Hancock GR, Young KS, Hosfield DJ, Joiner C, Sullivan EA, Yildiz Y, Lainé M, Greene GL, Fanning SW. Unconventional isoquinoline-based SERMs elicit fulvestrant-like transcriptional programs in ER+ breast cancer cells. npj Breast Cancer. 2022;8(1):130. doi: 10.1038/s41523-022-00497-9
Grinshpu, A., Chen, V., Sandusky, Z.M., Fanning, S.W., Jeselsohn, R. (2022) Mutated Estrogen Receptor Structure and Biology and Estrogen Receptor-Positive Advanced Breast Cancer. Accepted in Biochemica Biophysica acta.
Thomas Speltz, Xianghang Shangguan, Zeyu Qiao, Colin Swenson, Christopher Lee, Sean Fanning, Geoffrey Greene & Raymond Moellering. Hyperstable Synthetic Transcriptional Regulators Targeting Myc/Max-DNA Binding. Accepted to Nature Biotechnology
Ren P, Tiede C, Fanning SW, Adams T, Speirs V, Nelson ER, Cheng C, Moore TW, Greene GL, Tomlinson D, Selvin PR. Labeling of a mutant estrogen receptor with an Affimer in a breast cancer cell line. Biophys J. 2022 Jun 30;. doi:10.1016/j.bpj.2022.06.028. [Epub ahead of print] PubMed PMID: 35778844.
Hosfield DJ, Weber S, Li N-S, Suavage M, Joiner CF, Hancock GR, Sullivan EA, Nduwke E, Han R, Cush S, Lainé M, Mader SC, Greene GL, Fanning SW. Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells. eLife. 2022;11:e72512. doi: 10.7554/eLife.72512.
Mayne CG, Toy W, Carlson KE, Bhatt T, Fanning SW, Greene GL, Katzenellenbogen BS, Chandarlapaty S, Katzenellenbogen JA, Tajkhorshid E. Defining the Energetic Basis for a Conformational Switch Mediating Ligand-Independent Activation of Mutant Estrogen Receptors in Breast Cancer. Mol Cancer Res. 2021 May 21;. doi: 10.1158/1541-7786.MCR-20-1017. [Epub ahead of print] PubMed PMID: 34021071.
Lainé M, Fanning SW, Chang YF, Green B, Greene ME, Komm B, Kurleto JD, Phung L, Greene GL. Lasofoxifene as a potential treatment for therapy-resistant ER-positive metastatic breast cancer. Breast Cancer Res. 2021 May 12;23(1):54. doi: 10.1186/s13058-021-01431-w. PubMed PMID: 33980285; PubMed Central PMCID: PMC8117302.
Abderrahman B, Maximov PY, Curpan RF, Fanning SW, Hanspal JS, Fan P, Foulds CE, Chen Y, Malovannaya A, Jain A, Xiong R, Greene GL, Tonetti DA, Thatcher GRJ, Jordan VC. Rapid Induction of the Unfolded Protein Response and Apoptosis by Estrogen Mimic TTC-352 for the Treatment of Endocrine-Resistant Breast Cancer. Mol Cancer Ther. 2021 Jan;20(1):11-25. doi: 10.1158/1535-7163.MCT-20-0563. Epub 2020 Nov 11. PubMed PMID: 33177154; PubMed Central PMCID: PMC7790886.
Maximov PY, Abderrahman B, Hawsawi YM, Chen Y, Foulds CE, Jain A, Malovannaya A, Fan P, Curpan RF, Han R, Fanning SW, Broom BM, Quintana Rincon DM, Greenland JA, Greene GL, Jordan VC. The Structure-Function Relationship of Angular Estrogens and Estrogen Receptor Alpha to Initiate Estrogen-Induced Apoptosis in Breast Cancer Cells. Mol Pharmacol. 2020 Jul;98(1):24-37. doi: 10.1124/mol.120.119776. Epub 2020 May 3. PubMed PMID: 32362585; PubMed Central PMCID: PMC7294906.
Montgomery JE, Donnelly JA, Fanning SW, Speltz TE, Shangguan X, Coukos JS, Greene GL, Moellering RE. Versatile Peptide Macrocyclization with Diels-Alder Cycloadditions. J Am Chem Soc. 2019 Oct 16;141(41):16374-16381. doi: 10.1021/jacs.9b07578. Epub 2019 Sep 26. PubMed PMID: 31523967; PubMed Central PMCID: PMC7745206.
Fanning SW, Greene GL (2019) Next Generation ERα Inhibitors for Endocrine-Resistant ER+ Breast Cancer. Endocrinology. doi: 10.1210/en.2018-01095
12/18
Fanning SW, Jeselsohn R, Dharmarajan V, Mayne CG, Karimi M, Buchwalter G, Houtman R, Toy W, Fowler CE, Laine M, Carlson KE, Martin TA, Nowak J, Nwachukwu JC, Hosfield DJ, Chandarlapaty S, Tajkhorshid E, Nettles KW, Griffin PR, Shen Y, Katzenellenbogen JA, Brown M, Greene GL. The SERM/SERD Bazedoxifene Disrupts ESR1 Helix 12 to Overcome Acquired Hormone Resistance in Breast Cancer Cells. eLife. 2018. doi: 10.7554/eLife.37161
Fanning SW, Hodges-Gallagher L, Myles DC, Sun R, Fowler CE, Plant IN, Green BD, Harmon CL, Greene GL, Kushner PJ. Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity. Nature Communications. 2018;9(1):2368. Epub 2018/06/20. doi: 10.1038/s41467-018-04413-3. PubMed PMID: 29915250; PMCID: Pmc6006285.
Maximov PY, Abderrahman B, Fanning SW, Sengupta S, Fan P, Curpan RF, Quintana Rincon DM, Greenland JA, Rajan SS, Greene GL, Jordan VC. Endoxifen, 4-Hydroxytamoxifen and an Estrogenic Derivative Modulate Estrogen Receptor Complex Mediated Apoptosis in Breast Cancer. Molecular Pharmacology. 2018.
Speltz TE, Mayne CG, Fanning SW, Siddiqui Z, Tajkhorshid E, Greene GL, Moore TW. A “cross-stitched” peptide with improved helicity and proteolytic stability. Organic & Biomolecular Chemistry. 2018;16(20):3702-6. doi: 10.1039/C8OB00790J.
Toy W, Weir H, Razavi P, Lawson M, Goeppert AU, Mazzola AM, Smith A, Wilson J, Morrow C, Wong WL, De Stanchina E, Carlson KE, Martin TS, Uddin S, Li Z, Fanning S, Katzenellenbogen JA, Greene G, Baselga J, Chandarlapaty S. Activating ESR1 Mutations Differentially Affect the Efficacy of ER Antagonists. Cancer Discovery. 2016. doi: 10.1158/2159-8290.CD-15-1523. PubMed PMID: 27986707.
Speltz, TE, Fanning, SW, Mayne, CG, Fowler, C, Tajkhorshid, E, Greene, GL, Moore, TW. Stapled Peptides with γ-Methylated Hydrocarbon Chains for the Estrogen Receptor/Coactivator Interaction, Angew Chem Int Ed Engl., 2016;55(13):4252-5. doi: 10.1002/anie.201510557.
Fanning SW, Mayne CG, Dharmarajan V, Carlson KE, Martin TA, Novick SJ, Toy W, Green B, Panchamukhi S, Katzenellenbogen BS, Tajkhorshid E, Griffin PR, Shen Y, Chandarlapaty S, Katzenellenbogen JA, Greene GL. Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation. eLife. 2016;5:e12792. doi: 10.7554/eLife.12792.
Fanning SW, Walter R, Horn JR. Structural basis of an engineered dual-specific antibody: conformational diversity leads to a hypervariable loop metal-binding site. Protein Engineering Design and Selection. 2014;27(10):391-7. doi: 10.1093/protein/gzu033. PubMed PMID: 25143596.
Toy W, Shen Y, Won H, Green B, Sakr RA, Will M, Li Z, Gala K, Fanning SW, King TA, Hudis C, Chen D, Taran T, Hortobagyi G, Greene G, Berger M, Baselga J, Chandarlapaty S. ESR1 ligand-binding domain mutations in hormone-resistant breast cancer. Nature Genetics. 2013;45(12):1439-45. doi: 10.1038/ng.2822. PubMed PMID: 24185512; PMCID: PMC3903423.
Sztuba-Solinska J, Fanning SW, Horn JR, Bujarski JJ. Mutations in the coat protein-binding cis-acting RNA motifs debilitate RNA recombination of Brome mosaic virus. Virus Research. 2012;170(1-2):138-49. Epub 2012/10/20. doi: 10.1016/j.virusres.2012.10.001. PubMed PMID: 23079110.
Murtaugh ML, Fanning SW, Sharma TM, Terry AM, Horn JR. A combinatorial histidine scanning library approach to engineer highly pH-dependent protein switches. Protein Science. 2011;20(9):1619-31. Epub 2011/07/19. doi: 10.1002/pro.696. PubMed PMID: 21766385; PMCID: Pmc3190156.
Fanning SW, Horn JR. An anti-hapten camelid antibody reveals a cryptic binding site with significant energetic contributions from a nonhypervariable loop. Protein Sci. 2011;20(7):1196-207. doi: 10.1002/pro.648. PubMed PMID: 21557375; PMCID: PMC3149193. (Featured Cover Image).
Fanning SW, Murtaugh ML, Horn JR. A combinatorial approach to engineering a dual-specific metal switch antibody. Biochemistry. 2011;50(23):5093-5. Epub 2011/05/17. doi: 10.1021/bi2003845. PubMed PMID: 21568282. (Featured on Biochemistry’s Webpage).select
Mayne CG, Toy W, Carlson KE, Bhatt T, Fanning SW, Greene GL, Katzenellenbogen BS, Chandarlapaty S, Katzenellenbogen JA, Tajkhorshid E. Defining the Energetic Basis for a Conformational Switch Mediating Ligand-Independent Activation of Mutant Estrogen Receptors in Breast Cancer. Mol Cancer Res. 2021 May 21;. doi: 10.1158/1541-7786.MCR-20-1017. [Epub ahead of print] PubMed PMID: 34021071.
select
Lainé M, Fanning SW, Chang YF, Green B, Greene ME, Komm B, Kurleto JD, Phung L, Greene GL. Lasofoxifene as a potential treatment for therapy-resistant ER-positive metastatic breast cancer. Breast Cancer Res. 2021 May 12;23(1):54. doi: 10.1186/s13058-021-01431-w. PubMed PMID: 33980285; PubMed Central PMCID: PMC8117302.
select
Abderrahman B, Maximov PY, Curpan RF, Fanning SW, Hanspal JS, Fan P, Foulds CE, Chen Y, Malovannaya A, Jain A, Xiong R, Greene GL, Tonetti DA, Thatcher GRJ, Jordan VC. Rapid Induction of the Unfolded Protein Response and Apoptosis by Estrogen Mimic TTC-352 for the Treatment of Endocrine-Resistant Breast Cancer. Mol Cancer Ther. 2021 Jan;20(1):11-25. doi: 10.1158/1535-7163.MCT-20-0563. Epub 2020 Nov 11. PubMed PMID: 33177154; PubMed Central PMCID: PMC7790886.
select
Maximov PY, Abderrahman B, Hawsawi YM, Chen Y, Foulds CE, Jain A, Malovannaya A, Fan P, Curpan RF, Han R, Fanning SW, Broom BM, Quintana Rincon DM, Greenland JA, Greene GL, Jordan VC. The Structure-Function Relationship of Angular Estrogens and Estrogen Receptor Alpha to Initiate Estrogen-Induced Apoptosis in Breast Cancer Cells. Mol Pharmacol. 2020 Jul;98(1):24-37. doi: 10.1124/mol.120.119776. Epub 2020 May 3. PubMed PMID: 32362585; PubMed Central PMCID: PMC7294906.
select
Montgomery JE, Donnelly JA, Fanning SW, Speltz TE, Shangguan X, Coukos JS, Greene GL, Moellering RE. Versatile Peptide Macrocyclization with Diels-Alder Cycloadditions. J Am Chem Soc. 2019 Oct 16;141(41):16374-16381. doi: 10.1021/jacs.9b07578. Epub 2019 Sep 26. PubMed PMID: 31523967; PubMed Central PMCID: PMC7745206.
Grinshpu, A., Chen, V., Sandusky, Z.M., Fanning, S.W., Jeselsohn, R. (2022) Mutated Estrogen Receptor Structure and Biology and Estrogen Receptor-Positive Advanced Breast Cancer. Accepted in Biochemica Biophysica acta.
Thomas Speltz, Xianghang Shangguan, Zeyu Qiao, Colin Swenson, Christopher Lee, Sean Fanning, Geoffrey Greene & Raymond Moellering. Hyperstable Synthetic Transcriptional Regulators Targeting Myc/Max-DNA Binding. Accepted to Nature Biotechnology
Ren P, Tiede C, Fanning SW, Adams T, Speirs V, Nelson ER, Cheng C, Moore TW, Greene GL, Tomlinson D, Selvin PR. Labeling of a mutant estrogen receptor with an Affimer in a breast cancer cell line. Biophys J. 2022 Jun 30;. doi:10.1016/j.bpj.2022.06.028. [Epub ahead of print] PubMed PMID: 35778844.
Hosfield DJ, Weber S, Li N-S, Suavage M, Joiner CF, Hancock GR, Sullivan EA, Nduwke E, Han R, Cush S, Lainé M, Mader SC, Greene GL, Fanning SW. Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells. eLife. 2022;11:e72512. doi: 10.7554/eLife.72512.
Mayne CG, Toy W, Carlson KE, Bhatt T, Fanning SW, Greene GL, Katzenellenbogen BS, Chandarlapaty S, Katzenellenbogen JA, Tajkhorshid E. Defining the Energetic Basis for a Conformational Switch Mediating Ligand-Independent Activation of Mutant Estrogen Receptors in Breast Cancer. Mol Cancer Res. 2021 May 21;. doi: 10.1158/1541-7786.MCR-20-1017. [Epub ahead of print] PubMed PMID: 34021071.
Lainé M, Fanning SW, Chang YF, Green B, Greene ME, Komm B, Kurleto JD, Phung L, Greene GL. Lasofoxifene as a potential treatment for therapy-resistant ER-positive metastatic breast cancer. Breast Cancer Res. 2021 May 12;23(1):54. doi: 10.1186/s13058-021-01431-w. PubMed PMID: 33980285; PubMed Central PMCID: PMC8117302.
Abderrahman B, Maximov PY, Curpan RF, Fanning SW, Hanspal JS, Fan P, Foulds CE, Chen Y, Malovannaya A, Jain A, Xiong R, Greene GL, Tonetti DA, Thatcher GRJ, Jordan VC. Rapid Induction of the Unfolded Protein Response and Apoptosis by Estrogen Mimic TTC-352 for the Treatment of Endocrine-Resistant Breast Cancer. Mol Cancer Ther. 2021 Jan;20(1):11-25. doi: 10.1158/1535-7163.MCT-20-0563. Epub 2020 Nov 11. PubMed PMID: 33177154; PubMed Central PMCID: PMC7790886.
Maximov PY, Abderrahman B, Hawsawi YM, Chen Y, Foulds CE, Jain A, Malovannaya A, Fan P, Curpan RF, Han R, Fanning SW, Broom BM, Quintana Rincon DM, Greenland JA, Greene GL, Jordan VC. The Structure-Function Relationship of Angular Estrogens and Estrogen Receptor Alpha to Initiate Estrogen-Induced Apoptosis in Breast Cancer Cells. Mol Pharmacol. 2020 Jul;98(1):24-37. doi: 10.1124/mol.120.119776. Epub 2020 May 3. PubMed PMID: 32362585; PubMed Central PMCID: PMC7294906.
Montgomery JE, Donnelly JA, Fanning SW, Speltz TE, Shangguan X, Coukos JS, Greene GL, Moellering RE. Versatile Peptide Macrocyclization with Diels-Alder Cycloadditions. J Am Chem Soc. 2019 Oct 16;141(41):16374-16381. doi: 10.1021/jacs.9b07578. Epub 2019 Sep 26. PubMed PMID: 31523967; PubMed Central PMCID: PMC7745206.
Fanning SW, Greene GL (2019) Next Generation ERα Inhibitors for Endocrine-Resistant ER+ Breast Cancer. Endocrinology. doi: 10.1210/en.2018-01095
12/18
Fanning SW, Jeselsohn R, Dharmarajan V, Mayne CG, Karimi M, Buchwalter G, Houtman R, Toy W, Fowler CE, Laine M, Carlson KE, Martin TA, Nowak J, Nwachukwu JC, Hosfield DJ, Chandarlapaty S, Tajkhorshid E, Nettles KW, Griffin PR, Shen Y, Katzenellenbogen JA, Brown M, Greene GL. The SERM/SERD Bazedoxifene Disrupts ESR1 Helix 12 to Overcome Acquired Hormone Resistance in Breast Cancer Cells. eLife. 2018. doi: 10.7554/eLife.37161
Fanning SW, Hodges-Gallagher L, Myles DC, Sun R, Fowler CE, Plant IN, Green BD, Harmon CL, Greene GL, Kushner PJ. Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity. Nature Communications. 2018;9(1):2368. Epub 2018/06/20. doi: 10.1038/s41467-018-04413-3. PubMed PMID: 29915250; PMCID: Pmc6006285.
Maximov PY, Abderrahman B, Fanning SW, Sengupta S, Fan P, Curpan RF, Quintana Rincon DM, Greenland JA, Rajan SS, Greene GL, Jordan VC. Endoxifen, 4-Hydroxytamoxifen and an Estrogenic Derivative Modulate Estrogen Receptor Complex Mediated Apoptosis in Breast Cancer. Molecular Pharmacology. 2018.
Speltz TE, Mayne CG, Fanning SW, Siddiqui Z, Tajkhorshid E, Greene GL, Moore TW. A “cross-stitched” peptide with improved helicity and proteolytic stability. Organic & Biomolecular Chemistry. 2018;16(20):3702-6. doi: 10.1039/C8OB00790J.
Toy W, Weir H, Razavi P, Lawson M, Goeppert AU, Mazzola AM, Smith A, Wilson J, Morrow C, Wong WL, De Stanchina E, Carlson KE, Martin TS, Uddin S, Li Z, Fanning S, Katzenellenbogen JA, Greene G, Baselga J, Chandarlapaty S. Activating ESR1 Mutations Differentially Affect the Efficacy of ER Antagonists. Cancer Discovery. 2016. doi: 10.1158/2159-8290.CD-15-1523. PubMed PMID: 27986707.
Speltz, TE, Fanning, SW, Mayne, CG, Fowler, C, Tajkhorshid, E, Greene, GL, Moore, TW. Stapled Peptides with γ-Methylated Hydrocarbon Chains for the Estrogen Receptor/Coactivator Interaction, Angew Chem Int Ed Engl., 2016;55(13):4252-5. doi: 10.1002/anie.201510557.
Fanning SW, Mayne CG, Dharmarajan V, Carlson KE, Martin TA, Novick SJ, Toy W, Green B, Panchamukhi S, Katzenellenbogen BS, Tajkhorshid E, Griffin PR, Shen Y, Chandarlapaty S, Katzenellenbogen JA, Greene GL. Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation. eLife. 2016;5:e12792. doi: 10.7554/eLife.12792.
Fanning SW, Walter R, Horn JR. Structural basis of an engineered dual-specific antibody: conformational diversity leads to a hypervariable loop metal-binding site. Protein Engineering Design and Selection. 2014;27(10):391-7. doi: 10.1093/protein/gzu033. PubMed PMID: 25143596.
Toy W, Shen Y, Won H, Green B, Sakr RA, Will M, Li Z, Gala K, Fanning SW, King TA, Hudis C, Chen D, Taran T, Hortobagyi G, Greene G, Berger M, Baselga J, Chandarlapaty S. ESR1 ligand-binding domain mutations in hormone-resistant breast cancer. Nature Genetics. 2013;45(12):1439-45. doi: 10.1038/ng.2822. PubMed PMID: 24185512; PMCID: PMC3903423.
Sztuba-Solinska J, Fanning SW, Horn JR, Bujarski JJ. Mutations in the coat protein-binding cis-acting RNA motifs debilitate RNA recombination of Brome mosaic virus. Virus Research. 2012;170(1-2):138-49. Epub 2012/10/20. doi: 10.1016/j.virusres.2012.10.001. PubMed PMID: 23079110.
Murtaugh ML, Fanning SW, Sharma TM, Terry AM, Horn JR. A combinatorial histidine scanning library approach to engineer highly pH-dependent protein switches. Protein Science. 2011;20(9):1619-31. Epub 2011/07/19. doi: 10.1002/pro.696. PubMed PMID: 21766385; PMCID: Pmc3190156.
Fanning SW, Horn JR. An anti-hapten camelid antibody reveals a cryptic binding site with significant energetic contributions from a nonhypervariable loop. Protein Sci. 2011;20(7):1196-207. doi: 10.1002/pro.648. PubMed PMID: 21557375; PMCID: PMC3149193. (Featured Cover Image).
Fanning SW, Murtaugh ML, Horn JR. A combinatorial approach to engineering a dual-specific metal switch antibody. Biochemistry. 2011;50(23):5093-5. Epub 2011/05/17. doi: 10.1021/bi2003845. PubMed PMID: 21568282. (Featured on Biochemistry’s Webpage).select
Mayne CG, Toy W, Carlson KE, Bhatt T, Fanning SW, Greene GL, Katzenellenbogen BS, Chandarlapaty S, Katzenellenbogen JA, Tajkhorshid E. Defining the Energetic Basis for a Conformational Switch Mediating Ligand-Independent Activation of Mutant Estrogen Receptors in Breast Cancer. Mol Cancer Res. 2021 May 21;. doi: 10.1158/1541-7786.MCR-20-1017. [Epub ahead of print] PubMed PMID: 34021071.
select
Lainé M, Fanning SW, Chang YF, Green B, Greene ME, Komm B, Kurleto JD, Phung L, Greene GL. Lasofoxifene as a potential treatment for therapy-resistant ER-positive metastatic breast cancer. Breast Cancer Res. 2021 May 12;23(1):54. doi: 10.1186/s13058-021-01431-w. PubMed PMID: 33980285; PubMed Central PMCID: PMC8117302.
select
Abderrahman B, Maximov PY, Curpan RF, Fanning SW, Hanspal JS, Fan P, Foulds CE, Chen Y, Malovannaya A, Jain A, Xiong R, Greene GL, Tonetti DA, Thatcher GRJ, Jordan VC. Rapid Induction of the Unfolded Protein Response and Apoptosis by Estrogen Mimic TTC-352 for the Treatment of Endocrine-Resistant Breast Cancer. Mol Cancer Ther. 2021 Jan;20(1):11-25. doi: 10.1158/1535-7163.MCT-20-0563. Epub 2020 Nov 11. PubMed PMID: 33177154; PubMed Central PMCID: PMC7790886.
select
Maximov PY, Abderrahman B, Hawsawi YM, Chen Y, Foulds CE, Jain A, Malovannaya A, Fan P, Curpan RF, Han R, Fanning SW, Broom BM, Quintana Rincon DM, Greenland JA, Greene GL, Jordan VC. The Structure-Function Relationship of Angular Estrogens and Estrogen Receptor Alpha to Initiate Estrogen-Induced Apoptosis in Breast Cancer Cells. Mol Pharmacol. 2020 Jul;98(1):24-37. doi: 10.1124/mol.120.119776. Epub 2020 May 3. PubMed PMID: 32362585; PubMed Central PMCID: PMC7294906.
select
Montgomery JE, Donnelly JA, Fanning SW, Speltz TE, Shangguan X, Coukos JS, Greene GL, Moellering RE. Versatile Peptide Macrocyclization with Diels-Alder Cycloadditions. J Am Chem Soc. 2019 Oct 16;141(41):16374-16381. doi: 10.1021/jacs.9b07578. Epub 2019 Sep 26. PubMed PMID: 31523967; PubMed Central PMCID: PMC7745206.
