8ERA

RMC-5552 in complex with mTORC1 and FKBP12

Summary for 8ERA

• Entry DOI: 10.2210/pdb8era/pdb
• EMDB information: 28551
• Descriptor: Serine/threonine-protein kinase mTOR, Peptidyl-prolyl cis-trans isomerase FKBP1A, Target of rapamycin complex subunit LST8, ... (6 entities in total)
• Functional Keywords: antitumor, mtorc1, complex (isomerase-kinase) complex, complex (isomerase/kinase)
• Biological source: Homo sapiens (human); More
• Total number of polymer chains: 4
• Total formula weight: 487692.36

Authors

Tomlinson, A.C.A.,Yano, J.K. (deposition date: 2022-10-11, release date: 2022-12-28, Last modification date: 2023-01-25)

• Primary citation: Burnett, G.L.,Yang, Y.C.,Aggen, J.B.,Pitzen, J.,Gliedt, M.K.,Semko, C.M.,Marquez, A.,Evans, J.W.,Wang, G.,Won, W.S.,Tomlinson, A.C.A.,Kiss, G.,Tzitzilonis, C.,Thottumkara, A.P.,Cregg, J.,Mellem, K.T.,Choi, J.S.,Lee, J.C.,Zhao, Y.,Lee, B.J.,Meyerowitz, J.G.,Knox, J.E.,Jiang, J.,Wang, Z.,Wildes, D.,Wang, Z.,Singh, M.,Smith, J.A.M.,Gill, A.L.; Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors.; J.Med.Chem., 66:149-169, 2023; PubMed: 36533617; DOI: 10.1021/acs.jmedchem.2c01658

Experimental method

ELECTRON MICROSCOPY (2.86 Å)