Xiao Xunjun, Lowe Mark E
From the Department of Pediatrics, Children's Hospital of Pittsburgh at University of Pittsburgh Medical Center, Pittsburgh, Pennsylvania 15224.
From the Department of Pediatrics, Children's Hospital of Pittsburgh at University of Pittsburgh Medical Center, Pittsburgh, Pennsylvania 15224
J Biol Chem. 2015 Nov 27;290(48):28847-56. doi: 10.1074/jbc.M115.683375. Epub 2015 Oct 21.
Pancreatic triglyceride lipase (PNLIP) is essential for dietary fat digestion in children and adults, whereas a homolog, pancreatic lipase-related protein 2 (PNLIPRP2), is critical in newborns. The two lipases are structurally similar, yet they have different substrate specificities. PNLIP only cleaves neutral fats. PNLIPRP2 cleaves neutral and polar fats. To test the hypothesis that the differences in activity between PNLIP and PNLIPRP2 are governed by surface loops around the active site, we created multiple chimeras of both lipases by exchanging the surface loops singly or in combination. The chimeras were expressed, purified, and tested for activity against various substrates. The structural determinants of PNLIPRP2 galactolipase activity were contained in the N-terminal domain. Of the surface loops tested, the lid domain and the β5-loop influenced activity against triglycerides and galactolipids. Any chimera on PNLIP with the PNLIPRP2 lid domain or β5-loop had decreased triglyceride lipase activity similar to that of PNLIPRP2. The corresponding chimeras of PNLIPRP2 did not increase activity against neutral lipids. Galactolipase activity was abolished by the PNLIP β5-loop and decreased by the PNLIP lid domain. The source of the β9-loop had minimal effect on activity. We conclude that the lid domain and β5-loop contribute to substrate specificity but do not completely account for the differing activities of PNLIP and PNLIPRP2. Other regions in the N-terminal domain must contribute to the galactolipase activity of PNLIPRP2 through direct interactions with the substrate or by altering the conformation of the residues surrounding the hydrophilic cavity in PNLIPRP2.
胰腺甘油三酯脂肪酶(PNLIP)对儿童和成人的膳食脂肪消化至关重要,而其同源物胰腺脂肪酶相关蛋白2(PNLIPRP2)对新生儿至关重要。这两种脂肪酶结构相似,但底物特异性不同。PNLIP仅裂解中性脂肪。PNLIPRP2裂解中性和极性脂肪。为了验证PNLIP和PNLIPRP2之间活性差异受活性位点周围表面环调控的假说,我们通过单独或组合交换表面环,构建了两种脂肪酶的多个嵌合体。对嵌合体进行表达、纯化,并测试其对各种底物的活性。PNLIPRP2半乳糖脂酶活性的结构决定因素存在于N端结构域中。在所测试的表面环中,盖子结构域和β5环影响对甘油三酯和半乳糖脂的活性。任何带有PNLIPRP2盖子结构域或β5环的PNLIP嵌合体,其甘油三酯脂肪酶活性均降低,类似于PNLIPRP2。PNLIPRP2的相应嵌合体对中性脂质的活性并未增加。PNLIP的β5环消除了半乳糖脂酶活性,PNLIP的盖子结构域降低了该活性。β9环的来源对活性影响最小。我们得出结论,盖子结构域和β5环有助于底物特异性,但不能完全解释PNLIP和PNLIPRP2活性的差异。N端结构域中的其他区域必须通过与底物直接相互作用或改变PNLIPRP2亲水腔周围残基的构象,来促进PNLIPRP2的半乳糖脂酶活性。