Chemical compounds to monitor proteins (Homo sapiens)

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45256682537661225(+)-JQ1FXRGW4064CHIR-99021GSK3APFI-1Salvinorin AI-BET151KORBRD26-Et CDCABRD3BRD4BRDT


This pathway provides examples how chemical compounds can be used to monitor or trigger some biological effect, called chemical probes in chemical biologiy. The information is retrieved from the project and exemplifies how wikis can be used to expose this knowledge base and to allow discussion.

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  1. Maloney PR, Parks DJ, Haffner CD, Fivush AM, Chandra G, Plunket KD, Creech KL, Moore LB, Wilson JG, Lewis MC, Jones SA, Willson TM; ''Identification of a chemical tool for the orphan nuclear receptor FXR.''; J Med Chem, 2000 PubMed Europe PMC Scholia
  2. Picaud S, Da Costa D, Thanasopoulou A, Filippakopoulos P, Fish PV, Philpott M, Fedorov O, Brennan P, Bunnage ME, Owen DR, Bradner JE, Taniere P, O'Sullivan B, Müller S, Schwaller J, Stankovic T, Knapp S; ''PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains.''; Cancer Res, 2013 PubMed Europe PMC Scholia
  3. Pellicciari R, Fiorucci S, Camaioni E, Clerici C, Costantino G, Maloney PR, Morelli A, Parks DJ, Willson TM; ''6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity.''; J Med Chem, 2002 PubMed Europe PMC Scholia
  4. Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Roth B, Ross R, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ; ''The promise and peril of chemical probes.''; Nat Chem Biol, 2015 PubMed Europe PMC Scholia
  5. Filippakopoulos P, Qi J, Picaud S, Shen Y, Smith WB, Fedorov O, Morse EM, Keates T, Hickman TT, Felletar I, Philpott M, Munro S, McKeown MR, Wang Y, Christie AL, West N, Cameron MJ, Schwartz B, Heightman TD, La Thangue N, French CA, Wiest O, Kung AL, Knapp S, Bradner JE; ''Selective inhibition of BET bromodomains.''; Nature, 2010 PubMed Europe PMC Scholia
  6. Dawson MA, Prinjha RK, Dittmann A, Giotopoulos G, Bantscheff M, Chan WI, Robson SC, Chung CW, Hopf C, Savitski MM, Huthmacher C, Gudgin E, Lugo D, Beinke S, Chapman TD, Roberts EJ, Soden PE, Auger KR, Mirguet O, Doehner K, Delwel R, Burnett AK, Jeffrey P, Drewes G, Lee K, Huntly BJ, Kouzarides T; ''Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.''; Nature, 2011 PubMed Europe PMC Scholia
  7. Roth BL, Baner K, Westkaemper R, Siebert D, Rice KC, Steinberg S, Ernsberger P, Rothman RB; ''Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist.''; Proc Natl Acad Sci U S A, 2002 PubMed Europe PMC Scholia
  8. Ring DB, Johnson KW, Henriksen EJ, Nuss JM, Goff D, Kinnick TR, Ma ST, Reeder JW, Samuels I, Slabiak T, Wagman AS, Hammond ME, Harrison SD; ''Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo.''; Diabetes, 2003 PubMed Europe PMC Scholia


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117050view14:16, 16 May 2021EweitzModified title
89209view05:06, 23 August 2016EgonwOntology Term : 'drug pathway' added !
89208view05:06, 23 August 2016EgonwOntology Term : 'PW:0000002' removed !
89171view03:44, 23 August 2016AriuttaOntology Term : 'classic metabolic pathway' added !
81810view18:59, 30 August 2015EgonwAdded the last two probes on the website.
81809view18:35, 30 August 2015EgonwAdded the second FXR probe.
81808view16:18, 30 August 2015EgonwAdded another probe.
81125view08:47, 25 July 2015EgonwModified description
81123view08:20, 25 July 2015EgonwModified title
81121view18:19, 24 July 2015EgonwAdded the third BRD family compound (probe).
81120view17:59, 24 July 2015EgonwAdded the second probe.
81119view17:47, 24 July 2015EgonwAdd the other three targets.
81118view16:49, 24 July 2015EgonwAdded a link to the website for this compound.
81117view16:45, 24 July 2015EgonwModified description
81116view16:43, 24 July 2015EgonwNew pathway

External references


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NameTypeDatabase referenceComment
(+)-JQ1Metabolite46907787 (PubChem-compound)
6-Et CDCAMetabolite394730 (Chemspider)
BRD2GeneProductENSG00000204256 (Ensembl)
BRD3GeneProductENSG00000169925 (Ensembl)
BRD4GeneProductENSG00000141867 (Ensembl)
BRDTGeneProductENSG00000137948 (Ensembl)
CHIR-99021Metabolite9956119 (PubChem-compound)
FXRGeneProductNR1H4 (HGNC)
GSK3AGeneProduct2931 (Entrez Gene)
GW4064Metabolite9893571 (PubChem-compound)
I-BET151Metabolite52912189 (PubChem-compound)
KORGeneProduct4986 (Entrez Gene)
PFI-1Metabolite71271629 (PubChem-compound)
Salvinorin AMetabolite113947 (Chemspider)

Annotated Interactions

No annotated interactions

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