Page 127 - 中国全科医学2022-20

·2556· http://www.chinagp.net E-mail:zgqkyx@chinagp.net.cn

1331. drudis.2013.09.011.
［30］ALEXIADOU K，TAN T M M. Gastrointestinal peptides as ［41］ANSARULLAH，LU Y，HOLSTEIN M，et al. Stimulating
therapeutic targets to mitigate obesity and metabolic syndrome［J］. β-cell regeneration by combining a GPR119 agonist with a DPP-
CurrDiabetes Rep，2020，20（7）：1-7. DOI：10.1007/s11892- IV inhibitor［J］. PLoS One，2013，8（1）：e53345. DOI：
020-01309-9. 10.1371/journal.pone.0053345.
［31］YANG P Y，ZOU H F，AMSO Z，et al. New generation ［42］LI G，HUAN Y，YUAN B K，et al. Discovery of novel xanthine
oxyntomodulin peptides with improved pharmacokinetic profiles compounds targeting DPP-IV and GPR119 as anti-diabetic
exhibit weight reducing and anti-steatotic properties in mice［J］. agents［J］. Eur J Med Chem，2016，124：103-116. DOI：
Bioconjug Chem，2020，31（4）：1167-1176. DOI：10.1021/acs. 10.1016/j.ejmech.2016.08.023.
bioconjchem.0c00093. ［43］HUAN Y，JIANG Q，LI G，et al. The dual DPP4 inhibitor and
［32］DING W X，WANG H Y，PENG L J，et al. Novel peptidic dual GPR119 agonist HBK001 regulates glycemic control and beta cell
GLP-1/glucagon receptor agonist alleviates diabetes and diabetic function ex and in vivo［J］. Sci Rep，2017，7（1）：4351.
complications in combination with low-intensity ultrasound［J］. Eur DOI：10.1038/s41598-017-04633-5.
Rev Med Pharmacol Sci，2020，24（23）：12423-12436. DOI： ［44］LI G，MENG B X，YUAN B K，et al. The optimization of xanthine
10.26355/eurrev_202012_24038. derivatives leading to HBK001 hydrochloride as a potent dual ligand
［33］LAFFERTY R A，O'HARTE F P M，IRWIN N，et al. Proglucagon- targeting DPP-IV and GPR119［J］. Eur J Med Chem，2020，
derived peptides as therapeutics［J］. Front Endocrinol（Lausanne）， 188：112017. DOI：10.1016/j.ejmech.2019.112017.
2021，12：689678. DOI：10.3389/fendo.2021.689678. ［45］BOUHAJJA H，ABDELHEDI R，AMOURI A，et al. Potential role
［34］KIM M K，CHEONG Y H，LEE S H，et al. A novel GPR119 of liver enzyme levels as predictive markers of glucose metabolism
agonist DA-1241 preserves pancreatic function via the suppression disorders in a Tunisian population［J］. Can J Physiol Pharmacol，
of ER stress and increased PDX1 expression［J］. Biomedecine 2018，96（11）：1171-1180. DOI：10.1139/cjpp-2017-0579.
Pharmacother，2021，144：112324. DOI：10.1016/j. ［46］SHIBABAW T，DESSIE G，MOLLA M D，et al. Assessment of
biopha.2021.112324. liver marker enzymes and its association with type 2 diabetes mellitus
［35］MATSUMOTO K，YOSHITOMI T，ISHIMOTO Y，et al. DS- in Northwest Ethiopia［J］. BMC Res Notes，2019，12（1）：
8500a，an orally available G protein-coupled receptor 119 agonist， 707. DOI：10.1186/s13104-019-4742-x.
upregulates glucagon-like peptide-1 and enhances glucose- ［47］KAZIERAD D J，BERGMAN A，TAN B，et al. Effects of multiple
dependent insulin secretion and improves glucose homeostasis in type ascending doses of the glucagon receptor antagonist PF-06291874 in
2 diabetic rats［J］. J Pharmacol Exp Ther，2018，367（3）： patients with type 2 diabetes mellitus［J］. Diabetes Obes Metab，
509-517. DOI：10.1124/jpet.118.250019. 2016，18（8）：795-802. DOI：10.1111/dom.12672.
［36］YAMADA Y，TERAUCHI Y，WATADA H，et al. Efficacy and ［48］GUZMAN C B，ZHANG X M，LIU R，et al. Treatment with
safety of GPR119 agonist DS-8500a in Japanese patients with type 2 LY2409021，a glucagon receptor antagonist，increases liver fat in
diabetes：a randomized，double-blind，placebo-controlled，12- patients with type 2 diabetes［J］. Diabetes Obes Metab，2017，19
week study［J］. AdvTher，2018，35（3）：367-381. DOI： （11）：1521-1528. DOI：10.1111/dom.12958.
10.1007/s12325-018-0668-2. ［49］KAZDA C M，FRIAS J，FOGA I，et al. Treatment with the
［37］TERAUCHI Y，YAMADA Y，WATADA H，et al. Efficacy and glucagon receptor antagonist LY2409021 increases ambulatory
safety of the G protein-coupled receptor 119 agonist DS-8500a in blood pressure in patients with type 2 diabetes［J］. Diabetes Obes
Japanese type 2 diabetes mellitus patients with inadequate glycemic Metab，2017，19（8）：1071-1077. DOI：10.1111/dom.12904.
control on sitagliptin：a phase 2 randomized placebo-controlled ［50］VAJDA E G，POTTER S C，FUJITAKI J M，et al. LGD-6972，
study［J］. J Diabetes Investig，2018，9（6）：1333-1341. a potent，orally-bioavailable，small molecule glucagon receptor
DOI：10.1111/jdi.12846. antagonist for the treatment of type 2 diabetes［J］. Diabetes，
［38］KATO M，FURUIE H，KAMIYAMA E，et al. Safety and 2012，61：A252.
pharmacokinetics of DS-8500a，a novel GPR119 agonist，after ［51］VAJDA E G，LOGAN D，LASSETER K，et al. Pharmacokinetics
multiple oral doses in healthy Japanese males［J］. Clin Drug and pharmacodynamics of single and multiple doses of the glucagon
Investig，2018，38（6）：519-525. DOI：10.1007/s40261-018- receptor antagonist LGD-6972 in healthy subjects and subjects with
0633-5. type 2 diabetes mellitus［J］. Diabetes Obes Metab，2017，19（1）：
［39］RITTER K，BUNING C，HALLAND N，et al. G protein- 24-32. DOI：10.1111/dom.12752.
coupled receptor 119 （GPR119） agonists for the treatment ［52］PETTUS J H，D'ALESSIO D，FRIAS J P，et al. Efficacy and safety
of diabetes：recent progress and prevailing challenges［J］. of the glucagon receptor antagonist RVT-1502 in type 2 diabetes
J Med Chem，2016，59（8）：3579-3592. DOI：10.1021/acs. uncontrolled on metformin monotherapy：a 12-week dose-ranging
jmedchem.5b01198. study［J］. Diabetes Care，2020，43（1）：161-168. DOI：
［40］KANG S U. GPR119 agonists：a promising approach for T2DM 10.2337/dc19-1328.
treatment? A SWOT analysis of GPR119［J］. Drug Discov ［53］HÆDERSDAL S，LUND A，MAAGENSEN H，et al. The glucagon
Today，2013，18（23/24）：1309-1315. DOI：10.1016/j. receptor antagonist LY2409021 has no effect on postprandial glucose