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Asparaginase


Asparaginase
Systematic (IUPAC) name
E. coli L-asparagine amidohydrolase
Identifiers
CAS number	9015-68-3
ATC code	L01XX02
PubChem	?
DrugBank	BTD00011
Chemical data
Formula	C₁₃₇₇H₂₂₀₈N₃₈₂O₄₄₂S₁₇
Mol. mass	31731.9 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	8-30 hrs
Excretion	?
Therapeutic considerations
Pregnancy cat.	C(US)
Legal status
Routes	?

Asparaginase (EC 3.5.1.1) is an enzyme that catalyzes the hydrolysis of asparagine to aspartic acid. It is also marketed under the brand names Elspar®, Oncaspar, and Erwinase to treat acute lymphoblastic leukemia (ALL) and is also used in some mast cell tumor protocols. ^[1] Unlike other chemotherapy agents, it can be given as an intramuscular, subcutaneous, or intravenous injection without fear of tissue irritation.

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Mechanism of action

The rationale behind asparaginase is that it takes advantage of the fact that ALL leukemic cells are unable to synthesize the non-essential amino acid asparagine whereas normal cells are able to make their own asparagine. These leukemic cells depend on circulating asparagine. Asparaginase however catalyzes the conversion of L-asparagine to aspartic acid and ammonia. This deprives the leukemic cell of circulating asparagine.

Side effects

The main side effect is an allergic or hypersensitivity reaction. Asparaginase has also been associated with pancreatitis. Additionally, it can also be associated with a coagulopathy as it decreases protein synthesis, including synthesis of coagulation factors and anticoagulant factor, leading to bleeding or thrombotic events such as stroke.

References

^ Appel IM, van Kessel-Bakvis C, Stigter R, Pieters R (2007). "Influence of two different regimens of concomitant treatment with asparaginase and dexamethasone on hemostasis in childhood acute lymphoblastic leukemia". doi:10.1038/sj.leu.2404793. PMID 17554375.

v • d • e Chemotherapeutic agents/Antineoplastic agents (L01)
Alkylating and alkylating-like agents	Nitrogen mustards: (Chlorambucil, Chlormethine, Cyclophosphamide, Ifosfamide, Melphalan). Nitrosoureas:(Carmustine, Fotemustine, Lomustine, Streptozocin). Platinum (alkylating-like): (Carboplatin, Cisplatin, Oxaliplatin, BBR3464). Busulfan, Dacarbazine, Procarbazine, Temozolomide, ThioTEPA, Uramustine
Antimetabolites	Folic acid: (Aminopterin, Methotrexate, Pemetrexed, Raltitrexed). Purine:(Cladribine, Clofarabine, Fludarabine, Mercaptopurine, Pentostatin, Thioguanine). Pyrimidine:(Capecitabine, Cytarabine, Fluorouracil, Floxuridine, Gemcitabine)
Spindle poison/mitotic inhibitor	Taxane: (Docetaxel, Paclitaxel). Vinca: (Vinblastine, Vincristine, Vindesine, Vinorelbine).
Cytotoxic/antitumor antibiotics	Anthracycline family: (Daunorubicin, Doxorubicin, Epirubicin, Idarubicin, Mitoxantrone, Valrubicin) - streptomyces (Actinomycin, Bleomycin, Mitomycin, Plicamycin) - Hydroxyurea
Topoisomerase inhibitors	Camptotheca: (Camptothecin, Topotecan, Irinotecan), Podophyllum:(Etoposide, Teniposide)
CI monoclonal antibodies	Receptor tyrosine kinase (Cetuximab, Panitumumab, Trastuzumab) - CD20 (Rituximab, Tositumomab) - other (Alemtuzumab, Bevacizumab, Gemtuzumab)
Photosensitizers	Aminolevulinic acid, Methyl aminolevulinate, Porfimer sodium, Verteporfin
Tyrosine kinase inhibitors	Dasatinib, Erlotinib, Gefitinib, Imatinib, Lapatinib, Nilotinib, Sorafenib, Sunitinib
Other	retinoids (Alitretinoin, Tretinoin) - Altretamine, Amsacrine, Anagrelide, Arsenic trioxide, Asparaginase (Pegaspargase), Bexarotene, Bortezomib, Denileukin diftitox, Estramustine, Ixabepilone, Masoprocol, Mitotane

v • d • e Carbon-nitrogen non-peptide hydrolases (EC 3.5)
3.5.1 - Amidohydrolases	Asparaginase - Glutaminase - Urease - Biotinidase - Aspartoacylase - Ceramidase -Aspartylglucosaminidase - Fatty acid amide hydrolase - Histone deacetylase (Sirtuin)
3.5.2	Barbiturase - Beta-lactamase
3.5.3	Arginase
3.5.4 - Aminohydrolases	Guanine deaminase - Adenosine deaminase - AMP deaminase - Inosine monophosphate synthase - DCMP deaminase - GTP cyclohydrolase I
Other	Nitrilase - Thiaminase II

v • d • e Amino acid metabolism enzymes
phenylalanine→tyrosine→fumarate→TCA	Phenylalanine hydroxylase - Tyrosine aminotransferase - 4-Hydroxyphenylpyruvate dioxygenase - Homogentisate 1,2-dioxygenase - Fumarylacetoacetate hydrolase
tyrosine→dopamine→epinephrine	Tyrosine hydroxylase - Aromatic L-amino acid decarboxylase - Dopamine beta hydroxylase - Phenylethanolamine N-methyltransferase
leucine→HMG-CoA (keto)	Branched-chain alpha-keto acid dehydrogenase complex - Isovaleryl coenzyme A dehydrogenase - Methylcrotonyl-CoA carboxylase
isoleucine/valine→propionyl-CoA	Branched-chain alpha-keto acid dehydrogenase complex
methionine→cysteine→propionyl-CoA	Methionine adenosyltransferase - Adenosylhomocysteinase - (or MTR) - Cystathionine beta synthase - Cystathionine gamma-lyase
propionyl-CoA→succinyl-CoA→TCA	Propionyl-CoA carboxylase - Methylmalonyl-CoA mutase
serine→glycine	Serine hydroxymethyltransferase
histidine	to histamine: Histidine decarboxylase - to glutamate: Histidine ammonia-lyase - Urocanate hydratase - Formiminotransferase cyclodeaminase
tryptophan→serotonin→melatonin	Tryptophan hydroxylase - Aromatic L-amino acid decarboxylase - 5-hydroxyindole-O-methyltransferase
asparagine→aspartate→oxaloacetate→TCA	Asparaginase/Asparagine synthetase - Aspartate transaminase
glutamate	Glutaminase - Glutamate decarboxylase
lysine→keto	Saccharopine dehydrogenase
other	Tyrosinase

Categories: Chemotherapeutic adjuvants | EC 3.5.1

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Asparaginase". A list of authors is available in Wikipedia.