Jon R Appel
Overview
Explore the profile of Jon R Appel including associated specialties, affiliations and a list of published articles.
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Articles
23
Citations
256
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0
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Recent Articles
1.
Doering S, Freeman K, Debevec G, Geer P, Santos R, Lavoi T, et al.
J Med Chem
. 2023 May;
66(10):7063-7065.
PMID: 37155917
No abstract available.
2.
Doering S, Freeman K, Debevec G, Geer P, Santos R, Lavoi T, et al.
J Med Chem
. 2021 Apr;
64(9):5577-5592.
PMID: 33886285
The central melanocortin-3 and melanocortin-4 receptors (MC3R, MC4R) are key regulators of body weight and energy homeostasis. Herein, the discovery and characterization of first-in-class small molecule melanocortin agonists with selectivity...
3.
Doering S, Freeman K, Schnell S, Haslach E, Dirain M, Debevec G, et al.
J Med Chem
. 2017 Apr;
60(10):4342-4357.
PMID: 28453292
The centrally expressed melanocortin-3 and -4 receptors (MC3R/MC4R) have been studied as possible targets for weight management therapies, with a preponderance of studies focusing on the MC4R. Herein, a novel...
4.
Haslach E, Huang H, Dirain M, Debevec G, Geer P, Santos R, et al.
J Med Chem
. 2014 Feb;
57(11):4615-28.
PMID: 24517312
Human obesity has been linked to genetic factors and single nucleotide polymorphisms (SNPs). Melanocortin-4 receptor (MC4R) SNPs have been associated with up to 6% frequency in morbidly obese children and...
5.
Pinilla C, Edwards B, Appel J, Yates-Gibbins T, Giulianotti M, Medina-Franco J, et al.
Mol Pharmacol
. 2013 Jun;
84(3):314-24.
PMID: 23788657
The formylpeptide receptor (FPR1) and formylpeptide-like 1 receptor (FPR2) are G protein-coupled receptors that are linked to acute inflammatory responses, malignant glioma stem cell metastasis, and chronic inflammation. Although several...
6.
Santos R, Appel J, Giulianotti M, Edwards B, Sklar L, Houghten R, et al.
Molecules
. 2013 Jun;
18(6):6408-24.
PMID: 23722730
In the past 20 years, synthetic combinatorial methods have fundamentally advanced the ability to synthesize and screen large numbers of compounds for drug discovery and basic research. Mixture-based libraries and...
7.
Medina-Franco J, Edwards B, Pinilla C, Appel J, Giulianotti M, Santos R, et al.
J Chem Inf Model
. 2013 May;
53(6):1475-85.
PMID: 23705689
We present a general approach to describe the structure-activity relationships (SAR) of combinatorial data sets with activity for two biological endpoints with emphasis on the rapid identification of substitutions that...
8.
Yongye A, Vivoli M, Lindberg I, Appel J, Houghten R, Martinez-Mayorga K
PLoS One
. 2013 Mar;
8(2):e56957.
PMID: 23451118
The calcium-dependent serine endoproteases prohormone convertase 1/3 (PC1/3) and prohormone convertase 2 (PC2) play important roles in the homeostatic regulation of blood glucose levels, hence implicated in diabetes mellitus. Specifically,...
9.
Pinilla C, Appel J, Judkowski V, Houghten R
Curr Protoc Immunol
. 2012 Nov;
Chapter 9:9.5.1-9.5.16.
PMID: 23129156
This unit presents a combinatorial library method that consists of the synthesis and screening of mixture-based synthetic combinatorial libraries of peptide molecules. The protocols employ peptide libraries to identify peptides...
10.
Levesque C, Fugere M, Kwiatkowska A, Couture F, Desjardins R, Routhier S, et al.
J Med Chem
. 2012 Nov;
55(23):10501-11.
PMID: 23126600
The proprotein convertases (PCs) play an important role in protein precursor activation through processing at paired basic residues. However, significant substrate cleavage redundancy has been reported between PCs. The question...