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Structure-guided design fine-tunes pharmacokinetics, tolerability, and antitumor profile of multispecific frizzled antibodies.

Raman S, Beilschmidt M, To M, Lin K, Lui F, Jmeian Y, Ng M, Fernandez M, Fu Y, Mascall K, Duque A, Wang X, Pan G, Angers S, Moffat J, Sidhu SS, Magram J, Sinclair AM, Fransson J, Julien JP.

Proc Natl Acad Sci U S A. 2019 Apr 2;116(14):6812-6817. doi: 10.1073/pnas.1817246116. Epub 2019 Mar 20.


A synthetic anti-Frizzled antibody engineered for broadened specificity exhibits enhanced anti-tumor properties.

Pavlovic Z, Adams JJ, Blazer LL, Gakhal AK, Jarvik N, Steinhart Z, Robitaille M, Mascall K, Pan J, Angers S, Moffat J, Sidhu SS.

MAbs. 2018 Nov-Dec;10(8):1157-1167. doi: 10.1080/19420862.2018.1515565. Epub 2018 Sep 25.


Cell growth inhibition and apoptosis in breast cancer cells induced by anti-FZD7 scFvs: involvement of bioinformatics-based design of novel epitopes.

Zarei N, Fazeli M, Mohammadi M, Nejatollahi F.

Breast Cancer Res Treat. 2018 Jun;169(3):427-436. doi: 10.1007/s10549-017-4641-6. Epub 2018 Feb 6.


Genome-wide CRISPR screens reveal a Wnt-FZD5 signaling circuit as a druggable vulnerability of RNF43-mutant pancreatic tumors.

Steinhart Z, Pavlovic Z, Chandrashekhar M, Hart T, Wang X, Zhang X, Robitaille M, Brown KR, Jaksani S, Overmeer R, Boj SF, Adams J, Pan J, Clevers H, Sidhu S, Moffat J, Angers S.

Nat Med. 2017 Jan;23(1):60-68. doi: 10.1038/nm.4219. Epub 2016 Nov 21. Erratum in: Nat Med. 2017 Nov 7;23 (11):1384.


Wnt pathway inhibition via the targeting of Frizzled receptors results in decreased growth and tumorigenicity of human tumors.

Gurney A, Axelrod F, Bond CJ, Cain J, Chartier C, Donigan L, Fischer M, Chaudhari A, Ji M, Kapoun AM, Lam A, Lazetic S, Ma S, Mitra S, Park IK, Pickell K, Sato A, Satyal S, Stroud M, Tran H, Yen WC, Lewicki J, Hoey T.

Proc Natl Acad Sci U S A. 2012 Jul 17;109(29):11717-22. doi: 10.1073/pnas.1120068109. Epub 2012 Jul 2.


Surrogate Wnt agonists that phenocopy canonical Wnt and β-catenin signalling.

Janda CY, Dang LT, You C, Chang J, de Lau W, Zhong ZA, Yan KS, Marecic O, Siepe D, Li X, Moody JD, Williams BO, Clevers H, Piehler J, Baker D, Kuo CJ, Garcia KC.

Nature. 2017 May 11;545(7653):234-237. doi: 10.1038/nature22306. Epub 2017 May 3.


Unsaturated fatty acyl recognition by Frizzled receptors mediates dimerization upon Wnt ligand binding.

Nile AH, Mukund S, Stanger K, Wang W, Hannoush RN.

Proc Natl Acad Sci U S A. 2017 Apr 18;114(16):4147-4152. doi: 10.1073/pnas.1618293114. Epub 2017 Apr 4.


Frizzled-8 receptor is activated by the Wnt-2 ligand in non-small cell lung cancer.

Bravo DT, Yang YL, Kuchenbecker K, Hung MS, Xu Z, Jablons DM, You L.

BMC Cancer. 2013 Jul 1;13:316. doi: 10.1186/1471-2407-13-316.


An anti-Wnt5a antibody suppresses metastasis of gastric cancer cells in vivo by inhibiting receptor-mediated endocytosis.

Hanaki H, Yamamoto H, Sakane H, Matsumoto S, Ohdan H, Sato A, Kikuchi A.

Mol Cancer Ther. 2012 Feb;11(2):298-307. doi: 10.1158/1535-7163.MCT-11-0682. Epub 2011 Nov 18.


Frizzled-8 as a putative therapeutic target in human lung cancer.

Wang HQ, Xu ML, Ma J, Zhang Y, Xie CH.

Biochem Biophys Res Commun. 2012 Jan 6;417(1):62-6. doi: 10.1016/j.bbrc.2011.11.055. Epub 2011 Nov 25.


Antagonistic role of Klotho-derived peptides dynamics in the pancreatic cancer treatment through obstructing WNT-1 and Frizzled binding.

Fakhar M, Najumuddin, Gul M, Rashid S.

Biophys Chem. 2018 Sep;240:107-117. doi: 10.1016/j.bpc.2018.07.002. Epub 2018 Jul 7.


MiR-744 increases tumorigenicity of pancreatic cancer by activating Wnt/β-catenin pathway.

Zhou W, Li Y, Gou S, Xiong J, Wu H, Wang C, Yan H, Liu T.

Oncotarget. 2015 Nov 10;6(35):37557-69. doi: 10.18632/oncotarget.5317.


Assessment of Frizzled 6 membrane mobility by FRAP supports G protein coupling and reveals WNT-Frizzled selectivity.

Kilander MB, Dahlström J, Schulte G.

Cell Signal. 2014 Sep;26(9):1943-9. doi: 10.1016/j.cellsig.2014.05.012. Epub 2014 May 27.


Inactivating mutations of RNF43 confer Wnt dependency in pancreatic ductal adenocarcinoma.

Jiang X, Hao HX, Growney JD, Woolfenden S, Bottiglio C, Ng N, Lu B, Hsieh MH, Bagdasarian L, Meyer R, Smith TR, Avello M, Charlat O, Xie Y, Porter JA, Pan S, Liu J, McLaughlin ME, Cong F.

Proc Natl Acad Sci U S A. 2013 Jul 30;110(31):12649-54. doi: 10.1073/pnas.1307218110. Epub 2013 Jul 11.


Wnt5a promotes Frizzled-4 signalosome assembly by stabilizing cysteine-rich domain dimerization.

DeBruine ZJ, Ke J, Harikumar KG, Gu X, Borowsky P, Williams BO, Xu W, Miller LJ, Xu HE, Melcher K.

Genes Dev. 2017 May 1;31(9):916-926. doi: 10.1101/gad.298331.117. Epub 2017 May 25.


Frizzled7 as an emerging target for cancer therapy.

King TD, Zhang W, Suto MJ, Li Y.

Cell Signal. 2012 Apr;24(4):846-51. doi: 10.1016/j.cellsig.2011.12.009. Epub 2011 Dec 13. Review.


A selective peptide inhibitor of Frizzled 7 receptors disrupts intestinal stem cells.

Nile AH, de Sousa E Melo F, Mukund S, Piskol R, Hansen S, Zhou L, Zhang Y, Fu Y, Gogol EB, Kömüves LG, Modrusan Z, Angers S, Franke Y, Koth C, Fairbrother WJ, Wang W, de Sauvage FJ, Hannoush RN.

Nat Chem Biol. 2018 Jun;14(6):582-590. doi: 10.1038/s41589-018-0035-2. Epub 2018 Apr 9. Erratum in: Nat Chem Biol. 2018 May 4;:.


Structure-based Discovery of Novel Small Molecule Wnt Signaling Inhibitors by Targeting the Cysteine-rich Domain of Frizzled.

Lee HJ, Bao J, Miller A, Zhang C, Wu J, Baday YC, Guibao C, Li L, Wu D, Zheng JJ.

J Biol Chem. 2015 Dec 18;290(51):30596-606. doi: 10.1074/jbc.M115.673202. Epub 2015 Oct 26.


Fatty acid recognition in the Frizzled receptor family.

Nile AH, Hannoush RN.

J Biol Chem. 2019 Jan 11;294(2):726-736. doi: 10.1074/jbc.REV118.005205. Epub 2018 Dec 10. Review.


Krüppel-like factor 9 suppressed tumorigenicity of the pancreatic ductal adenocarcinoma by negatively regulating frizzled-5.

Ji P, Fan X, Ma X, Wang X, Zhang J, Mao Z.

Biochem Biophys Res Commun. 2018 May 23;499(4):815-821. doi: 10.1016/j.bbrc.2018.03.229. Epub 2018 Apr 4. Erratum in: Biochem Biophys Res Commun. 2019 Mar 12;510(3):487.


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