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Human Relaxin Receptor Is Fully Functional in Humanized Mice and Is Activated by Small Molecule Agonist ML290.

Kaftanovskaya EM, Soula M, Myhr C, Ho BA, Moore SN, Yoo C, Cervantes B, How J, Marugan J, Agoulnik IU, Agoulnik AI.

J Endocr Soc. 2017 Jun;1(6):712-725. doi: 10.1210/js.2017-00112. Epub 2017 May 8.


ML290 is a biased allosteric agonist at the relaxin receptor RXFP1.

Kocan M, Sarwar M, Ang SY, Xiao J, Marugan JJ, Hossain MA, Wang C, Hutchinson DS, Samuel CS, Agoulnik AI, Bathgate RAD, Summers RJ.

Sci Rep. 2017 Jun 7;7(1):2968. doi: 10.1038/s41598-017-02916-5.


Relaxin-like peptides in male reproduction - a human perspective.

Ivell R, Agoulnik AI, Anand-Ivell R.

Br J Pharmacol. 2017 May;174(10):990-1001. doi: 10.1111/bph.13689. Epub 2017 Feb 27. Review. Erratum in: Br J Pharmacol. 2017 Dec;174(24):4836.


Synthetic non-peptide low molecular weight agonists of the relaxin receptor 1.

Agoulnik AI, Agoulnik IU, Hu X, Marugan J.

Br J Pharmacol. 2017 May;174(10):977-989. doi: 10.1111/bph.13656. Epub 2016 Nov 30. Review.


Nuclear Receptor Corepressor 1 Expression and Output Declines with Prostate Cancer Progression.

Lopez SM, Agoulnik AI, Zhang M, Peterson LE, Suarez E, Gandarillas GA, Frolov A, Li R, Rajapakshe K, Coarfa C, Ittmann MM, Weigel NL, Agoulnik IU.

Clin Cancer Res. 2016 Aug 1;22(15):3937-49. doi: 10.1158/1078-0432.CCR-15-1983. Epub 2016 Mar 11.


Structural Insights into the Activation of Human Relaxin Family Peptide Receptor 1 by Small-Molecule Agonists.

Hu X, Myhr C, Huang Z, Xiao J, Barnaeva E, Ho BA, Agoulnik IU, Ferrer M, Marugan JJ, Southall N, Agoulnik AI.

Biochemistry. 2016 Mar 29;55(12):1772-83. doi: 10.1021/acs.biochem.5b01195. Epub 2016 Mar 4.


Constitutive Notch Signaling Causes Abnormal Development of the Oviducts, Abnormal Angiogenesis, and Cyst Formation in Mouse Female Reproductive Tract.

Ferguson L, Kaftanovskaya EM, Manresa C, Barbara AM, Poppiti RJ, Tan Y, Agoulnik AI.

Biol Reprod. 2016 Mar;94(3):67. doi: 10.1095/biolreprod.115.134569. Epub 2016 Feb 3.


Long-Lasting Consequences of Testosterone Exposure.

Agoulnik IU, Agoulnik AI.

Endocrinology. 2015 Oct;156(10):3488-9. doi: 10.1210/en.2015-1719. No abstract available.


Activation of Relaxin Family Receptor 1 from Different Mammalian Species by Relaxin Peptide and Small-Molecule Agonist ML290.

Huang Z, Myhr C, Bathgate RA, Ho BA, Bueno A, Hu X, Xiao J, Southall N, Barnaeva E, Agoulnik IU, Marugan JJ, Ferrer M, Agoulnik AI.

Front Endocrinol (Lausanne). 2015 Aug 17;6:128. doi: 10.3389/fendo.2015.00128. eCollection 2015.


Conditional deletion of the relaxin receptor gene in cells of smooth muscle lineage affects lower reproductive tract in pregnant mice.

Kaftanovskaya EM, Huang Z, Lopez C, Conrad K, Agoulnik AI.

Biol Reprod. 2015 Apr;92(4):91. doi: 10.1095/biolreprod.114.127209. Epub 2015 Feb 25.


Genetic ablation of androgen receptor signaling in fetal Leydig cell lineage affects Leydig cell functions in adult testis.

Kaftanovskaya EM, Lopez C, Ferguson L, Myhr C, Agoulnik AI.

FASEB J. 2015 Jun;29(6):2327-37. doi: 10.1096/fj.14-263632. Epub 2015 Feb 20.


Normal fertility in male mice with deletion of β-catenin gene in germ cells.

Rivas B, Huang Z, Agoulnik AI.

Genesis. 2014 Apr;52(4):328-32. doi: 10.1002/dvg.22742. Epub 2014 Jan 31.


The fate of spermatogonial stem cells in the cryptorchid testes of RXFP2 deficient mice.

Ferguson L, How JJ, Agoulnik AI.

PLoS One. 2013 Oct 3;8(10):e77351. doi: 10.1371/journal.pone.0077351. eCollection 2013.


NOTCH1 gain of function in germ cells causes failure of spermatogenesis in male mice.

Huang Z, Rivas B, Agoulnik AI.

PLoS One. 2013 Jul 30;8(7):e71213. doi: 10.1371/journal.pone.0071213. Print 2013.


Discovery, optimization, and biological activity of the first potent and selective small-molecule agonist series of human relaxin receptor 1 (RXFP1).

Xiao J, Chen CZ, Huang Z, Agoulnik IU, Ferrer M, Southall N, Hu X, Zheng W, Agoulnik AI, Marugan JJ.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Mar 10 [updated 2013 May 8].


Identification and optimization of small-molecule agonists of the human relaxin hormone receptor RXFP1.

Xiao J, Huang Z, Chen CZ, Agoulnik IU, Southall N, Hu X, Jones RE, Ferrer M, Zheng W, Agoulnik AI, Marugan JJ.

Nat Commun. 2013;4:1953. doi: 10.1038/ncomms2953.


Reduced androgen receptor expression accelerates the onset of ERBB2 induced breast tumors in female mice.

Hodgson MC, Vanostran G, Alghamdi S, Poppiti RJ, Agoulnik AI, Agoulnik IU.

PLoS One. 2013 Apr 8;8(4):e60455. doi: 10.1371/journal.pone.0060455. Print 2013.


Testicular cancer and cryptorchidism.

Ferguson L, Agoulnik AI.

Front Endocrinol (Lausanne). 2013 Mar 20;4:32. doi: 10.3389/fendo.2013.00032. eCollection 2013.


Left-sided cryptorchidism in mice with Wilms' tumour 1 gene deletion in gubernaculum testis.

Kaftanovskaya EM, Neukirchner G, Huff V, Agoulnik AI.

J Pathol. 2013 May;230(1):39-47. doi: 10.1002/path.4161. Epub 2013 Mar 12.


Mechanisms of INSL3 signaling in male reproductive organs.

Huang Z, Kaftanovskaya EM, Rivas B, Agoulnik AI.

Ital J Anat Embryol. 2013;118(1 Suppl):32-3.


Identification of small-molecule agonists of human relaxin family receptor 1 (RXFP1) by using a homogenous cell-based cAMP assay.

Chen CZ, Southall N, Xiao J, Marugan JJ, Ferrer M, Hu X, Jones RE, Feng S, Agoulnik IU, Zheng W, Agoulnik AI.

J Biomol Screen. 2013 Jul;18(6):670-7. doi: 10.1177/1087057112469406. Epub 2012 Dec 4.


Insulin-like 3 signaling is important for testicular descent but dispensable for spermatogenesis and germ cell survival in adult mice.

Huang Z, Rivas B, Agoulnik AI.

Biol Reprod. 2012 Dec 21;87(6):143. doi: 10.1095/biolreprod.112.103382. Print 2012 Jun.


Rethinking dog domestication by integrating genetics, archeology, and biogeography.

Larson G, Karlsson EK, Perri A, Webster MT, Ho SY, Peters J, Stahl PW, Piper PJ, Lingaas F, Fredholm M, Comstock KE, Modiano JF, Schelling C, Agoulnik AI, Leegwater PA, Dobney K, Vigne JD, Vilà C, Andersson L, Lindblad-Toh K.

Proc Natl Acad Sci U S A. 2012 Jun 5;109(23):8878-83. doi: 10.1073/pnas.1203005109. Epub 2012 May 21.


Cryptorchidism in mice with an androgen receptor ablation in gubernaculum testis.

Kaftanovskaya EM, Huang Z, Barbara AM, De Gendt K, Verhoeven G, Gorlov IP, Agoulnik AI.

Mol Endocrinol. 2012 Apr;26(4):598-607. doi: 10.1210/me.2011-1283. Epub 2012 Feb 9.


Spermatogenesis in cryptorchidism.

Agoulnik AI, Huang Z, Ferguson L.

Methods Mol Biol. 2012;825:127-47. doi: 10.1007/978-1-61779-436-0_11.


Relaxin increases human endothelial progenitor cell NO and migration and vasculogenesis in mice.

Segal MS, Sautina L, Li S, Diao Y, Agoulnik AI, Kielczewski J, McGuane JT, Grant MB, Conrad KP.

Blood. 2012 Jan 12;119(2):629-36. doi: 10.1182/blood-2011-04-346007. Epub 2011 Oct 25.


Expression of LDL-A module of relaxin receptor in prostate cancer cells inhibits tumorigenesis.

Feng S, Agoulnik AI.

Int J Oncol. 2011 Dec;39(6):1559-65. doi: 10.3892/ijo.2011.1159. Epub 2011 Aug 12.


Uterine cysts in female mice deficient for caveolin-1 and insulin-like 3 receptor RXFP2.

Li Z, Feng S, Lopez V, Elhammady G, Anderson ML, Kaftanovskaya EM, Agoulnik AI.

Endocrinology. 2011 Jun;152(6):2474-82. doi: 10.1210/en.2010-1015. Epub 2011 Apr 5.


Suppression of insulin-like3 receptor reveals the role of β-catenin and Notch signaling in gubernaculum development.

Kaftanovskaya EM, Feng S, Huang Z, Tan Y, Barbara AM, Kaur S, Truong A, Gorlov IP, Agoulnik AI.

Mol Endocrinol. 2011 Jan;25(1):170-83. doi: 10.1210/me.2010-0330. Epub 2010 Dec 8.


A missense mutation in LRR8 of RXFP2 is associated with cryptorchidism.

Harris RM, Finlayson C, Weiss J, Fisher L, Hurley L, Barrett T, Emge D, Bathgate RA, Agoulnik AI, Jameson JL.

Mamm Genome. 2010 Oct;21(9-10):442-9. doi: 10.1007/s00335-010-9291-5. Epub 2010 Oct 22.


Suppression of relaxin receptor RXFP1 decreases prostate cancer growth and metastasis.

Feng S, Agoulnik IU, Truong A, Li Z, Creighton CJ, Kaftanovskaya EM, Pereira R, Han HD, Lopez-Berestein G, Klonisch T, Ittmann MM, Sood AK, Agoulnik AI.

Endocr Relat Cancer. 2010 Oct 29;17(4):1021-33. doi: 10.1677/ERC-10-0073. Print 2010 Dec.


INSL3 has tumor-promoting activity in thyroid cancer.

Hombach-Klonisch S, Bialek J, Radestock Y, Truong A, Agoulnik AI, Fiebig B, Willing C, Weber E, Hoang-Vu C, Klonisch T.

Int J Cancer. 2010 Aug 1;127(3):521-31. doi: 10.1002/ijc.25068.


Relaxin/RXFP1 signaling in prostate cancer progression.

Feng S, Agoulnik IU, Li Z, Han HD, Lopez-Berestein G, Sood A, Ittmann MM, Agoulnik AI.

Ann N Y Acad Sci. 2009 Apr;1160:379-80. doi: 10.1111/j.1749-6632.2008.03793.x.


Relaxin signaling in uterine fibroids.

Li Z, Burzawa JK, Troung A, Feng S, Agoulnik IU, Tong X, Anderson ML, Kovanci E, Rajkovic A, Agoulnik AI.

Ann N Y Acad Sci. 2009 Apr;1160:374-8. doi: 10.1111/j.1749-6632.2008.03803.x.


Estrogen and TCDD influence RLN2 gene activity in estrogen receptor-positive human breast cancer cells.

Kietz S, Feng S, Agoulnik A, Hombach-Klonisch S.

Ann N Y Acad Sci. 2009 Apr;1160:367-73. doi: 10.1111/j.1749-6632.2009.03836.x.


INSL3 plays a role in the balance between bone formation and resorption.

Pepe A, Ferlin A, Gianesello L, Facciolli A, Agoulnik AI, Foresta C.

Ann N Y Acad Sci. 2009 Apr;1160:219-20. doi: 10.1111/j.1749-6632.2008.03785.x.


New roles for INSL3 in adults.

Ferlin A, Pepe A, Gianesello L, Garolla A, Feng S, Facciolli A, Morello R, Agoulnik AI, Foresta C.

Ann N Y Acad Sci. 2009 Apr;1160:215-8. doi: 10.1111/j.1749-6632.2008.03787.x.


INSL3/RXFP2 signaling in testicular descent.

Feng S, Ferlin A, Truong A, Bathgate R, Wade JD, Corbett S, Han S, Tannour-Louet M, Lamb DJ, Foresta C, Agoulnik AI.

Ann N Y Acad Sci. 2009 Apr;1160:197-204. doi: 10.1111/j.1749-6632.2009.03841.x. Review.


Normal prostate morphology in relaxin-mutant mice.

Ganesan A, Klonisch T, McGuane JT, Feng S, Agoulnik AI, Parry LJ.

Reprod Fertil Dev. 2009;21(3):440-50.


Mutations in the insulin-like factor 3 receptor are associated with osteoporosis.

Ferlin A, Pepe A, Gianesello L, Garolla A, Feng S, Giannini S, Zaccolo M, Facciolli A, Morello R, Agoulnik AI, Foresta C.

J Bone Miner Res. 2008 May;23(5):683-93. doi: 10.1359/jbmr.080204.


Relaxin acts on stromal cells to promote epithelial and stromal proliferation and inhibit apoptosis in the mouse cervix and vagina.

Yao L, Agoulnik AI, Cooke PS, Meling DD, Sherwood OD.

Endocrinology. 2008 May;149(5):2072-9. doi: 10.1210/en.2007-1176. Epub 2008 Jan 24.


Relaxin and related peptides in male reproduction.

Agoulnik AI.

Adv Exp Med Biol. 2007;612:49-64. Review.


Developmental expression and gene regulation of insulin-like 3 receptor RXFP2 in mouse male reproductive organs.

Feng S, Bogatcheva NV, Truong A, Korchin B, Bishop CE, Klonisch T, Agoulnik IU, Agoulnik AI.

Biol Reprod. 2007 Oct;77(4):671-80. Epub 2007 Jul 5.


Novel mutations involving the INSL3 gene associated with cryptorchidism.

El Houate B, Rouba H, Sibai H, Barakat A, Chafik A, Chadli el B, Imken L, Bogatcheva NV, Feng S, Agoulnik AI, McElreavey K.

J Urol. 2007 May;177(5):1947-51.


Relaxin promotes prostate cancer progression.

Feng S, Agoulnik IU, Bogatcheva NV, Kamat AA, Kwabi-Addo B, Li R, Ayala G, Ittmann MM, Agoulnik AI.

Clin Cancer Res. 2007 Mar 15;13(6):1695-702.


T222P mutation of the insulin-like 3 hormone receptor LGR8 is associated with testicular maldescent and hinders receptor expression on the cell surface membrane.

Bogatcheva NV, Ferlin A, Feng S, Truong A, Gianesello L, Foresta C, Agoulnik AI.

Am J Physiol Endocrinol Metab. 2007 Jan;292(1):E138-44. Epub 2006 Aug 22.


Over expression of insulin-like 3 does not prevent cryptorchidism in GNRHR or HOXA10 deficient mice.

Feng S, Bogatcheva NV, Truong A, Engel W, Adham IM, Agoulnik AI.

J Urol. 2006 Jul;176(1):399-404.


Insulin-like factor 3 gene mutations in testicular dysgenesis syndrome: clinical and functional characterization.

Ferlin A, Bogatcheva NV, Gianesello L, Pepe A, Vinanzi C, Agoulnik AI, Foresta C.

Mol Hum Reprod. 2006 Jun;12(6):401-6. Epub 2006 May 10.


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