Macrocyclic peptides that inhibit Wnt signalling via interaction with Wnt3a
Literature Information
Publication Date
2020-03-24
DOI
10.1039/D0CB00016G
Impact Factor
0
Authors
Manuel E. Otero-Ramirez, Kyoko Matoba, Emiko Mihara, Junichi Takagi, Hiroaki Suga
View Original
Abstract
Here we report de novo macrocyclic peptide binders to Wnt3a, a member of the Wnt protein family. By means of the Random non-standard Peptides Integrated Discovery (RaPID) system, we have performed in vitro selection against the complex of mouse Wnt3a (mWnt3a) with human afamin (hAFM) to discover macrocyclic peptides that bind mWnt3a with KD values as tight as 110 nM. One of these peptides, WAp-D04 (Wnt–AFM-peptide-D04), was able to inhibit the receptor-mediated signaling process, which was demonstrated in a Wnt3a-dependent reporter cell-line. Based on this initial hit, we applied a block-mutagenesis scanning display to identify a mutant inhibitor, WAp-D04-W10P, with 5-fold greater potency in a reporter assay. This work represents the first instance of molecules capable of inhibiting Wnt signaling through direct interaction with a Wnt protein, a molecular class for which targeting has been challenging due its highly hydrophobic nature.
Related Literature
Semi-automatic instrumentation for nucleic acid extraction and purification to quantify pathogens on surfaces
Won-Nyoung Lee, Hyun Jin Yoo, Kim Huyen Nguyen, Changyoon Baek, Junhong Min
2019-09-27
Paper
DOI: 10.1039/C9AN00896A
Enzyme-linked immunosorbent assay utilizing thin-layered microfluidics
Tatsuro Nakao, Yutaka Kazoe, Emi Mori, Hisashi Shimizu
2019-09-18
Paper
DOI: 10.1039/C9AN01491H
Real-time monitoring of calcification process by Sporosarcina pasteurii biofilm
Dustin Harris, Jyothir Ganesh Ummadi, Andrew R. Thurber, Yvan Allau, Circe Verba, Frederick Colwell, Marta E. Torres, Dipankar Koley
2016-02-29
Paper
DOI: 10.1039/C6AN00007J
Cooperative hydrogen-bonding of the adenine–thymine pair as a strategy for lowering the limit of detection of thymine by surface-enhanced Raman spectroscopy
Mónica B. Mamián-López, Paola Corio, Marcia L. A. Temperini
2016-04-20
Paper
DOI: 10.1039/C6AN00222F
An intramolecular charge transfer and excited state intramolecular proton transfer based fluorescent probe for highly selective detection and imaging of formaldehyde in living cells
Wen Chen, Mei Yang, Na Luo, Fenglin Wang, Ru-Qin Yu, Jian-Hui Jiang
2019-10-03
Paper
DOI: 10.1039/C9AN01778J
Rapid detection of synthetic cannabinoids in herbal highs using surface-enhanced Raman scattering produced by gold nanoparticle co-aggregation in a wet system
Hiroki Segawa, Takao Fukuoka, Tamitake Itoh, Yuichi Imai, Yuko T. Iwata, Tadashi Yamamuro, Kenji Kuwayama, Kenji Tsujikawa, Tatsuyuki Kanamori, Hiroyuki Inoue
2019-10-07
Paper
DOI: 10.1039/C9AN01512D
A fluorescent turn-on probe for visualizing lysosomes in hypoxic tumor cells
Yingchao Liu, Feiyi Wang, Qiang Fei, Ben Shi, Jiancai An, Chunchang Zhao, Chen-Ho Tung
2016-04-15
Communication
DOI: 10.1039/C6AN00369A
Development of portable defocusing micro-scale spatially offset Raman spectroscopy
Marco Realini, Alessandra Botteon, Claudia Conti, Chiara Colombo, Pavel Matousek
2016-04-08
Paper
DOI: 10.1039/C6AN00413J
Investigation of an SPR biosensor for determining the influence of connexin 43 expression on the cytotoxicity of cisplatin
Yijia Wang, Shiwu Zhang, Chunze Zhang, Zhenying Zhao, Xiaoli Zheng, Lihua Xue, Jun Liu, X.-C. Yuan
2016-04-20
Paper
DOI: 10.1039/C6AN00264A
A novel logic gate based on liquid-crystals responding to the DNA conformational transition
Fubing Xiao, Hui Tan, Yan Wu, Shuzhen Liao, Zhaoyang Wu, Guoli Shen, Ruqin Yu
2016-04-13
Communication
DOI: 10.1039/C6AN00504G
You might also like
Compound Q&A
How should waste containing 6-Chloro-5-(2'-hydroxy-3'-methoxy-4-biphenylyl)-3-(3-methoxyphenyl)-1H-pyrrolo[3,2-d]pyrimidine-2,4(3H,5H)-dione (CAS: 1346607-05-3) be handled?
Waste containing 6-Chloro-5-(2'-hydroxy-3'-methoxy-4-biphenylyl)-3-(3-methoxyphe...
1346607-05-36-Chloro-5-(2'-hydro...
Compound Q&A
What are the main uses of (3alpha,5alpha)-3-Hydroxypregnane-11,20-dione (CAS: 23930-19-0)?
(3alpha,5alpha)-3-Hydroxypregnane-11,20-dione is primarily used in the pharmaceu...
23930-19-0(3alpha,5alpha)-3-Hy...
Compound Q&A
What is the market or research trend for 4-Amino-6-chloro-2-pyridinecarboxylic acid (CAS: 546141-56-4)?
The market for 4-Amino-6-chloro-2-pyridinecarboxylic acid (CAS: 546141-56-4) is ...
546141-56-44-Amino-6-chloro-2-p...
Compound Q&A
Are there alternatives to (2-Benzoylethyl)trimethylammonium chloride (CAS: 24472-88-6) in synthesis?
Alternatives to (2-Benzoylethyl)trimethylammonium chloride (CAS: 24472-88-6) in ...
24472-88-6(2-Benzoylethyl)trim...
Compound Q&A
Is N-[4-Nitro-3-(trifluoromethyl)phenyl]acetamide (CAS: 393-12-4) safe?
N-[4-Nitro-3-(trifluoromethyl)phenyl]acetamide (CAS: 393-12-4) is generally safe...
393-12-4N-[4-Nitro-3-(triflu...
Compound Q&A
Are there alternatives to [(4R,5R,6S)-5-hydroxy-10-imino-3,7-dioxa-1,9-diazatricyclo[6.4.0.02,6]dodeca-8,11-dien-4-yl]methyl dihydrogen phosphate (CAS: 39679-56-6) in synthesis?
Alternative reagents such as other phosphates or similar functional groups can b...
39679-56-6[(4R,5R,6S)-5-hydrox...
Compound Q&A
Are there alternatives to N,N'-Bis(3-aminopropyl)-1,3-propanediamine (CAS: 4605-14-5) in synthesis?
There are alternatives to N,N'-Bis(3-aminopropyl)-1,3-propanediamine (CAS: 4605-...
4605-14-5N,N'-Bis(3-aminoprop...
Compound Q&A
What precautions should be taken when handling Aluminium trihexadecanoate (CAS: 555-35-1)?
When handling Aluminium trihexadecanoate, it is important to use appropriate per...
555-35-1Aluminium trihexadec...
Compound Q&A
What is (1,1-Dioxido-3-oxo-1,2-benzothiazol-2(3H)-yl)acetic acid (CAS: 52188-11-1)?
(1,1-Dioxido-3-oxo-1,2-benzothiazol-2(3H)-yl)acetic acid is a chemical compound ...
52188-11-1(1,1-Dioxido-3-oxo-1...
Compound Q&A
Are there alternatives to 5,5-dimethyloxolan-2-one (CAS: 3123-97-5) in synthesis?
Several alternatives to 5,5-dimethyloxolan-2-one (CAS: 3123-97-5) can be used in...
3123-97-55,5-dimethyloxolan-2...
Source Journal
Recommended Compounds
![2-Methyl-2-propanyl [2-(2-oxa-6-azaspiro[3.3]hept-6-yl)ethyl]carbamate structure](https://static.chemtradehub.com/structs/141/1415562-38-7-c0a4.webp "2-Methyl-2-propanyl [2-(2-oxa-6-azaspiro[3.3]hept-6-yl)ethyl]carbamate structure")
2-Methyl-2-propanyl [2-(2-oxa-6-azaspiro[3.3]hept-6-yl)ethyl]carbamate
CAS Number:
1415562-38-7
Molecular Formula:
C12H22N2O3
5-Bromo-4-chloro-2-(trifluoromethyl)quinazoline
CAS Number:
2089311-03-3
Molecular Formula:
C9H3BrClF3N2
![4-{[4-(Trifluoromethoxy)benzyl]oxy}benzonitrile structure](https://static.chemtradehub.com/structs/103/1036629-63-6-2172.webp "4-{[4-(Trifluoromethoxy)benzyl]oxy}benzonitrile structure")
4-{[4-(Trifluoromethoxy)benzyl]oxy}benzonitrile
CAS Number:
1036629-63-6
Molecular Formula:
C15H10F3NO2
Recommended Suppliers
Disclaimer
This page provides academic journal information for reference and research purposes only. We are not affiliated with any journal publishers and do not handle publication submissions. For publication-related inquiries, please contact the respective journal publishers directly.
If you notice any inaccuracies in the information displayed, please contact us at support@chemtradehub.com. We will promptly review and address your concerns.