nontoxic crystalline solid called hemozoin (β-hematin), …

Advances in the research on the targets of anti-malaria actions of artemisinin

J Yang, Y He, Y Li, X Zhang, YK Wong, S Shen… - Pharmacology & …, 2020 - Elsevier
… the digestion of hemoglobin to release heme inhibited the activation of artemisinin, whereas
the … developed a detoxification mechanism that converts hematin to non-toxic hemozoin (…

Antimalarial drugs

BJ Sawyer, MIH Khan, HV Le - … Chemistry of Chemotherapeutic Agents, 2023 - Elsevier
… They can inhibit hemozoin biocrystallization and inhibitmechanism of hemozoin
biocrystallization. Under the acidic condition inside the food vacuoles, β-hematin, a heme dimer …