QWF

GtoPdb Ligand ID: 9568

Synonyms: Boc-Gln-D-Trp(CH0)-Phe-OBzl | N^α-[N^α-[N^α-(tert-butyloxycabonyl)-L-glutaminyl]-N¹-formyl-D-tryptophyl-L-phenylalanine benzyl ester

Compound class: Peptide or derivative

Comment: QWF was originally identified as a tripeptide derivative of the substance P-derived octapeptide and NK₁ receptor selective antagonist D-Pro-Gln-Gln-D-TrpPhe-D-Trp-D-Trp-Phe-NH₂ [2]. It has more recently been reported to antagonise MRGPRX2 [1], and is claimed in patent WO2016118632 which covers the use of QWF derivatives as MRGPRX2 antagonists for the prevention and treatment of itch [3].

References
1. Azimi E, Reddy VB, Shade KC, Anthony RM, Talbot S, Pereira PJ, Lerner EA. (2016) Dual action of neurokinin-1 antagonists on Mas-related GPCRs. JCI Insight, 1 (16): e89362. [PMID:27734033]
2. Hagiwara D, Miyake H, Morimoto H, Murai M, Fujii T, Matsuo M. (1992) Studies on neurokinin antagonists. 1. The design of novel tripeptides possessing the glutaminyl-D-tryptophylphenylalanine sequence as substance P antagonists. J Med Chem, 35 (11): 2015-25. [PMID:1375965]
3. Lerner EA, Azimi E, Reddy VB. (2016) Prevention and treatment of itch with an mrgpr antagonist. Patent number: WO2016118632. Assignee: The General Hospital Corporation. Priority date: 20/01/2015. Publication date: 28/07/2016.

References

1. Azimi E, Reddy VB, Shade KC, Anthony RM, Talbot S, Pereira PJ, Lerner EA. (2016)
Dual action of neurokinin-1 antagonists on Mas-related GPCRs.
JCI Insight, 1 (16): e89362. [PMID:27734033]

2. Hagiwara D, Miyake H, Morimoto H, Murai M, Fujii T, Matsuo M. (1992)
Studies on neurokinin antagonists. 1. The design of novel tripeptides possessing the glutaminyl-D-tryptophylphenylalanine sequence as substance P antagonists.
J Med Chem, 35 (11): 2015-25. [PMID:1375965]

3. Lerner EA, Azimi E, Reddy VB. (2016)
Prevention and treatment of itch with an mrgpr antagonist.
Patent number: WO2016118632. Assignee: The General Hospital Corporation. Priority date: 20/01/2015. Publication date: 28/07/2016.