G protein-coupled receptor 35 also known as GPR35 is a
G protein-coupled receptor which in humans is encoded by the GPR35gene.[5] Heightened expression of GPR35 is found in immune and gastrointestinal tissues, including the
crypts of Lieberkühn.
Ligands
Endogenous ligands
Although GPR35 is still considered an orphan receptor, there have been attempts to deorphanize it by identifying
endogenous molecules that can activate the receptor. All of the currently proposed ligands are either
unselective towards GPR35, or they lack high
potency, a characteristic feature of natural ligands.[6] The following list includes the most prominent examples:
Zaprinast is currently the
gold standard in the
biochemical evaluation of novel synthetic GPR35 agonists, because it remains potent in an
animal model. Most other known agonists display high selectivity towards the human GPR35
orthologue. This phenomenon is well established for other GPCRs and complicates the development of
pharmaceutical drugs.[6][14][15]
Both ML145 and ML144 unfurl their antagonistic activity through
inverse agonism. They are, however, highly species-selective, and practically inactive at the
rodent receptor orthologues.[17]
^
abYang, Yuhua; Lu, Jenny Ying-Lin; Wu, Xiaosu; Summer, Shamin; Whoriskey, John; Saris, Christiaan; Reagan, Jeff D. (2010). "G-Protein-Coupled Receptor 35 Is a Target of the Asthma Drugs Cromolyn Disodium and Nedocromil Sodium". Pharmacology. 86 (1). S. Karger AG: 1–5.
doi:
10.1159/000314164.
ISSN1423-0313.
PMID20559017.
S2CID9421354.
^Taniguchi Y, Tonai-Kachi H, Shinjo K (2006). "Zaprinast, a well-known cyclic guanosine monophosphate-specific phosphodiesterase inhibitor, is an agonist for GPR35". FEBS Lett. 580 (21): 5003–8.
doi:
10.1016/j.febslet.2006.08.015.
PMID16934253.
S2CID43142927.
^Gütschow, Michael; Schlenk, Miriam; Gäb, Jürgen; Paskaleva, Minka; Alnouri, Mohamad Wessam; Scolari, Silvia; Iqbal, Jamshed; Müller, Christa E. (2012-04-12). "Benzothiazinones: A Novel Class of Adenosine Receptor Antagonists Structurally Unrelated to Xanthine and Adenine Derivatives". Journal of Medicinal Chemistry. 55 (7). American Chemical Society (ACS): 3331–3341.
doi:
10.1021/jm300029s.
ISSN0022-2623.
PMID22409573.
^
abSusanne Heynen-Genel;
Russell Dahl; Shenghua Shi; Michelle Sauer; Santosh Hariharan; Eduard Sergienko; Shakeela Dad; Thomas DY Chung; Derek Stonich; Ying Su; Marc Caron; Pingwei Zhao; Mary E Abood; Lawrence S Barak (2010).
"Selective GPR35 Antagonists - Probes 1 & 2". National Center for Biotechnology Information (US).
PMID21433393. Bookshelf ID NBK50703. {{
cite journal}}: Cite journal requires |journal= (
help)
G protein-coupled receptor 35 also known as GPR35 is a
G protein-coupled receptor which in humans is encoded by the GPR35gene.[5] Heightened expression of GPR35 is found in immune and gastrointestinal tissues, including the
crypts of Lieberkühn.
Ligands
Endogenous ligands
Although GPR35 is still considered an orphan receptor, there have been attempts to deorphanize it by identifying
endogenous molecules that can activate the receptor. All of the currently proposed ligands are either
unselective towards GPR35, or they lack high
potency, a characteristic feature of natural ligands.[6] The following list includes the most prominent examples:
Zaprinast is currently the
gold standard in the
biochemical evaluation of novel synthetic GPR35 agonists, because it remains potent in an
animal model. Most other known agonists display high selectivity towards the human GPR35
orthologue. This phenomenon is well established for other GPCRs and complicates the development of
pharmaceutical drugs.[6][14][15]
Both ML145 and ML144 unfurl their antagonistic activity through
inverse agonism. They are, however, highly species-selective, and practically inactive at the
rodent receptor orthologues.[17]
^
abYang, Yuhua; Lu, Jenny Ying-Lin; Wu, Xiaosu; Summer, Shamin; Whoriskey, John; Saris, Christiaan; Reagan, Jeff D. (2010). "G-Protein-Coupled Receptor 35 Is a Target of the Asthma Drugs Cromolyn Disodium and Nedocromil Sodium". Pharmacology. 86 (1). S. Karger AG: 1–5.
doi:
10.1159/000314164.
ISSN1423-0313.
PMID20559017.
S2CID9421354.
^Taniguchi Y, Tonai-Kachi H, Shinjo K (2006). "Zaprinast, a well-known cyclic guanosine monophosphate-specific phosphodiesterase inhibitor, is an agonist for GPR35". FEBS Lett. 580 (21): 5003–8.
doi:
10.1016/j.febslet.2006.08.015.
PMID16934253.
S2CID43142927.
^Gütschow, Michael; Schlenk, Miriam; Gäb, Jürgen; Paskaleva, Minka; Alnouri, Mohamad Wessam; Scolari, Silvia; Iqbal, Jamshed; Müller, Christa E. (2012-04-12). "Benzothiazinones: A Novel Class of Adenosine Receptor Antagonists Structurally Unrelated to Xanthine and Adenine Derivatives". Journal of Medicinal Chemistry. 55 (7). American Chemical Society (ACS): 3331–3341.
doi:
10.1021/jm300029s.
ISSN0022-2623.
PMID22409573.
^
abSusanne Heynen-Genel;
Russell Dahl; Shenghua Shi; Michelle Sauer; Santosh Hariharan; Eduard Sergienko; Shakeela Dad; Thomas DY Chung; Derek Stonich; Ying Su; Marc Caron; Pingwei Zhao; Mary E Abood; Lawrence S Barak (2010).
"Selective GPR35 Antagonists - Probes 1 & 2". National Center for Biotechnology Information (US).
PMID21433393. Bookshelf ID NBK50703. {{
cite journal}}: Cite journal requires |journal= (
help)