ArticleJournal of medicinal chemistry2009
Structures of falcipain-2 and falcipain-3 bound to small molecule inhibitors: implications for substrate specificity.
Article in Journal of medicinal chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 54 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
54 citing papers in PubMed, 167 citations in OpenAlex.
- Co(II), Cu(II), and Ni(II) Coordination Complexes: Synthesis, Characterization, Experimental, and Computational Study on Potential Antiplasmodial Activity.ChemMedChem · 2026Article
- Antiplasmodial Activity of Methylangolensate FromJournal of tropical medicine · 2026Article
- Malaria parasite cysteine and aspartic proteases as key drug targets for antimalarial therapy.Journal of molecular modeling · 2025Review
- Decoding substrate recognition in malapain-2 through structural and mutational insights.Computational and structural biotechnology journal · 2025Article
- Reinvestigation of diphenylmethylpiperazine analogues of pyrazine as new class ofRSC medicinal chemistry · 2024Article
- Three Decades of Targeting Falcipains to Develop Antiplasmodial Agents: What have we Learned and What can be Done Next?Current medicinal chemistry · 2024Review
- Chemo-proteomics in antimalarial target identification and engagement.Medicinal research reviews · 2023Review
- Identification of Potential Antimalarial Drug Candidates Targeting Falcipain-2 Protein of Malaria Parasite-A Computational Strategy.Biotech (Basel (Switzerland)) · 2022Article
- Evaluation of anti-malarial potency of new pyrazole-hydrazine coupled to Schiff base derivatives.Malaria journal · 2022Article
- Evaluation of antiplasmodial activity in silico and in vitro of N-acylhydrazone derivatives.BMC chemistry · 2022Article
- Examination of the impact molecular charge has on NTSR1-targeted agents incorporated with cysteine protease inhibitors.European journal of medicinal chemistry · 2022Article
- Target-Based Virtual Screening of Natural Compounds Identifies a Potent Antimalarial With Selective Falcipain-2 Inhibitory Activity.Frontiers in pharmacology · 2022Article
- Microsecond-long simulation reveals the molecular mechanism for the dual inhibition of falcipain-2 and falcipain-3 by antimalarial lead compounds.Frontiers in molecular biosciences · 2022Article
- Synthesis, Molecular Docking and Antiplasmodial Activities of New Tetrahydro-β-Carbolines.International journal of molecular sciences · 2021Article
- X-ray Structure Determination, Antioxidant Voltammetry Studies of Butein and 2',4'-Dihydroxy-3,4-dimethoxychalcone. Computational Studies of 4 Structurally Related 2',4'-diOH Chalcones to Examine Their Antimalarial Activity by Binding to Falcipain-2.Molecules (Basel, Switzerland) · 2021Article
- Article
- Allosteric pockets and dynamic residue network hubs of falcipain 2 in mutations including those linked to artemisinin resistance.Computational and structural biotechnology journal · 2021Article
- Structures of the free and inhibitors-bound forms of bromelain and ananain from Ananas comosus stem and in vitro study of their cytotoxicity.Scientific reports · 2020Article
- A Novel Series of [1,2,4]Triazolo[4,3-a]Pyridine Sulfonamides as Potential Antimalarial Agents: In Silico Studies, Synthesis and In Vitro Evaluation.Molecules (Basel, Switzerland) · 2020Article
- A cysteine protease of Babesia microti and its interaction with tick cystatins.Parasitology research · 2020Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
Falcipain-2 and falcipain-3 are critical hemoglobinases of Plasmodium falciparum, the most virulent human malaria parasite. We have determined the 2.9 A crystal structure of falcipain-2 in complex with the epoxysuccinate E64 and the 2.5 A crystal structure of falcipain-3 in complex with the aldehyde leupeptin. These complexes represent the first crystal structures of plasmodial cysteine proteases with small molecule inhibitors and the first reported crystal structure of falcipain-3. Our structural analyses indicate that the relative shape and flexibility of the S2 pocket are affected by a number of discrete amino acid substitutions. The cumulative effect of subtle differences, including those at "gatekeeper" positions, may explain the observed kinetic differences between these two closely related enzymes.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.