Recombinant Human Abhydrolase domain-containing protein 3 (ABHD3)
Description
Introduction to Recombinant Human Abhydrolase Domain-Containing Protein 3 (ABHD3)
Recombinant Human Abhydrolase domain-containing protein 3 (ABHD3), also known as lung α/β-hydrolase 3 (LABH3), is a serine hydrolase enzyme that, in humans, is encoded by the ABHD3 gene . It belongs to the α/β-hydrolase domain (ABHD) superfamily of proteins, a diverse group involved in lipid metabolism, signaling, and regulation . ABHD3 is a 409-amino acid protein with a molecular weight of approximately 46 kDa . It is highly expressed in tissues such as the appendix, colon, gall bladder, lymph nodes, stomach, thyroid, small intestine, and duodenum .
Biochemical Features and Biological Roles
ABHD3 is involved in the catabolism of medium-chain phospholipids, distinguishing it from other known phospholipases . It demonstrates specificity towards phosphatidylcholines (PCs) containing a C14 acyl chain and oxidatively truncated phospholipids . Metabolomic studies have confirmed that ABHD3 inhibition leads to an increase of medium-chain PCs in human cells . ABHD3 displays activity with C5-C8 substrates and oxidatively truncated PCs (oxPCs), such as azPAF (1-hexadecyl-2-azelaoyl-glycerol-3-phosphocholine) .
ABHD3 in Lipid Metabolism
ABHD3 plays a multifaceted role in the catabolism of medium-chain phospholipids, a role distinct from other known phospholipases . It selectively cleaves medium-chain and oxidatively-truncated phospholipids . ABHD3-deficient mice exhibit elevated myristoyl (C14)-phospholipids, including C14-lysophosphatidylcholine, which confirms the physiological relevance of ABHD3's substrate assignments .
Inhibitors of ABHD3
Several compounds have been identified as inhibitors of ABHD3 . These inhibitors can be categorized as follows:
Clinical Significance and Pathological Conditions
ABHD3 is upregulated in several pathological conditions, including human ovarian cancer cell lines exposed to standard treatments . Genome-wide association studies have identified associations between the ABHD3 gene and plasma lipid levels, suggesting a role in lipid-related diseases .
Table Summarizing Key ABHD3 Inhibitors
| Inhibitor | $$IC_{50}$$ (μM) | Selectivity | Mechanism |
|---|---|---|---|
| β-aminocyano(MIDA)boronate 2 | 0.14 | Selective for ABHD3, >95% blockade at 0.5 μM without affecting 60 other serine hydrolases in SW620 cells | Covalent inhibition via boron atom |
| N-hydroxyhydantoin carbamate 5 (ABC47) | 0.1 | Inhibits ABHD3, ABHD4, ABHD6, HSL, PLA2G7, and CES2 | Unknown |
| N-hydroxyhydantoin carbamate 6 (ABC34) | 7.6 | Inhibits ABHD3, ABHD4, ABHD6, HSL, PLA2G7, and CES2 | Unknown |
| Compound 45 | N/A | Complete inhibition of ABHD10 with few off-targets, near-complete inactivation of ABHD10 at 10 μM and of ACOT1/2 at 100 μM, CPVL inhibition confirmed | Conversion into corresponding boronic acid is required |
Product Specs
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Target Background
Recombinant Human Abhydrolase domain-containing protein 3 (ABHD3) is a phospholipase potentially involved in phospholipid remodeling. It exhibits preferential phospholipase A1 activity, selectively cleaving myristate (C14)-containing phosphatidylcholines, primarily targeting acyl groups at the sn1 position. Minor phospholipase A2 activity on sn2 acyl groups may also occur. Beyond (C14)-containing phosphatidylcholines, ABHD3 may also act on other medium-chain-containing and oxidatively truncated phospholipids.
