PMID- 26522946
OWN - NLM
STAT- MEDLINE
DCOM- 20161005
LR  - 20220311
IS  - 1464-3405 (Electronic)
IS  - 0960-894X (Linking)
VI  - 25
IP  - 23
DP  - 2015 Dec 1
TI  - The use of porcupine inhibitors to target Wnt-driven cancers.
PG  - 5472-6
LID - S0960-894X(15)30141-4 [pii]
LID - 10.1016/j.bmcl.2015.10.032 [doi]
AB  - Over the past decade, academic groups and pharmaceutical companies have uncovered 
      several components and targets for intervention in the Wnt pathway. One approach 
      is to block Wnt signalling through the use of orally bioavailable small molecules 
      that prevent Wnt ligand secretion. In recent years, the membrane bound O-acyl 
      transferase (MBOAT) porcupine (PORCN) has emerged as a molecular target of 
      interest in the search for clinical options to treat Wnt-driven cancers. This 
      review shall provide an overview of the reported small molecule inhibitors for 
      PORCN and discuss the progress made in identifying human disease models that are 
      responsive to PORCN inhibitors.
CI  - Copyright (c) 2015 Elsevier Ltd. All rights reserved.
FAU - Ho, Soo Yei
AU  - Ho SY
AD  - Experimental Therapeutics Centre, 31 Biopolis Way, #03-01 Nanos, Singapore 
      138669, Singapore. Electronic address: syho@etc.a-star.edu.sg.
FAU - Keller, Thomas H
AU  - Keller TH
AD  - Experimental Therapeutics Centre, 31 Biopolis Way, #03-01 Nanos, Singapore 
      138669, Singapore.
LA  - eng
PT  - Journal Article
PT  - Review
DEP - 20151023
PL  - England
TA  - Bioorg Med Chem Lett
JT  - Bioorganic & medicinal chemistry letters
JID - 9107377
RN  - 0 (Benzothiazoles)
RN  - 0 (IWP-1 compound)
RN  - 0 (IWP-2 compound)
RN  - 0 (Membrane Proteins)
RN  - EC 2.3.- (Acyltransferases)
RN  - EC 2.3.1.- (PORCN protein, human)
SB  - IM
MH  - Acyltransferases
MH  - Animals
MH  - Benzothiazoles/*chemistry/pharmacology
MH  - HEK293 Cells
MH  - Humans
MH  - Membrane Proteins/*antagonists & inhibitors
MH  - Molecular Structure
MH  - Neoplasms/*drug therapy
MH  - *Wnt Signaling Pathway
OTO - NOTNLM
OT  - Acyltransferase
OT  - Palmitoleation
OT  - Phenotypic assays
OT  - Porcupine inhibitors
OT  - Wnt-driven cancers
OT  - Wnt-signalling pathway
EDAT- 2015/11/03 06:00
MHDA- 2016/10/07 06:00
CRDT- 2015/11/03 06:00
PHST- 2015/09/04 00:00 [received]
PHST- 2015/10/05 00:00 [revised]
PHST- 2015/10/12 00:00 [accepted]
PHST- 2015/11/03 06:00 [entrez]
PHST- 2015/11/03 06:00 [pubmed]
PHST- 2016/10/07 06:00 [medline]
AID - S0960-894X(15)30141-4 [pii]
AID - 10.1016/j.bmcl.2015.10.032 [doi]
PST - ppublish
SO  - Bioorg Med Chem Lett. 2015 Dec 1;25(23):5472-6. doi: 10.1016/j.bmcl.2015.10.032. 
      Epub 2015 Oct 23.