David R Janero
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Explore the profile of David R Janero including associated specialties, affiliations and a list of published articles.
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71
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1088
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Recent Articles
1.
Janero D
Expert Opin Drug Discov
. 2023 Nov;
19(2):147-159.
PMID: 37936504
Introduction: Escalating costs and inherent uncertainties associated with drug discovery invite initiatives to improve its efficiency and de-risk campaigns for inventing better therapeutics. One such initiative involves recognizing and exploiting...
2.
Garai S, Schaffer P, Laprairie R, Janero D, Pertwee R, Straiker A, et al.
Bioorg Med Chem
. 2021 Oct;
50:116421.
PMID: 34634617
Allosteric modulators of cannabinoid 1 receptor (CB1R) show translational promise over orthosteric ligands due to their potential to elicit therapeutic benefit without cannabimimetic side effects. The prototypic 2-phenylindole CB1R allosteric...
3.
Garai S, Leo L, Szczesniak A, Hurst D, Schaffer P, Zagzoog A, et al.
J Med Chem
. 2021 Apr;
64(12):8104-8126.
PMID: 33826336
We apply the magic methyl effect to improve the potency/efficacy of GAT211, the prototypic 2-phenylindole-based cannabinoid type-1 receptor (CB1R) agonist-positive allosteric modulator (ago-PAM). Introducing a methyl group at the α-position...
4.
5.
Schaffer P, Kulkarni P, Janero D, Thakur G
Bioorg Med Chem
. 2020 Oct;
28(21):115727.
PMID: 33065437
Specific tuning of cannabinoid 1 receptor (CB1R) activity by small-molecule allosteric modulators is a therapeutic modality with multiple properties inherently advantageous to therapeutic applications. We previously generated a library of...
6.
Garai S, Kulkarni P, Schaffer P, Leo L, Brandt A, Zagzoog A, et al.
J Med Chem
. 2019 Nov;
63(2):542-568.
PMID: 31756109
Cannabinoid 1 receptor (CB1R) allosteric ligands hold a far-reaching therapeutic promise. We report the application of fluoro- and nitrogen-walk approaches to enhance the drug-like properties of GAT211, a prototype CB1R...
7.
Szymanski D, Papanastasiou M, Pandarinathan L, Zvonok N, Janero D, Pavlopoulos S, et al.
J Med Chem
. 2018 Nov;
61(24):11199-11208.
PMID: 30444608
Upon ultraviolet activation, cannabinergic aliphatic azido (N) ligands covalently label cannabinoid receptors, prominent G-protein-coupled receptor (GPCR) drug targets. We report here the mechanism of covalent attachment to selected substrates of...
8.
Karageorgos I, Silin V, Zvonok N, Marino J, Janero D, Makriyannis A
Anal Biochem
. 2017 Aug;
536:90-95.
PMID: 28822686
Human monoacylglycerol lipase (hMAGL) plays a key role in homeostatic tuning of the endocannabinoid signaling system and supports aggressive tumorogenesis, making this enzyme a promising therapeutic target. hMAGL features a...
9.
Kulkarni A, Garai S, Janero D, Thakur G
Methods Enzymol
. 2017 Jul;
593:281-315.
PMID: 28750808
Also expressed in various peripheral tissues, the type-1 cannabinoid receptor (CB1R) is the predominant G protein-coupled receptor (GPCR) in brain, where it is responsible for retrograde control of neurotransmitter release....
10.
Janero D, Korde A, Makriyannis A
Methods Enzymol
. 2017 Jul;
593:217-235.
PMID: 28750804
Detailed characterization of the ligand-binding motifs and structure-function correlates of the principal GPCRs of the endocannabinoid-signaling system, the cannabinoid 1 (CB1R) and cannabinoid 2 (CB2R) receptors, is essential to inform...