Trypanosoma
Trypanosoma spp. are divergent protozoan parasites that cause human African trypanosomiasis, Chagas disease, and animal trypanosomiasis[1][2]. Their core biology centers on stage-specific adaptation between mammalian hosts and insect vectors, requiring changes in morphology, organelle positioning, surface biology, and gene expression[2][3]. Mechanistically, kinetoplastids contain glycosomes that compartmentalize major glycolytic and pentose-phosphate enzymes, supporting energy and carbohydrate metabolism[4]. cAMP signaling differs from mammalian pathways because trypanosomatids lack G-protein-coupled receptors, possess structurally different adenylyl cyclases, and express class 1 cyclic nucleotide phosphodiesterases PDEA-D[5]. Compared with related isoforms, only T. brucei PDEB, expressed as PDEB1 and PDEB2, has been reported essential after ablation[5]. Disease models use T. brucei to study bloodstream infection, tsetse-vector differentiation, antigenic variation, cytokinesis, and drug discovery[2][3]. For experimental intervention, N-myristoyltransferase inhibition causes trypanosomatid cell death, compromises virulence, and cures T. brucei infection in rodents[6]. Neuropeptides also kill T. brucei by disrupting lysosome integrity, redistributing glycolytic enzymes, and inducing autophagic-like cell death[7].
References:
- [1]. Lopes AH, et al. Trypanosomatids: odd organisms, devastating diseases. Open Parasitol J. 2010;4:30-59.
- [2]. Dean S. Basic Biology of Trypanosoma brucei with Reference to the Development of Chemotherapies. Curr Pharm Des. 2021;27(14):1650-1670. [Content Brief]
- [3]. Matthews KR. The developmental cell biology of Trypanosoma brucei. J Cell Sci. 2005 Jan 15;118(Pt 2):283-90. doi: 10.1242/jcs.01649. Erratum in: J Cell Sci. 2005 May 1;118(Pt 9):2078. PMID: 15654017; PMCID: PMC2686837. et al. The developmental cell biology of Trypanosoma brucei. J Cell Sci. 2005 Jan 15;118(Pt 2):283-90. [Content Brief]
- [4]. Hannaert V, et al. Evolution of energy metabolism and its compartmentation in Kinetoplastida. Kinetoplastid Biology and Disease. 2003;2:11.
- [5]. Tagoe DN, et al. The ever unfolding story of cAMP signaling in trypanosomatids: vive la difference! Front Pharmacol. 2015 Sep 7;6:185. [Content Brief]
- [6]. Goldston AM, et al. Acylation in trypanosomatids: an essential process and potential drug target. Trends Parasitol. 2014 Jul;30(7):350-60. [Content Brief]
- [7]. Delgado M, et al. Neuropeptides kill African trypanosomes by targeting intracellular compartments and inducing autophagic-like cell death. Cell Death Differ. 2009 Mar;16(3):406-16. [Content Brief]
All Product Categories
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Trypanosoma Related Products (80)
Related Products (80)
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Fexinidazole
0 ImagesSynonyms: HOE 239Fexinidazole (HOE 239) is an orally active, potent nitroimidazole antitrypanosomal agent. Fexinidazole shows trypanocidal activity against T. brucei subspecies and strains with IC50s of 0.7-3.3 μM (0.2-0.9 μg/ml). Fexinidazol has the potential for human sleeping sickness (HAT) caused by infection with T. brucei.
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Ajugol
0 ImagesAjugol is an orally active iridoid glycoside found in the traditional Chinese medicine Leonurus japonicus. Ajugol is an autophagy activator. Ajugol activates TFEB-mediated autophagy and lysosomal biogenesis. Ajugol also has anti-inflammatory effects. Ajugol has great potential in the research of asthma, non-alcoholic fatty liver disease (NAFLD), and osteoarthritis.
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NPD-001
0 ImagesNPD-001 is a potent Trypanosoma brucei phosphodiesterases 1/2 (TbrPDEB1/2) inhibitor, with IC50 values of 4 and 3 nM, respectively. NPD-001 also inhibits hPDE4. NPD-001 can increase cAMP levels in parasites, prevent cytokinesis, and cause the parasites to form multinucleated, multi-flagellated cells that eventually lyse. NPD-001 can be used for the research of infection.
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Pafuramidine
0 ImagesSynonyms: DB289Pafuramidine (DB289) is an orally active proagent of Furamidine (HY-110137A). Pafuramidine is a potent anti-parasitic agent, can be used to research trypanosomiasis, Pneumocystis pneumonia and malaria.
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Nifurtimox
0 ImagesNifurtimox, an antiprotozoal agent, which is generally used for the treatment of infections with Trypanosoma cruzi, has been used in the therapy of neuroblastoma. Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH).
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α-Terpinene
0 ImagesCat. No.: HY-W020182CAS No.: 99-86-5Synonyms: Terpileneα-Terpinene (Terpilene) is a monoterpene found in the essential oils of a large variety of foods and aromatic plants such as Mentha piperita. α-Terpinene is active against Trypanosoma evansi and has the potential for trypanosomosis treatment. α-Terpinene has antioxidant and antifungal properties.
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Lupenone
0 ImagesLupenone is an orally active lupine-type triterpenoid that can be isolated from Musa basjoo. Lupenone Lupenone plays a role through the PI3K/Akt/mTOR and NF-κB signaling pathways. Lupenone has anti-inflammatory, antiviral, antidiabetic and anticancer activities.
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Justicidin B
0 ImagesJusticidin B is a potent anticancer lignan and proapoptotic agent. Justicidin B is also a bone resorption inhibitor, and has strong antiviral, fungicidal, antiprotozoal effects. Justicidin B significantly inhibits platelet aggregation.
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GNF6702
0 ImagesGNF6702 is a selective inhibitor of the kinetoplastid proteasome. GNF6702 clears parasites in murine models of leishmaniasis, Chagas disease, and human African trypanosomiasis.
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Cruzain-IN-1
0 ImagesCruzain-IN-1 is a covalent and reversible Cruzain inhibitor, with an IC50 of 10 nM.
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Antiparasitic agent-30
0 ImagesCat. No.: HY-179690CAS No.: 671754-20-4Antiparasitic agent-30 is a potent adenosine kinase TbrAK modulator and antitrypanosomal agent. Antiparasitic agent-30 exhibits significant inhibitory activity against Trypanosoma brucei rhodesiense, while enhancing the activity of recombinant TbrAK(EC50=38 nM, Ka=75 nM-497 nM). Antiparasitic agent-30 exerts its pharmacological effects by eliminating intrinsic substrate inhibition and hyperactivating TbrAK in Trypanosoma brucei rhodesiense. Antiparasitic agent-30 serves as a valuable tool molecule for studying acute African human trypanosomiasis (sleeping sickness).
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T.cruzi-IN-1
0 ImagesT.cruzi-IN-1 is a potent Trypanosoma cruzi inhibitor with an IC50 of 8 nM. T.cruzi-IN-1, a 4-trifluoromethyl substituted analog, has the potential for both the acute and chronic stages of Chagas disease.
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Diazepinomicin
0 ImagesCat. No.: HY-N6674CAS No.: 733035-26-2Synonyms: ECO-4601; TLN-4601; BU 4664LDiazepinomicin (ECO-4601) is an anticancer and antibacterial agent. Diazepinomicin can be produced by a Micromonospora strain. Diazepinomicin induces Apoptosis. Diazepinomicin inhibits the proteases Rhodesain and Cathepsin L at an IC50 of 70-90 μM. Diazepinomicin possesses anti-inflammatory and anti-tumor activity. Diazepinomicin has demonstrated activity against hepatocellular carcinoma. Diazepinomicin shows antiparasitic activity against trypomastigote forms of Trypanosoma brucei with an IC50 of 13.5 μM. Diazepinomicin exhibits moderate antibacterial activity against specific Gram-positive bacteria, with an MIC of approximately 32 μg/mL.
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Pentamidine-d4 dihydrochloride
0 ImagesSynonyms: MP-601205-d4 dihydrochloridePentamidine-d4 (dihydrochloride) is the deuterium labeled Pentamidine dihydrochloride. Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dihydrochloride has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
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SDZ285428
0 ImagesSDZ285428 is a CYP51 inhibitor. SDZ285428 inhibits Trypanosoma cruzi (TC) CYP51 with I/E2 <1 (5 min) and I/E2=9 (1 h). SDZ285428 inhibits Trypanosoma brucei (TB) CYP51 with I/E2 <1 (5 min) and I/E2=35 (1 h).
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7-Deazaguanosine
0 Images7-Deazaguanosine is a purine nucleoside analogue with antitrypanosomal activity.
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Pentamidine dimesylate
0 ImagesPentamidine (MP-601205) dimesylate is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dimesylate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dimesylate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dimesylate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
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NPD-1335
0 ImagesNPD1335 is a Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1) inhibitor with submicromolar activities against T. brucei parasites. NPD1335 displays a greatly improved cytotoxicity profile. NPD1335 increases intracellular cAMP levels and results in the distortion of the cell cycle and cell death. NPD-1335 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Antitrypanosomal agent 4
0 ImagesCat. No.: HY-146049CAS No.: 2456427-48-6Antitrypanosomal agent 4 (compound 19) is a potent and blood-brain barrier permeable antitrypanosomal agent. Antitrypanosomal agent 4 has good activity against Trypanosoma cruzi (T. cruzi) and Trypanosoma brucei brucei (T. b. brucei) with IC50s of 1.2 μM and 70 nM, respectively. Antitrypanosomal agent 4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
