Bradley A Zinker
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Explore the profile of Bradley A Zinker including associated specialties, affiliations and a list of published articles.
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26
Citations
398
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Recent Articles
1.
Jurica E, Wu X, Williams K, Haque L, Rampulla R, Mathur A, et al.
Bioorg Med Chem
. 2023 Apr;
85:117273.
PMID: 37030194
GPR40 AgoPAMs are highly effective antidiabetic agents that have a dual mechanism of action, stimulating both glucose-dependent insulin and GLP-1 secretion. The early lipophilic, aromatic pyrrolidine and dihydropyrazole GPR40 AgoPAMs...
2.
Cheng D, Zinker B, Luo Y, Shipkova P, De Oliveira C, Krishna G, et al.
Cell Metab
. 2022 Nov;
34(11):1732-1748.e5.
PMID: 36323235
Monoacylglycerol acyltransferase 2 (MGAT2) is an important enzyme highly expressed in the human small intestine and liver for the regulation of triglyceride absorption and homeostasis. We report that treatment with...
3.
Shi Y, Wang Y, Meng W, Brigance R, Ryono D, Bolton S, et al.
J Med Chem
. 2022 Feb;
65(5):4291-4317.
PMID: 35179904
Glucokinase (GK) is a key regulator of glucose homeostasis, and its small-molecule activators represent a promising opportunity for the treatment of type 2 diabetes. Several GK activators have been advanced...
4.
Cheng P, Kaltenbach 3rd R, Zhang H, Shi J, Tao S, Li J, et al.
J Med Chem
. 2021 Oct;
64(21):15549-15581.
PMID: 34709814
The oxycyclohexyl acid BMS-986278 () is a potent lysophosphatidic acid receptor 1 (LPA) antagonist, with a human LPA of 6.9 nM. The structure-activity relationship (SAR) studies starting from the LPA...
5.
Chatterjee S, Mukherjee S, Sankara Sivaprasad L, Naik T, Gautam S, Murali B, et al.
J Pharmacol Exp Ther
. 2020 Oct;
376(1):29-39.
PMID: 33127749
Expression and functional changes in the organic anion transporting polypeptide (OATP)-multidrug resistance-associated protein (MRP) axis of transporters are well reported in patients with nonalcoholic steatohepatitis (NASH). These changes can impact...
6.
Shi J, Gu Z, Jurica E, Wu X, Haque L, Williams K, et al.
J Med Chem
. 2018 Jan;
61(3):681-694.
PMID: 29316397
G protein-coupled receptor 40 (GPR40) has become an attractive target for the treatment of diabetes since it was shown clinically to promote glucose-stimulated insulin secretion. Herein, we report our efforts...
7.
Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode
Jurica E, Wu X, Williams K, Hernandez A, Nirschl D, Rampulla R, et al.
J Med Chem
. 2017 Jan;
60(4):1417-1431.
PMID: 28112924
A novel series of pyrrolidine-containing GPR40 agonists is described as a potential treatment for type 2 diabetes. The initial pyrrolidine hit was modified by moving the position of the carboxylic...
8.
Waring J, Yang Y, Healan-Greenberg C, Adler A, Dickinson R, McNally T, et al.
J Pharmacol Exp Ther
. 2007 Nov;
324(2):507-16.
PMID: 18025247
Acetyl CoA carboxylase (ACC) 2, which catalyzes the carboxylation of acetyl-CoA to form malonyl-CoA, has been identified as a potential target for type 2 diabetes and obesity. Small-molecule inhibitors of...
9.
Backes B, Longenecker K, Hamilton G, Stewart K, Lai C, Kopecka H, et al.
Bioorg Med Chem Lett
. 2007 Feb;
17(7):2005-12.
PMID: 17276063
A novel series of pyrrolidine-constrained phenethylamines were developed as dipeptidyl peptidase IV (DPP4) inhibitors for the treatment of type 2 diabetes. The cyclohexene ring of lead-like screening hit 5 was...
10.
Pei Z, Li X, von Geldern T, Madar D, Longenecker K, Yong H, et al.
J Med Chem
. 2006 Oct;
49(22):6439-42.
PMID: 17064063
Dipeptidyl peptidase IV (DPP4) deactivates glucose-regulating hormones such as GLP-1 and GIP, thus, DPP4 inhibition has become a useful therapy for type 2 diabetes. Optimization of the high-throughput screening lead...