Jeffrey S Albert
Overview
Explore the profile of Jeffrey S Albert including associated specialties, affiliations and a list of published articles.
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18
Citations
146
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Recent Articles
1.
Canterbury D, Godin F, Desjardins S, Bayrakdarian M, Albert J, Perry D, et al.
Org Lett
. 2018 Aug;
20(17):5336-5339.
PMID: 30118238
A practical and asymmetric synthesis of a small-molecule CXCR7 modulator featuring a highly functionalized and hindered tertiary β-amino amide framework is reported. The cornerstone of this strategy relied on the...
2.
Varnes J, Xiong H, Forst J, Holmquist C, Ernst G, Frietze W, et al.
Bioorg Med Chem Lett
. 2018 Mar;
28(6):1043-1049.
PMID: 29486970
A series of isoquinuclidine benzamides as glycine uptake inhibitors for the treatment of schizophrenia are described. Potency, lipophilicity, and intrinsic human microsomal clearance were parameters for optimization. Potency correlated with...
3.
Malmquist J, Varnas K, Svedberg M, Vallee F, Albert J, Finnema S, et al.
ACS Chem Neurosci
. 2017 Oct;
9(2):224-229.
PMID: 29072902
Positron emission tomography (PET), together with a suitable radioligand, is one of the more prominent methods for measuring changes in synaptic neurotransmitter concentrations in vivo. The radioligand of choice for...
4.
Johnstone S, Albert J
Bioorg Med Chem Lett
. 2017 Apr;
27(11):2239-2258.
PMID: 28408223
New strategies to potentially improve drug safety and efficacy emerge with allosteric programs. Biased allosteric modulators can be designed with high subtype selectivity and defined receptor signaling endpoints, however, selecting...
5.
Varnes J, Geschwindner S, Holmquist C, Forst J, Wang X, Dekker N, et al.
Bioorg Med Chem Lett
. 2015 Nov;
26(1):197-202.
PMID: 26597534
Fragment-based drug design (FBDD) relies on direct elaboration of fragment hits and typically requires high resolution structural information to guide optimization. In fragment-assisted drug discovery (FADD), fragments provide information to...
6.
Laliberte S, Vallee F, Fournier P, Bedard L, Labrecque J, Albert J
Bioorg Med Chem Lett
. 2014 Jun;
24(14):3204-6.
PMID: 24880903
We describe the discovery and advancement of a novel series of TRPA1 antagonist having an aryl-N-(3-(alkylamino)-5-(trifluoromethyl)phenyl)benzamide scaffold. The physical and in vitro DMPK profiles are discussed.
7.
Hu Y, St-Onge M, Laliberte S, Vallee F, Jin S, Bedard L, et al.
Bioorg Med Chem Lett
. 2014 May;
24(14):3199-203.
PMID: 24835202
A series of TRPA1 antagonists is described having a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine or a 1-aryloxyisoquinoline scaffold. These compounds have high ligand efficiency and favorable physical properties and may thus serve as scaffolds...
8.
Geschwindner S, Dekker N, Horsefield R, Tigerstrom A, Johansson P, Scott C, et al.
J Med Chem
. 2013 Mar;
56(8):3228-34.
PMID: 23509991
We describe the development of a novel fragment screening methodology employing a plate-based optical biosensor system that can operate in a 384-well format. The method is based on the "inhibition...
9.
Radresa O, Pare M, Albert J
Curr Top Med Chem
. 2013 Feb;
13(3):367-85.
PMID: 23432066
During inflammation, several Transient Receptor Potential (TRP) channels are directly or indirectly activated by inflammatory signaling molecules and microenvironmental changes including heat, oxidative conditions or low pH. In either case,...
10.
Albert J
Prog Med Chem
. 2011 May;
48:133-61.
PMID: 21544959
Since the original identification of BACE in 1999 and until quite recently, BACE was often regarded as a "difficult" drug target, much as renin has proven to be. The reasons...