The interplay between cytokines and the Kynurenine pathway in inflammation and atherosclerosis

R Baumgartner, MJ Forteza, DFJ Ketelhuth - Cytokine, 2019 - Elsevier
The kynurenine pathway (KP) is the major metabolic route of tryptophan (Trp) metabolism.
Indoleamine 2, 3-dioxygenase (IDO1), the enzyme responsible for the first and rate-limiting …

The G protein-coupled receptors deorphanization landscape

C Laschet, N Dupuis, J Hanson - Biochemical Pharmacology, 2018 - Elsevier
G protein-coupled receptors (GPCRs) are usually highlighted as being both the largest
family of membrane proteins and the most productive source of drug targets. However, most …

Discovery of new GPCR ligands to illuminate new biology

BL Roth, JJ Irwin, BK Shoichet - Nature chemical biology, 2017 - nature.com
Although a plurality of drugs target G-protein-coupled receptors (GPCRs), most have
emerged from classical medicinal chemistry and pharmacology programs and resemble one …

[HTML][HTML] Orphan G protein-coupled receptors: The role in CNS disorders

MS Alavi, A Shamsizadeh, H Azhdari-Zarmehri… - Biomedicine & …, 2018 - Elsevier
There are various types of receptors in the central nervous system (CNS). G protein-coupled
receptors (GPCRs) have the highest expression with a wide range of physiological …

The dark sides of the GPCR tree‐research progress on understudied GPCRs

MM Scharf, LJ Humphrys, S Berndt… - British Journal of …, 2024 - Wiley Online Library
A large portion of the human GPCRome is still in the dark and understudied, consisting even
of entire subfamilies of GPCRs such as odorant receptors, class A and C orphans, adhesion …

Discovery of TAK-041: a potent and selective GPR139 agonist explored for the treatment of negative symptoms associated with schizophrenia

HA Reichard, HH Schiffer, H Monenschein… - Journal of medicinal …, 2021 - ACS Publications
The orphan G-protein-coupled receptor GPR139 is highly expressed in the habenula, a
small brain nucleus that has been linked to depression, schizophrenia (SCZ), and substance …

Systemic and intra-habenular activation of the orphan G protein-coupled receptor GPR139 decreases compulsive-like alcohol drinking and hyperalgesia in alcohol …

J Kononoff, M Kallupi, A Kimbrough, D Conlisk… - Eneuro, 2018 - eneuro.org
GPR139 is an orphan G protein-coupled receptor (GPCR) that is expressed mainly in the
brain, with the highest expression in the medial habenula. The modulation of GPR139 …

The role of orphan receptor GPR139 in neuropsychiatric behavior

M Dao, HM Stoveken, Y Cao… - …, 2022 - nature.com
Abstract Orphan G protein Coupled Receptors (GPCRs) present attractive targets both for
understanding neuropsychiatric diseases and for development of novel therapeutics …

[HTML][HTML] The orphan G protein-coupled receptor GPR139 is activated by the peptides: Adrenocorticotropic hormone (ACTH), α-, and β-melanocyte stimulating hormone …

AC Nøhr, MA Shehata, AS Hauser, V Isberg… - Neurochemistry …, 2017 - Elsevier
GPR139 is an orphan G protein-coupled receptor that is expressed primarily in the brain.
Not much is known regarding the function of GPR139. Recently we have shown that …

Development of predictive models for identifying potential S100A9 inhibitors based on machine learning methods

J Lee, S Kumar, SY Lee, SJ Park, M Kim - Frontiers in Chemistry, 2019 - frontiersin.org
S100A9 is a potential therapeutic target for various disease including prostate cancer,
colorectal cancer, and Alzheimer's disease. However, the sparsity of atomic level data, such …