Details of the Drug-Related molecule(s) Interaction Atlas

General Information of DTT (ID: TTKP2SU)

• DTT Name: Transient receptor potential cation channel V4 (TRPV4) DTT Info
• Gene Name: TRPV4

Molecule-Related Drug & Molecule List

2 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
GSK2798745	DM7V96W	Heart failure	BD10-BD13	Phase 2	[1]
phorbol 12-myristate 13-acetate	DMJWD62	Acute myeloid leukaemia	2A60	Phase 2	[2]

15 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
4-Pyridin-2-yl-piperazine-1-carboxylic acid amide	DMFC8Q4	Discovery agent	N.A.	Investigative	[3]
4alpha-PDD	DMTSPLX	Discovery agent	N.A.	Investigative	[2]
4alpha-PDH	DMUOLES	Discovery agent	N.A.	Investigative	[4]
5'-iodoresiniferatoxin	DMQINY5	Discovery agent	N.A.	Investigative	[3]
5,6-epoxyeicosatrienoic acid	DMXTYCU	Discovery agent	N.A.	Investigative	[5]
bisandrographolide	DMRSKGC	Discovery agent	N.A.	Investigative	[6]
CAPSAZEPINE	DM4ATCI	Discovery agent	N.A.	Investigative	[7]
citric acid	DM80YI7	Discovery agent	N.A.	Investigative	[8]
GSK1016790A	DMDHZR1	Discovery agent	N.A.	Investigative	[9]
GSK2193874	DMY2XV3	Discovery agent	N.A.	Investigative	[10]
HC067047	DMIXY1O	Discovery agent	N.A.	Investigative	[11]
Pyrrolidin-1-yl-thiourea	DMYNZXC	Discovery agent	N.A.	Investigative	[3]
RN1734	DMA3ZXM	Discovery agent	N.A.	Investigative	[12]
RN1747	DMIPZTM	Discovery agent	N.A.	Investigative	[12]
SC-0030	DMD2WEQ	Discovery agent	N.A.	Investigative	[13]

References

• [1] Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
• [2] Activation of TRPV4 channels (hVRL-2/mTRP12) by phorbol derivatives. J Biol Chem. 2002 Apr 19;277(16):13569-77.
• [3] N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands. Bioorg Med Chem Lett. 2004 Apr 5;14(7):1693-6.
• [4] Modulation of the transient receptor potential vanilloid channel TRPV4 by 4alpha-phorbol esters: a structure-activity study. J Med Chem. 2009 May 14;52(9):2933-9.
• [5] Anandamide and arachidonic acid use epoxyeicosatrienoic acids to activate TRPV4 channels. Nature. 2003 Jul 24;424(6947):434-8.
• [6] Bisandrographolide from Andrographis paniculata activates TRPV4 channels. J Biol Chem. 2006 Oct 6;281(40):29897-904.
• [7] Chain-branched acyclic phenethylthiocarbamates as vanilloid receptor antagonists. Bioorg Med Chem Lett. 2003 May 5;13(9):1549-52.
• [8] Impaired pressure sensation in mice lacking TRPV4. J Biol Chem. 2003 Jun 20;278(25):22664-8.
• [9] N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinary bladder contraction and hyperactivity: Part I. J Pharmacol Exp Ther. 2008 Aug;326(2):432-42.
• [10] An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure. Sci Transl Med. 2012 Nov 7;4(159):159ra148.
• [11] Inhibition of the cation channel TRPV4 improves bladder function in mice and rats with cyclophosphamide-induced cystitis. Proc Natl Acad Sci U S A. 2010 Nov 2;107(44):19084-9.
• [12] Identification and characterization of novel TRPV4 modulators. Biochem Biophys Res Commun. 2009 Nov 20;389(3):490-4.
• [13] Novel non-vanilloid VR1 antagonist of high analgesic effects and its structural requirement for VR1 antagonistic effects. Bioorg Med Chem Lett. 2003 Dec 15;13(24):4389-93.