Plasmodium falciparum histone deacetylase 1

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Chromatin modifying enzymes (Plasmodium spp.)
Plasmodium falciparum histone deacetylase 1

Target id: 3072

Nomenclature: Plasmodium falciparum histone deacetylase 1

Abbreviated Name: PfHDAC1

Family: Chromatin modifying enzymes (Plasmodium spp.)

Gene and Protein Information
Species	TM	AA	Chromosomal Location	Gene Symbol	Gene Name	Reference
Plasmodium falciparum 3D7	-	449		HDAC1	histone deacetylase 1

Previous and Unofficial Names
HDAC1 \| Pf3D7_09_v3:1,028,046..1,031,647(-) \| KDAC1 \| PFI1260c

Database Links
Alphafold	Q7K6A1 (Pf3D7)
ChEMBL Target	CHEMBL1293190 (Pf3D7)
PlasmoDB	PF3D7_0925700 (Pf3D7)
UniProtKB	Q7K6A1 (Pf3D7)

Ligand		Sp.	Assay description	Type	Action	Value	Parameter	Reference
JX21108		Pf3D7 Plasmodium falciparum 3D7 P. falciparum strain 3D7 (Pf3D7) was derived from isolate NF54 by limiting dilution. The complete genome of Pf3D7 has been sequenced (GenBank: LN999946.1). Pf3D7 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is sensitive to a panel of antimalarial compounds including chloroquine and pyrimethamine. ✖	Parasite growth inhibition assay	-	-	8.4	pEC₅₀	6
⤷	pEC₅₀ 8.4 (EC₅₀ 3.6x10^-9 M) SYBR Green I assay (72 hours) [6] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
JX21108		PfDd2 Plasmodium falciparum Dd2 P. falciparum strain Dd2 (PfDd2) is a clone derived from PfW2, following continuous culture in mefloquine. PfW2 was cloned from the Indochina III/CDC isolate, originally derived from a Laotian patient who failed chloroquine therapy. PfDd2 can be obtained from the Malaria Research and Reference Reagent Resource Center (MR4) and is reported to be resistant to chloroquine, pyrimethamine and mefloquine. ✖	Parasite growth inhibition assay	-	-	8.4	pEC₅₀	6
⤷	pEC₅₀ 8.4 (EC₅₀ 4x10^-9 M) SYBR Green I assay (72 hours) [6] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
quisinostat		Pf3D7 Plasmodium falciparum 3D7 P. falciparum strain 3D7 (Pf3D7) was derived from isolate NF54 by limiting dilution. The complete genome of Pf3D7 has been sequenced (GenBank: LN999946.1). Pf3D7 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is sensitive to a panel of antimalarial compounds including chloroquine and pyrimethamine. ✖	Parasite growth inhibition assay	-	-	8.3	pEC₅₀	6
⤷	pEC₅₀ 8.3 (EC₅₀ 5.2x10^-9 M) SYBR Green I assay (72 hours) [6] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
quisinostat		PfDd2 Plasmodium falciparum Dd2 P. falciparum strain Dd2 (PfDd2) is a clone derived from PfW2, following continuous culture in mefloquine. PfW2 was cloned from the Indochina III/CDC isolate, originally derived from a Laotian patient who failed chloroquine therapy. PfDd2 can be obtained from the Malaria Research and Reference Reagent Resource Center (MR4) and is reported to be resistant to chloroquine, pyrimethamine and mefloquine. ✖	Parasite growth inhibition assay	-	-	8.1	pEC₅₀	6
⤷	pEC₅₀ 8.1 (EC₅₀ 7.1x10^-9 M) SYBR Green I assay (72 hours) [6] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
JX21108		PfNF54 Plasmodium falciparum NF54 P. falciparum strain NF54 (PfNF54) was derived from a patient who had never left the Netherlands. PfNF54 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is sensitive to a panel of antimalarial compounds including chloroquine and pyrimethamine. ✖	Parasite gametocyte viability assay	-	-	7.4 – 8.2	pEC₅₀	6
⤷	pEC₅₀ 8.2 (EC₅₀ 5.9x10^-9 M) Parasite late stage (IV) gametocyte assay using luciferase reporter line [6] Lifecycle stages: Plasmodium sexual blood stage (gametocyte) pEC₅₀ 7.4 (EC₅₀ 3.88x10^-8 M) Parasite early stage (II) gametocyte assay using luciferase reporter line [6] Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
compound 1u [PMID: 30245402]		PfDd2 Plasmodium falciparum Dd2 P. falciparum strain Dd2 (PfDd2) is a clone derived from PfW2, following continuous culture in mefloquine. PfW2 was cloned from the Indochina III/CDC isolate, originally derived from a Laotian patient who failed chloroquine therapy. PfDd2 can be obtained from the Malaria Research and Reference Reagent Resource Center (MR4) and is reported to be resistant to chloroquine, pyrimethamine and mefloquine. ✖	Parasite growth inhibition assay	-	-	9.0	pIC₅₀	3
⤷	pIC₅₀ 9.0 (IC₅₀ 1x10^-9 M) [³H]-hypoxanthine incorporation [3] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
JX35		Pf3D7 Plasmodium falciparum 3D7 P. falciparum strain 3D7 (Pf3D7) was derived from isolate NF54 by limiting dilution. The complete genome of Pf3D7 has been sequenced (GenBank: LN999946.1). Pf3D7 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is sensitive to a panel of antimalarial compounds including chloroquine and pyrimethamine. ✖	Parasite growth inhibition assay	-	-	8.9	pIC₅₀	11
⤷	pIC₅₀ 8.9 (IC₅₀ 1.26x10^-9 M) SYBR Green I assay (72h) [11] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
JX35		PfDd2 Plasmodium falciparum Dd2 P. falciparum strain Dd2 (PfDd2) is a clone derived from PfW2, following continuous culture in mefloquine. PfW2 was cloned from the Indochina III/CDC isolate, originally derived from a Laotian patient who failed chloroquine therapy. PfDd2 can be obtained from the Malaria Research and Reference Reagent Resource Center (MR4) and is reported to be resistant to chloroquine, pyrimethamine and mefloquine. ✖	Parasite growth inhibition assay	-	-	8.8	pIC₅₀	11
⤷	pIC₅₀ 8.8 (IC₅₀ 1.61x10^-9 M) SYBR Green I assay (72h) [11] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
compound 1u [PMID: 30245402]		Pf3D7 Plasmodium falciparum 3D7 P. falciparum strain 3D7 (Pf3D7) was derived from isolate NF54 by limiting dilution. The complete genome of Pf3D7 has been sequenced (GenBank: LN999946.1). Pf3D7 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is sensitive to a panel of antimalarial compounds including chloroquine and pyrimethamine. ✖	Parasite growth inhibition assay	-	-	8.4	pIC₅₀	3
⤷	pIC₅₀ 8.4 (IC₅₀ 4x10^-9 M) [³H]-hypoxanthine incorporation [3] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
compound 2h [PMID: 30664827]		Pf3D7 Plasmodium falciparum 3D7 P. falciparum strain 3D7 (Pf3D7) was derived from isolate NF54 by limiting dilution. The complete genome of Pf3D7 has been sequenced (GenBank: LN999946.1). Pf3D7 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is sensitive to a panel of antimalarial compounds including chloroquine and pyrimethamine. ✖	Parasite growth inhibition assay	-	-	8.3	pIC₅₀	8
⤷	pIC₅₀ 8.3 (IC₅₀ 5.2x10^-9 M) [³H]-hypoxanthine incorporation [8] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
panobinostat		Pk Plasmodium knowlesi P. knowlesi (Pk) is one of five protozoan parasite species of the genus Plasmodium that cause malaria in humans. This species of the parasite was originally identified as causing simian malaria but it is becoming a significant cause of zoonotic malaria and is an emerging public health issue in Southeast Asia. Pk has a 24-hour asexual replication cycle in erythrocytes and can progress quickly to severe clinical disease with fatal cases reported. ✖	Parasite growth inhibition assay	-	-	8.1	pIC₅₀	2
⤷	pIC₅₀ 8.1 (IC₅₀ 9x10^-9 M) [³H]-hypoxanthine incorporation (48h) [2] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
panobinostat		Pf3D7 Plasmodium falciparum 3D7 P. falciparum strain 3D7 (Pf3D7) was derived from isolate NF54 by limiting dilution. The complete genome of Pf3D7 has been sequenced (GenBank: LN999946.1). Pf3D7 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is sensitive to a panel of antimalarial compounds including chloroquine and pyrimethamine. ✖	Parasite growth inhibition assay	-	-	8.0	pIC₅₀	4
⤷	pIC₅₀ 8.0 (IC₅₀ 1x10^-8 M) [³H]-hypoxanthine incorporation [4] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
JX35		PfNF54 Plasmodium falciparum NF54 P. falciparum strain NF54 (PfNF54) was derived from a patient who had never left the Netherlands. PfNF54 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is sensitive to a panel of antimalarial compounds including chloroquine and pyrimethamine. ✖	Parasite late stage (V) gametocyte assay	-	-	7.9	pIC₅₀	11
⤷	pIC₅₀ 7.9 (IC₅₀ 1.242x10^-8 M) [11] Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
FNDR-20123		PfTM90C2B Plasmodium falciparum TM90C2B P. falciparum TM90C2B (PfTM90C2B) is a clinical isolate, first described during a Phase 2 clinical trial to determine atovaquone efficacy in Thailand (PMID:8651372). A point mutation (Y268S) at the Q_o site of cytochrome b results in a 3,000-fold loss of atovaquone sensitivity. It is used as a screening tool for the development of new cytochrome b inhibitors. ✖	Parasite growth inhibition assay	-	-	7.9	pIC₅₀	9
⤷	pIC₅₀ 7.9 (IC₅₀ 1.326x10^-8 M) [9] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
FNDR-20123		Pf7G8 Plasmodium falciparum 7G8 P. falciparum strain 7G8 (Pf7G8) was subcloned from the IMTM22 strain by limiting dilution. The original IMTM22 strain was isolated from a 12 year old male near Manaus, Brazil in 1980. Pf7G8 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4). This strain is a gametocyte producer and is reported to be chloroquine-sensitive and pyrimethamine-resistant. ✖	Parasite growth inhibition assay	-	-	7.8	pIC₅₀	9
⤷	pIC₅₀ 7.8 (IC₅₀ 1.436x10^-8 M) [9] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
JX35		PfNF54 Plasmodium falciparum NF54 P. falciparum strain NF54 (PfNF54) was derived from a patient who had never left the Netherlands. PfNF54 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is sensitive to a panel of antimalarial compounds including chloroquine and pyrimethamine. ✖	Parasite early stage (II) gametocyte assay	-	-	7.8	pIC₅₀	11
⤷	pIC₅₀ 7.8 (IC₅₀ 1.583x10^-8 M) [11] Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
FNDR-20123		PfDd2 Plasmodium falciparum Dd2 P. falciparum strain Dd2 (PfDd2) is a clone derived from PfW2, following continuous culture in mefloquine. PfW2 was cloned from the Indochina III/CDC isolate, originally derived from a Laotian patient who failed chloroquine therapy. PfDd2 can be obtained from the Malaria Research and Reference Reagent Resource Center (MR4) and is reported to be resistant to chloroquine, pyrimethamine and mefloquine. ✖	Parasite growth inhibition assay	-	-	7.8	pIC₅₀	9
⤷	pIC₅₀ 7.8 (IC₅₀ 1.75x10^-8 M) [9] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
FNDR-20123		PfK1 Plasmodium falciparum K1 P. falciparum strain K1 (PfK1) was isolated in Kanchanaburi, Thailand in 1979. PfK1 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is reported to be a multidrug-resistant strain. ✖	Parasite growth inhibition assay	-	-	7.7	pIC₅₀	9
⤷	pIC₅₀ 7.7 (IC₅₀ 1.905x10^-8 M) [9] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
compound 1u [PMID: 30245402]		Pb Plasmodium berghei P. berghei (Pb) is a malaria parasite that infects mammals other than humans with the natural mammalian host being the thicket rat (G. surdaster) from Central Africa. Pb is used in rodent model studies of malaria. ✖	Parasite liver stage assay	-	-	7.6	pIC₅₀	3
⤷	pIC₅₀ 7.6 (IC₅₀ 2.5x10^-8 M) P. berghei Luciferase liver stage assay [3] Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
FNDR-20123		PfNF54 Plasmodium falciparum NF54 P. falciparum strain NF54 (PfNF54) was derived from a patient who had never left the Netherlands. PfNF54 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is sensitive to a panel of antimalarial compounds including chloroquine and pyrimethamine. ✖	Parasite growth inhibition assay	-	-	7.6	pIC₅₀	9
⤷	pIC₅₀ 7.6 (IC₅₀ 2.527x10^-8 M) [9] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
panobinostat		PfDd2 Plasmodium falciparum Dd2 P. falciparum strain Dd2 (PfDd2) is a clone derived from PfW2, following continuous culture in mefloquine. PfW2 was cloned from the Indochina III/CDC isolate, originally derived from a Laotian patient who failed chloroquine therapy. PfDd2 can be obtained from the Malaria Research and Reference Reagent Resource Center (MR4) and is reported to be resistant to chloroquine, pyrimethamine and mefloquine. ✖	Parasite growth inhibition assay	-	-	7.5	pIC₅₀	4
⤷	pIC₅₀ 7.5 (IC₅₀ 3x10^-8 M) [³H]-hypoxanthine incorporation [4] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
FNDR-20123		Pf3D7 Plasmodium falciparum 3D7 P. falciparum strain 3D7 (Pf3D7) was derived from isolate NF54 by limiting dilution. The complete genome of Pf3D7 has been sequenced (GenBank: LN999946.1). Pf3D7 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is sensitive to a panel of antimalarial compounds including chloroquine and pyrimethamine. ✖	Parasite growth inhibition assay	-	-	7.4	pIC₅₀	9
⤷	pIC₅₀ 7.4 (IC₅₀ 4.1x10^-8 M) SYBR Green assay [9] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
panobinostat		PfHB3 Plasmodium falciparum HB3 P. falciparum strain HB3 (PfHB3) was cloned from the Honduras I/CDC strain, originally isolated from a patient in Choluteca, Honduras, during an outbreak of urban malaria in January 1980. PfHB3 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is reported to be chloroquine sensitive. ✖	Parasite gametocyte viability assay	-	-	6.9	pIC₅₀	10
⤷	pIC₅₀ 6.9 (IC₅₀ 1.18x10^-7 M) AlamarBlue viability assay [10] Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
panobinostat		PfDd2 Plasmodium falciparum Dd2 P. falciparum strain Dd2 (PfDd2) is a clone derived from PfW2, following continuous culture in mefloquine. PfW2 was cloned from the Indochina III/CDC isolate, originally derived from a Laotian patient who failed chloroquine therapy. PfDd2 can be obtained from the Malaria Research and Reference Reagent Resource Center (MR4) and is reported to be resistant to chloroquine, pyrimethamine and mefloquine. ✖	Parasite gametocyte viability assay	-	-	6.8	pIC₅₀	10
⤷	pIC₅₀ 6.8 (IC₅₀ 1.48x10^-7 M) AlamarBlue viability assay [10] Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
FNDR-20123		Pf Plasmodium falciparum P. falciparum (Pf) is one of five protozoan parasite species of the genus Plasmodium that cause malaria in humans. Pf is responsible for the majority of malaria related deaths and is the most prevalent species in sub-Saharan Africa. ✖	Parasite dual gamete formation assay (DGFA)	-	-	6.7	pIC₅₀	9
⤷	pIC₅₀ 6.7 (IC₅₀ 1.9x10^-7 M) Activity against male gametocytes. IC₅₀ values of 190 nM for male and > 5 µM for female gametocytes [9] Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
panobinostat		Pf3D7 Plasmodium falciparum 3D7 P. falciparum strain 3D7 (Pf3D7) was derived from isolate NF54 by limiting dilution. The complete genome of Pf3D7 has been sequenced (GenBank: LN999946.1). Pf3D7 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is sensitive to a panel of antimalarial compounds including chloroquine and pyrimethamine. ✖	Parasite gametocyte viability assay	-	-	6.0	pIC₅₀	10
⤷	pIC₅₀ 6.0 (IC₅₀ 9.35x10^-7 M) AlamarBlue viability assay [10] Lifecycle stages: Plasmodium sexual blood stage (gametocyte)

Malaria Pharmacology Comments
The histone deacetylase (HDAC) family of enzymes are involved in the post-translational modification of histones by removal of acetyl groups from lysine residues. Removal of the acetyl groups facilitates tighter packing of chromatin (heterochromatin formation) leading to transcriptional repression. In humans, the 18 members of the HDAC family have been classified in to five subfamilies based on phylogenetic comparison with yeast homologues (see our HDACs Concise family page for more details). A recent review and analysis of the P. falciparum genome confirmed and classified the five known HDACs for this species of the parasite and identified a novel putative HDAC [7]: Class I contains PfHDAC1 Class II contains PfHDA1 and PfHDA2 Class III contains the sirtuin-like PfSir2A and PfSir2B PfCHD1 is a novel unclassified HDAC This family of enzymes has been shown to be involved in the regulation of a number of processes during development of the malaria parasite including schizogony, gemetocytogenesis , antigenic variation and hepatocyte invasion. HDACs have been identified as attractive molecular targets in the search for novel mechanisms to treat cancer and several small molecule HDAC inhibitors are already approved for clinical use. HDAC inhibitors have also emerged as potential therapies in a number of other disesases including malaria [1,4-5].

Malaria Pharmacology Comments

The histone deacetylase (HDAC) family of enzymes are involved in the post-translational modification of histones by removal of acetyl groups from lysine residues. Removal of the acetyl groups facilitates tighter packing of chromatin (heterochromatin formation) leading to transcriptional repression. In humans, the 18 members of the HDAC family have been classified in to five subfamilies based on phylogenetic comparison with yeast homologues (see our HDACs Concise family page for more details). A recent review and analysis of the P. falciparum genome confirmed and classified the five known HDACs for this species of the parasite and identified a novel putative HDAC [7]:
Class I contains PfHDAC1
Class II contains PfHDA1 and PfHDA2
Class III contains the sirtuin-like PfSir2A and PfSir2B
PfCHD1 is a novel unclassified HDAC
This family of enzymes has been shown to be involved in the regulation of a number of processes during development of the malaria parasite including schizogony, gemetocytogenesis , antigenic variation and hepatocyte invasion.
HDACs have been identified as attractive molecular targets in the search for novel mechanisms to treat cancer and several small molecule HDAC inhibitors are already approved for clinical use. HDAC inhibitors have also emerged as potential therapies in a number of other disesases including malaria [1,4-5].

References

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1. Andrews KT, Tran TN, Lucke AJ, Kahnberg P, Le GT, Boyle GM, Gardiner DL, Skinner-Adams TS, Fairlie DP. (2008) Potent antimalarial activity of histone deacetylase inhibitor analogues. Antimicrob Agents Chemother, 52 (4): 1454-61. [PMID:18212103]

2. Chua MJ, Arnold MS, Xu W, Lancelot J, Lamotte S, Späth GF, Prina E, Pierce RJ, Fairlie DP, Skinner-Adams TS et al.. (2017) Effect of clinically approved HDAC inhibitors on Plasmodium, Leishmania and Schistosoma parasite growth. Int J Parasitol Drugs Drug Resist, 7 (1): 42-50. [PMID:28107750]

3. Diedrich D, Stenzel K, Hesping E, Antonova-Koch Y, Gebru T, Duffy S, Fisher G, Schöler A, Meister S, Kurz T et al.. (2018) One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. Eur J Med Chem, 158: 801-813. [PMID:30245402]

4. Engel JA, Jones AJ, Avery VM, Sumanadasa SD, Ng SS, Fairlie DP, Skinner-Adams T, Andrews KT. (2015) Profiling the anti-protozoal activity of anti-cancer HDAC inhibitors against Plasmodium and Trypanosoma parasites. Int J Parasitol Drugs Drug Resist, 5 (3): 117-26. [PMID:26199860]

5. Hansen FK, Sumanadasa SD, Stenzel K, Duffy S, Meister S, Marek L, Schmetter R, Kuna K, Hamacher A, Mordmüller B et al.. (2014) Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. Eur J Med Chem, 82: 204-13. [PMID:24904967]

6. Huang Z, Li R, Tang T, Ling D, Wang M, Xu D, Sun M, Zheng L, Zhu F, Min H et al.. (2020) A novel multistage antiplasmodial inhibitor targeting Plasmodium falciparum histone deacetylase 1. Cell Discov, 6 (1): 93. [PMID:33311461]

7. Kanyal A, Rawat M, Gurung P, Choubey D, Anamika K, Karmodiya K. (2018) Genome-wide survey and phylogenetic analysis of histone acetyltransferases and histone deacetylases of Plasmodium falciparum. FEBS J, 285 (10): 1767-1782. [PMID:29284196]

8. Mackwitz MKW, Hesping E, Antonova-Koch Y, Diedrich D, Woldearegai TG, Skinner-Adams T, Clarke M, Schöler A, Limbach L, Kurz T et al.. (2019) Structure-Activity and Structure-Toxicity Relationships of Peptoid-Based Histone Deacetylase Inhibitors with Dual-Stage Antiplasmodial Activity. ChemMedChem, 14 (9): 912-926. [PMID:30664827]

9. Potluri V, Shandil RK, Gavara R, Sambasivam G, Campo B, Wittlin S, Narayanan S. (2020) Discovery of FNDR-20123, a histone deacetylase inhibitor for the treatment of Plasmodium falciparum malaria. Malar J, 19 (1): 365. [PMID:33046062]

10. Sun W, Tanaka TQ, Magle CT, Huang W, Southall N, Huang R, Dehdashti SJ, McKew JC, Williamson KC, Zheng W. (2014) Chemical signatures and new drug targets for gametocytocidal drug development. Sci Rep, 4: 3743. [PMID:24434750]

11. Wang M, Tang T, Li R, Huang Z, Ling D, Zheng L, Ding Y, Liu T, Xu W, Zhu F et al.. (2022) Drug Repurposing of Quisinostat to Discover Novel Plasmodium falciparum HDAC1 Inhibitors with Enhanced Triple-Stage Antimalarial Activity and Improved Safety. J Med Chem, 65 (5): 4156-4181. [PMID:35175762]

How to cite this page

Chromatin modifying enzymes (Plasmodium spp.): Plasmodium falciparum histone deacetylase 1. Last modified on 30/03/2022. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=3072.