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Activin receptor antagonists for cancer-related anemia and bone disease.

Fields SZ, Parshad S, Anne M, Raftopoulos H, Alexander MJ, Sherman ML, Laadem A, Sung V, Terpos E.

Expert Opin Investig Drugs. 2013 Jan;22(1):87-101. doi: 10.1517/13543784.2013.738666. Epub 2012 Nov 6. Review.


Multiple-dose, safety, pharmacokinetic, and pharmacodynamic study of sotatercept (ActRIIA-IgG1), a novel erythropoietic agent, in healthy postmenopausal women.

Sherman ML, Borgstein NG, Mook L, Wilson D, Yang Y, Chen N, Kumar R, Kim K, Laadem A.

J Clin Pharmacol. 2013 Nov;53(11):1121-30. doi: 10.1002/jcph.160. Epub 2013 Sep 9.


Activin receptor signaling: a potential therapeutic target for osteoporosis.

Lotinun S, Pearsall RS, Horne WC, Baron R.

Curr Mol Pharmacol. 2012 Jun;5(2):195-204. Review.


Signal transduction pathway through activin receptors as a therapeutic target of musculoskeletal diseases and cancer.

Tsuchida K, Nakatani M, Uezumi A, Murakami T, Cui X.

Endocr J. 2008 Mar;55(1):11-21. Epub 2007 Sep 14. Review.


An activin receptor IIA ligand trap promotes erythropoiesis resulting in a rapid induction of red blood cells and haemoglobin.

Carrancio S, Markovics J, Wong P, Leisten J, Castiglioni P, Groza MC, Raymon HK, Heise C, Daniel T, Chopra R, Sung V.

Br J Haematol. 2014 Jun;165(6):870-82. doi: 10.1111/bjh.12838. Epub 2014 Mar 18.


SB-431542 is a potent and specific inhibitor of transforming growth factor-beta superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7.

Inman GJ, Nicolás FJ, Callahan JF, Harling JD, Gaster LM, Reith AD, Laping NJ, Hill CS.

Mol Pharmacol. 2002 Jul;62(1):65-74.


Inhibitor-resistant type I receptors reveal specific requirements for TGF-beta signaling in vivo.

Ho DM, Chan J, Bayliss P, Whitman M.

Dev Biol. 2006 Jul 15;295(2):730-42. Epub 2006 May 8.


[Current approaches in multiple myeloma and other cancer-related bone diseases].

Engelhardt M, Kleber M, Udi J, Wäsch R.

Dtsch Med Wochenschr. 2012 May;137(20):1057-61. doi: 10.1055/s-0032-1304921. Epub 2012 Apr 27. Review. German.


The orphan receptor ALK7 and the Activin receptor ALK4 mediate signaling by Nodal proteins during vertebrate development.

Reissmann E, Jörnvall H, Blokzijl A, Andersson O, Chang C, Minchiotti G, Persico MG, Ibáñez CF, Brivanlou AH.

Genes Dev. 2001 Aug 1;15(15):2010-22.


Circulating activin-A is elevated in patients with advanced multiple myeloma and correlates with extensive bone involvement and inferior survival; no alterations post-lenalidomide and dexamethasone therapy.

Terpos E, Kastritis E, Christoulas D, Gkotzamanidou M, Eleutherakis-Papaiakovou E, Kanellias N, Papatheodorou A, Dimopoulos MA.

Ann Oncol. 2012 Oct;23(10):2681-6. Epub 2012 Apr 6.


Stromal cell-mediated inhibition of erythropoiesis can be attenuated by Sotatercept (ACE-011), an activin receptor type II ligand trap.

Iancu-Rubin C, Mosoyan G, Wang J, Kraus T, Sung V, Hoffman R.

Exp Hematol. 2013 Feb;41(2):155-166.e17. doi: 10.1016/j.exphem.2012.12.002. Epub 2012 Dec 20.


rHuEPO and improved treatment outcomes: potential modes of action.

Blackwell K, Gascón P, Sigounas G, Jolliffe L.

Oncologist. 2004;9 Suppl 5:41-7. Review.


Sclerostin: a possible target for the management of cancer-induced bone disease.

Gkotzamanidou M, Dimopoulos MA, Kastritis E, Christoulas D, Moulopoulos LA, Terpos E.

Expert Opin Ther Targets. 2012 Aug;16(8):761-9. doi: 10.1517/14728222.2012.697154. Epub 2012 Jul 5. Review.


Activin A promotes multiple myeloma-induced osteolysis and is a promising target for myeloma bone disease.

Vallet S, Mukherjee S, Vaghela N, Hideshima T, Fulciniti M, Pozzi S, Santo L, Cirstea D, Patel K, Sohani AR, Guimaraes A, Xie W, Chauhan D, Schoonmaker JA, Attar E, Churchill M, Weller E, Munshi N, Seehra JS, Weissleder R, Anderson KC, Scadden DT, Raje N.

Proc Natl Acad Sci U S A. 2010 Mar 16;107(11):5124-9. doi: 10.1073/pnas.0911929107. Epub 2010 Mar 1.


Inhibiting activin-A signaling stimulates bone formation and prevents cancer-induced bone destruction in vivo.

Chantry AD, Heath D, Mulivor AW, Pearsall S, Baud'huin M, Coulton L, Evans H, Abdul N, Werner ED, Bouxsein ML, Key ML, Seehra J, Arnett TR, Vanderkerken K, Croucher P.

J Bone Miner Res. 2010 Dec;25(12):2633-46. doi: 10.1002/jbmr.142. Epub 2010 Jun 7. Erratum in: J Bone Miner Res. 2012 Sep;27(9):2036-7. J Bone Miner Res. 2011 Feb;26(2):439.


Identification of a functional binding site for activin on the type I receptor ALK4.

Harrison CA, Gray PC, Koerber SC, Fischer W, Vale W.

J Biol Chem. 2003 Jun 6;278(23):21129-35. Epub 2003 Mar 28.


Cripto is a noncompetitive activin antagonist that forms analogous signaling complexes with activin and nodal.

Kelber JA, Shani G, Booker EC, Vale WW, Gray PC.

J Biol Chem. 2008 Feb 22;283(8):4490-500. Epub 2007 Dec 18.


Specific activation of Smad1 signaling pathways by the BMP7 type I receptor, ALK2.

Macías-Silva M, Hoodless PA, Tang SJ, Buchwald M, Wrana JL.

J Biol Chem. 1998 Oct 2;273(40):25628-36.

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