Pipeline

We are advancing our clinical-stage pipeline of differentiated treatments focused on chronic diseases with unmet need around the globe, including cardiovascular, metabolic and pulmonary conditions.

Program

Indication

Discovery

IND-enabling

Phase 1

Phase 2

Oral GLP-1R Franchise

GSBR-1290

GLP-1R

Type 2 Diabetes and Obesity

Phase 1

Next Gen GSBR

Dual GLP-1R / GIPR

Type 2 Diabetes and Obesity

Discovery

Oral APJR

ANPA-0073

APJR

Cardiopulmonary

Phase 1

Oral LPA1R

LTSE-2578

LPA1R

Idiopathic Pulmonary Fibrosis (IPF)

IND-enabling

Therapeutic Area Focus

Chronic diseases are rapidly increasing worldwide, escalating the demand for life-changing medicines. These conditions represent 73% of all deaths worldwide and 60% of the global burden of disease. At Structure, we are determined to transform these devastating figures with innovative, small molecule medicines.

417 Million

suffer from Type 2 Diabetes

46% increase by 2045
90% of T2DM patients are overweight or obese

Diabetes
Obesity
NAFLD/NASH

150 Million

suffer from our cardiopulmonary disease areas of focus

>2x increase in incidence of pulmonary fibrosis over last 30 yrs
Mortality can occur within 3-5 yrs

Pulmonary Hypertension
Pulmonary Fibrosis
Heart Failure

Presentations & Publications

Foundational Publications

Explore over two decades of publications that are the foundation of Structure’s innovative technology and approach.

All 2013 2022-2017 2016-2012 2011-2006 2005-2000

Structure Based Discovery and Anti-fibrotic Activity of Novel Antagonists of Lysophosphatidic Acid Receptor 1 (LPAR1) (Presented at ATS 2023)

May 27, 2023/by Justin

A First-in-Human Single/Multiple Ascending Dose Study of ANPA-0073, a Novel Small Molecule G-protein Biased Apelin Receptor Agonist, in Healthy Volunteers (Presented at ATS 2023)

May 27, 2023/by Justin

Discovery of G-protein Biased Small Molecule APJ Agonist for Pulmonary Disease (Presented at ATS 2023)

May 27, 2023/by Justin

Yang Yue, Lier Liu, Li-Jie Wu, Yiran Wu, Ling Wang, Fei Li, Junlin Liu, Gye-Won Han, Bo Chen, Xi Lin, Rebecca L Brouillette, Émile Breault, Jean-Michel Longpré, Songting Shi, Hui Lei, Philippe Sarret, Raymond C Stevens, Michael A Hanson, Fei Xu “Structural insight into apelin receptor-G protein stoichiometry” Nat Struct Mol Biol. 2022 Jul;29(7):688-697. doi: 10.1038/s41594-022-00797-5. Epub 2022 Jul 11.

December 6, 2022/by eallison

C. Martin, L.E. Gimenez, S.Y. Williams, Y. Jing, Y. Wu, C. Hollanders, O. Van der Poorten, S. Gonzalez, K. Van Holsbeeck, S. Previti, A. Lamouroux, S. Zhao, D. Tourwe, R.C. Stevens, R.D. Cone, S. Ballet “Structure based design of melanocortin 4 receptor ligands based on the SHU-9119-hMC4R cocrystal structure.” J. Med. Chem. 64, 357-369 (2021). doi: 10.1021/acs.jmedchem.0c01620.

February 13, 2021/by Admin

J. Singla, K.L. White, R.C. Stevens, F. Abler “Assessment of scoring functions to rank the quality of 3D subtomogram clusters from cryo-electron tomography” J. Struct. Biol. Online 19 Mar (2021). doi: 10.1016/j.jsb.2021.107727.

February 13, 2021/by Admin

Z. Wang, T. Gurlo, A.V. Matveyenko, D. Elashoff, P. Wang, M. Rosenberger, J.A. Junge, R.C. Stevens, K.L. White, S.E. Fraser, P.C. Butler “Live-cell imaging of glucose-induced metabolic coupling of β and α cell metabolism in health and type 2 diabetes” Commun. Biol. 4, 594 (2021). doi: 10.1038/s42003-021-02113-1.

February 13, 2021/by Admin

F. Zhao, C. Zhang, Q. Zhou, K. Hang, X. Zou, Y. Chen, F. Wu, Q. Rao, A. Dai, W. Yin, D.D. Shen, Y. Zhang, T. Xia, R.C. Stevens, H.E. Xu, D. Yang, L. Zhao, M.W. Wang “Structural insights into hormone recognition by the human glucose-dependent insulinotropic polypeptide receptor.” Elife 10, e68719 (2021). doi: 10.7554/eLife.68719.

February 13, 2021/by Admin

M. Audet, K. Villers, J. Velasquez, M. Chu, C. Hanson, R.C. Stevens “Small-scale approach for precrystallization screening in GPCR X-ray crystallography” Nat. Protoc. 15, 144-160 (2020). doi: 10.1038/s41596-019-0259-y.

February 13, 2020/by Admin

R. Lamichhane, J.J. Liu, K.L. White, V. Katritch, R.C. Stevens, K. Wüthrich, D.P. Millar “Biased signaling in the G-protein-coupled receptor β2AR is governed by conformational exchange kinetics” Structure 28, 371-377 (2020). doi: 10.1016/j.str.2020.01.001. PMC7213800.

February 13, 2020/by Admin

Structure Based Discovery and Anti-fibrotic Activity of Novel Antagonists of Lysophosphatidic Acid Receptor 1 (LPAR1) (Presented at ATS 2023)

May 27, 2023/by Justin

A First-in-Human Single/Multiple Ascending Dose Study of ANPA-0073, a Novel Small Molecule G-protein Biased Apelin Receptor Agonist, in Healthy Volunteers (Presented at ATS 2023)

May 27, 2023/by Justin

Discovery of G-protein Biased Small Molecule APJ Agonist for Pulmonary Disease (Presented at ATS 2023)

May 27, 2023/by Justin

Yang Yue, Lier Liu, Li-Jie Wu, Yiran Wu, Ling Wang, Fei Li, Junlin Liu, Gye-Won Han, Bo Chen, Xi Lin, Rebecca L Brouillette, Émile Breault, Jean-Michel Longpré, Songting Shi, Hui Lei, Philippe Sarret, Raymond C Stevens, Michael A Hanson, Fei Xu “Structural insight into apelin receptor-G protein stoichiometry” Nat Struct Mol Biol. 2022 Jul;29(7):688-697. doi: 10.1038/s41594-022-00797-5. Epub 2022 Jul 11.

December 6, 2022/by eallison

C. Martin, L.E. Gimenez, S.Y. Williams, Y. Jing, Y. Wu, C. Hollanders, O. Van der Poorten, S. Gonzalez, K. Van Holsbeeck, S. Previti, A. Lamouroux, S. Zhao, D. Tourwe, R.C. Stevens, R.D. Cone, S. Ballet “Structure based design of melanocortin 4 receptor ligands based on the SHU-9119-hMC4R cocrystal structure.” J. Med. Chem. 64, 357-369 (2021). doi: 10.1021/acs.jmedchem.0c01620.

February 13, 2021/by Admin

J. Singla, K.L. White, R.C. Stevens, F. Abler “Assessment of scoring functions to rank the quality of 3D subtomogram clusters from cryo-electron tomography” J. Struct. Biol. Online 19 Mar (2021). doi: 10.1016/j.jsb.2021.107727.

February 13, 2021/by Admin

Z. Wang, T. Gurlo, A.V. Matveyenko, D. Elashoff, P. Wang, M. Rosenberger, J.A. Junge, R.C. Stevens, K.L. White, S.E. Fraser, P.C. Butler “Live-cell imaging of glucose-induced metabolic coupling of β and α cell metabolism in health and type 2 diabetes” Commun. Biol. 4, 594 (2021). doi: 10.1038/s42003-021-02113-1.

February 13, 2021/by Admin

F. Zhao, C. Zhang, Q. Zhou, K. Hang, X. Zou, Y. Chen, F. Wu, Q. Rao, A. Dai, W. Yin, D.D. Shen, Y. Zhang, T. Xia, R.C. Stevens, H.E. Xu, D. Yang, L. Zhao, M.W. Wang “Structural insights into hormone recognition by the human glucose-dependent insulinotropic polypeptide receptor.” Elife 10, e68719 (2021). doi: 10.7554/eLife.68719.

February 13, 2021/by Admin

M. Audet, K. Villers, J. Velasquez, M. Chu, C. Hanson, R.C. Stevens “Small-scale approach for precrystallization screening in GPCR X-ray crystallography” Nat. Protoc. 15, 144-160 (2020). doi: 10.1038/s41596-019-0259-y.

February 13, 2020/by Admin

R. Lamichhane, J.J. Liu, K.L. White, V. Katritch, R.C. Stevens, K. Wüthrich, D.P. Millar “Biased signaling in the G-protein-coupled receptor β2AR is governed by conformational exchange kinetics” Structure 28, 371-377 (2020). doi: 10.1016/j.str.2020.01.001. PMC7213800.

February 13, 2020/by Admin

F. Wu, L. Yang, K. Hang, M. Laursen, L. Wu, G.W. Han, Q. Ren, N.K. Roed, G. Lin, M.A. Hanson, H. Jiang, M.W. Wang, S. Reedtz-Runge, G. Song, R.C. Stevens “Full-length human GLP-1 receptor structure without orthosteric ligands” Nat. Commun. 11, 1272 (2020). doi: 10.1038/s41467-020-14934-5. PMC7062719.

February 13, 2020/by Admin

J. Yu, L.E. Gimenez, C.C. Hernandez, Y. Wu, A.H. Wein, G.W. Han, K. McClary, S.R. Mittal, K. Burdsall, B. Stauch, L. Wu, S.N. Stevens, A. Peisley, S.Y. Williams, V. Chen, G.L. Millhauser, S. Zhao, R.D. Cone, R.C. Stevens “Determination of the melanocortin-4 receptor structure identifies Ca2+ as a cofactor for ligand binding” Science 368, 428-433 (2020). online 24 April 2020. doi: 10.1126/science.aaz8995. PMC7567314.

February 13, 2020/by Admin

M. Audet, K.L. White, B. Breton, B. Zarzycka, G.W. Han, Y. Lu, C. Gati, A. Batyuk, P. Popov, J. Velasquez, D. Manahan, H. Hu, U. Weierstall, W. Liu, W. Shui, V., Katritch, V. Cherezov, M.A. Hanson, R.C. Stevens “Crystal structure of misoprostol bound to the labor inducer prostaglandin E2 receptor” Nat. Chem. Biol. 15, 11-17 (2019). doi: 10.1038/s41589-018-0160-y. PMC6289721.

February 13, 2019/by Admin

D. Yang, C. de Graaf, L. Yang, G. Song, A. Dai, X. Cai, Y. Feng, S. Reedtz-Runge, M.A. Hanson, H. Yang, H. Jiang, R.C. Stevens, M.W. Wang “Structural determinants of binding the seven-transmembrane domain of the glucagon-like peptide-1 receptor” J. Biol. Chem. 291, 12991-13004 (2016). PMC4933217.

(20)39445-X/fulltext

February 13, 2016/by Admin

X.E. Zhou, X. Gao, A. Barty, Y. Kang, Y. He, W. Liu, A. Ishchenko, T.A. White, O. Yefanov, G.W. Han, Q. Xu, P.W. de Waal, K.M. Suino-Powell, S. Boutet, G.J. Williams, M. Wang, D. Li, M. Caffrey, H.N. Chapman, J.C. Spence, P. Fromme, U. Weierstall, R.C. Stevens, V. Cherezov, K. Melcher, H.E. Xu “X-ray laser diffraction structure determination of the rhodopsin-arrestin complex” Sci. Data 3, 160021 (2016). PMC4828943.

February 13, 2016/by Admin

X. Lv, J. Liu, Q. Shi, Q. Tan, D. Wu, J.J. Skinner, A.L. Walker, L. Zhao, X. Gu, N. Chen, L. Xue, P. Si, L. Zhang, Z. Wang, V. Katritch, Z.J. Liu, R.C. Stevens “In vitro expression and analysis of the 826 human G protein-coupled receptors” Protein Cell 7, 325-337 (2016). PMC4853319.

February 13, 2016/by Admin

S. Yuan, H.C. Chan, H. Vogel, S. Filipek, R.C. Stevens, K. Palczewski “The molecular mechanisms of P2Y1 receptor activation” Angew. Chem. Int. Ed. Engl. 55, 10331-10335 (2016). PMC4996126.

February 13, 2016/by Admin

A. Batyuk, L. Galli, A. Ishchenko, G.W. Han, C. Gati, P.A. Popov, M.Y. Lee, B. Stauch, T.A. White, A. Barty, A. Aquila, M.S. Hunter, M. Liang, S. Boutet, M. Pu, Z.J. Liu, G. Nelson, D. James, C. Li, Y. Zhao, J.C. Spence, W. Liu, P. Fromme, V. Katritch, U. Weierstall, R.C. Stevens, V. Cherezov “Native phasing of x-ray free-electron laser data for a G protein-coupled receptor” Sci. Adv. 2, e1600292 (2016). PMC5035125.

February 13, 2016/by Admin

T. Hua, K. Vemuri, M. Pu, L. Qu, G.W. Han, Y. Wu, S. Zhao, W. Shui, S. Li, A. Korde, R.B. Laprairie, E.L. Stahl, J.-H. Ho, N. Zvonok, H. Zhou, I. Kufareva, B. Wu, Q. Zhao, M.A. Hanson, L.M. Bohn, A. Makriyannis, R.C. Stevens, Z.-J. Liu “Crystal structure of the human cannabinoid receptor CB1” Cell 167, 750-762 (2016). PMC5322940.

February 13, 2016/by Admin

M.T. Eddy, T. Didenko, R.C. Stevens, K. Wüthrich “2-Adrenergic receptor conformational response to fusion protein in the third intracellular loop” Structure 24, 1-8 (2016). PMC5144828.

February 13, 2016/by Admin

Y. Zheng, L. Qin, N.V. Ortiz Zacarias, H. de Vries, G.W. Han, M. Gustavsson, M. Dabros, C. Zhao, R. Cherney, P. Carter, D. Stamos, R. Abagyan, V. Cherezov, R.C. Stevens, A.P. IJzerman, L.H. Heitman, A. Tebben, I. Kufareva, T.M. Handel “Structure of CC Chemokine Receptor 2 with Orthosteric and Allosteric Antagonists” Nature 540, 458-461 (2016). PMC5159191.

February 13, 2016/by Admin

E. Kiselev, R. Balasubramanian, E. Uliassi, K.A. Brown, K. Trujillo, V. Katritch, E. Hammes, R.C. Stevens, T.K. Harden, K.A. Jacobson “Design, synthesis and pharmacological characterization of a fluorescent agonist of the P2Y14 receptor” Bioorg. Med. Chem. Lett. 25, 4733-9 (2015). PMC4607650.

February 13, 2015/by Admin

R. Laminchhane, J.J. Liu, G. Pljevaljcic, K.L. White, E. van der Schans, V. Katritch, R.C. Stevens, K. Wüthrich, D.P. Millar “Single-molecule view of basal activity and activation mechanisms of the G protein-coupled receptor 2AR” Proc. Natl. Acad. Sci. USA 17, 14254-14259 (2015). PMC4655547.

February 13, 2015/by Admin

A.A. Thompson, J.J. Liu, E. Chun, D. Wacker, H. Wu, V. Cherezov, R.C. Stevens. “GPCR stabilization using bicelle-like architecture of mixed sterol-detergent micelles” Methods 55, 310-317 (2011). PMC3264755.

February 13, 2011/by Admin

F. Xu, W. Liu, M.A. Hanson, R.C. Stevens, V. Cherezov “Development of an automated high throughput LCP-FRAP assay to guide membrane protein crystallization in lipid mesophases” Cryst Growth Des 11, 1193-1201 (2011). PMC3108193.

February 13, 2011/by Admin

F. Xu, H. Wu, V. Katritch, G.W. Han, K.A. Jacobson, Z.-G. Gao, V. Cherezov, R.C. Stevens “Structure of an agonist-bound human A2A adenosine receptor” Science 332, 322-327 (2011). PMC3086811.

February 13, 2011/by Admin

T. Shimamura, M. Shiroishi, S. Weyand, H. Tsujimoto, G. Winter, V. Katritch, R. Abagyan, V. Cherezov, W. Liu, G.W. Han, T. Kobayashi, R.C. Stevens, S. Iwata. “Structure of the human histamine H1 receptor in complex with doxepin” Nature 475, 65-70 (2011). PMC3131495.

February 13, 2011/by Admin

C. de Graaf, A.J. Kooistra, H.F. Vischer, V. Katritch, M. Kuijer, M. Shiroshi, S. Iwata, T. Shimamura, R.C. Stevens, I.J.P. de Esch, R. Leurs. “Crystal structure-based virtual screening for novel fragment-like ligands of the human histamine H1 receptor” J Med. Chem. 54, 8195-8206 (2011). PMC3228891.

February 13, 2011/by Admin

I. Kufareva, M. Rueda, V. Katritch, participants of GPCR Dock 2010, R.C. Stevens, R. Abagyan. “Status of GPCR modeling and docking as reflected by community-wide GPCR Dock 2010 assessment” Structure 19, 1108-1126 (2011). PMC3154726.

February 13, 2011/by Admin

V. Cherezov, E. Abola, R.C. Stevens “Toward drug design: Recent progress in the structure determination of GPCRs, a membrane protein family with high potential as pharmaceutical targets” Methods Mol. Biol. 654, 141-168 (2010). PMC2973844.

February 13, 2010/by Admin

C.G. Tate, R.C. Stevens “Growth and excitement in membrane protein structural biology” Curr. Opin. Struct. Biol. 20, 399-400 (2010).

February 13, 2010/by Admin

F. Siu, R.C. Stevens “RAMP-ing up Class B GPCR ECD structural coverage” Structure 18, 1067-1068 (2010).

February 13, 2010/by Admin

B. Wu, E.Y.T. Chien, C.D. Mol, G. Fenalti, W. Liu, V. Katritch, R. Abagyan, A. Brooun, P. Wells, F.C. Bi, D.J. Hamel, P. Kuhn, T.M. Handel, V. Cherezov, R.C. Stevens “Structures of the CXCR4 chemokine GPCR with small molecule and cyclic peptide antagonists” Science 330, 1066-1071 (2010). PMC3074590.

February 13, 2010/by Admin

G. Snell, C. Cork, R. Nordmeyer, E. Cornell, G. Meigs, D. Yegian, J. Jaklevic, J. Jin, R.C. Stevens, T. Earnest “Automated sample mounting and alignment system for biological crystallography at a synchrotron source” Structure 12, 537-545 (2004).

February 13, 2013/by Admin

K.E. Goodwill, M.G. Tennant, R.C. Stevens “High-throughput X-ray crystallography for structure-based drug design” Drug Disc. Today 6, S113-8 (2001).

February 13, 2011/by Admin

D.C. Carter, P. Rhodes, D.E. McRee, L. Tari, D.R. Dougan, G. Snell, E. Abola, R.C. Stevens “Reduction in diffuse-convective disturbances in nanovolume protein crystallization experiments” J. Appl. Crystallogr. 38, 87-90 (2005).

February 13, 2005/by Admin

M. Bern, D. Goldberg, R.C. Stevens, P. Kuhn “Automatic classification of protein crystallization images using a curve tracking algorithm” J. Appl. Cryst. 37, 279-287 (2004).

February 13, 2004/by Admin

R. Page, K. Moy, E.C. Sims, J. Velasquez, B. McManus, C. Grittini, T.L. Clayton, R.C. Stevens “Scalable high-throughput micro-expression device for recombinant proteins” BioTechniques 37, 364-370 (2004).

February 13, 2004/by Admin

R. Page, R.C. Stevens “Crystallization data mining in structural genomics: using positive and negative results to optimize protein crystallization screens.” Methods 34, 373-389 (2004).

February 13, 2004/by Admin

D. Hosfield, J. Palan, M. Hilgers, D. Scheibe, D. McRee, R.C. Stevens “A fully integrated protein crystallization platform for small molecule drug discovery” J. Struct. Biol. 142, 207-217, (2003).

February 13, 2003/by Admin

R.C. Stevens “The cost and value of three-dimensional protein structure” Drug Disc. World 4, 35-48 (2003).

February 13, 2003/by Admin

B.D. Santarsiero, D.T. Yegian, C.C. Lee, G. Spraggon, J. Gu, D. Scheibe, D.C. Uber, E.W. Cornell, R.A. Nordmeyer, W.F. Kolbe, J. Jin, A.L. Jones, J.M. Jaklevic, P. G. Schultz, R.C. Stevens “An approach to rapid protein crystallization using nanodroplets” J. Appl. Crystallogr. 35, 278-281 (2002).

February 13, 2002/by Admin

P. Kuhn, K. Wilson, M.G. Patch, R.C. Stevens “The genesis of high-throughput structure-based drug discovery using protein crystallography” Curr. Opin. Chem. Biol. 6, 704-710 (2002).

February 13, 2002/by Admin