David J Unett
Overview
Explore the profile of David J Unett including associated specialties, affiliations and a list of published articles.
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14
Citations
167
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Recent Articles
1.
Ren A, Zhu X, Feichtinger K, Lehman J, Kasem M, Schrader T, et al.
Bioorg Med Chem Lett
. 2020 Jan;
30(5):126929.
PMID: 31952960
A series of potential new 5-HT receptor scaffolds based on a simplification of the clinically studied, 5-HTR agonist vabicaserin, were designed. An in vivo feeding assay early in our screening...
2.
Gaidarov I, Adams J, Frazer J, Anthony T, Chen X, Gatlin J, et al.
Cell Signal
. 2018 Jun;
50:9-24.
PMID: 29928987
Angiotensin (1-7) has been reported to be a ligand for the GPCR MAS1. Small molecule MAS1 modulators have also been recently characterized. Aside from convincing evidence for MAS1 activation of...
3.
Gaidarov I, Anthony T, Gatlin J, Chen X, Mills D, Solomon M, et al.
Pharmacol Res
. 2018 Feb;
131:185-198.
PMID: 29471103
GPR84 is an orphan G-protein coupled receptor, expressed on monocytes, macrophages and neutrophils and is significantly upregulated by inflammatory stimuli. The physiological role of GPR84 remains largely unknown. Medium chain...
4.
Han S, Thoresen L, Jung J, Zhu X, Thatte J, Solomon M, et al.
ACS Med Chem Lett
. 2017 Dec;
8(12):1309-1313.
PMID: 29259753
The discovery of a novel, selective and fully efficacious CB agonist with satisfactory pharmacokinetic and pharmaceutical properties is described. Compound was efficacious in a rat model of osteoarthritis pain following...
5.
Tran T, Kramer B, Shin Y, Vallar P, Boatman P, Zou N, et al.
J Med Chem
. 2017 Jan;
60(3):913-927.
PMID: 28072531
The design and synthesis of a new series of potent non-prostanoid IP receptor agonists that showed oral efficacy in the rat monocrotaline model of pulmonary arterial hypertension (PAH) are described....
6.
Han S, Narayanan S, Kim S, Calderon I, Zhu X, Kawasaki A, et al.
Bioorg Med Chem Lett
. 2015 Jun;
25(15):3034-8.
PMID: 26048791
The design and optimization of a novel trans-1,4-dioxycyclohexane GPR119 agonist series is described. A lead compound 21 was found to be a potent and efficacious GPR119 agonist across species, and...
7.
Tran T, Shin Y, Kramer B, Choi J, Zou N, Vallar P, et al.
Bioorg Med Chem Lett
. 2015 Feb;
25(5):1030-5.
PMID: 25666818
The design and synthesis of two closely related series of prostacyclin receptor agonist compounds that showed excellent human IP receptor potency and efficacy is described. Compounds from this series showed...
8.
Buzard D, Lopez L, Moody J, Kawasaki A, Schrader T, Kasem M, et al.
ACS Med Chem Lett
. 2014 Dec;
5(12):1334-9.
PMID: 25516794
S1P1 is a validated target for treatment of autoimmune disease, and functional antagonists with superior safety and pharmacokinetic properties are being sought as second generation therapeutics. We describe the discovery...
9.
Buzard D, Kim S, Lopez L, Kawasaki A, Zhu X, Moody J, et al.
ACS Med Chem Lett
. 2014 Dec;
5(12):1313-7.
PMID: 25516790
APD334 was discovered as part of our internal effort to identify potent, centrally available, functional antagonists of the S1P1 receptor for use as next generation therapeutics for treating multiple sclerosis...
10.
Han S, Thoresen L, Zhu X, Narayanan S, Jung J, Strah-Pleynet S, et al.
Bioorg Med Chem Lett
. 2014 Dec;
25(2):322-6.
PMID: 25488844
The design and synthesis of novel 1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalen-4-carboxamide CB2 selective ligands for the potential treatment of pain is described. Compound (R,R)-25 has good balance between CB2 agonist potency and selectivity over...