Entry Database : PDB / ID : 8t6g Structure visualization Downloads & linksTitle Identification of GDC-1971 (RLY-1971), a SHP2 inhibitor designed for the treatment of solid tumors ComponentsTyrosine-protein phosphatase non-receptor type 11 Details Keywords HYDROLASE / Phosphatase / Tumor target / inhibitorFunction / homology Function and homology informationFunction Domain/homology Component
negative regulation of cortisol secretion / intestinal epithelial cell migration / microvillus organization / negative regulation of growth hormone secretion / genitalia development / multicellular organismal reproductive process / atrioventricular canal development / negative regulation of cell adhesion mediated by integrin / STAT5 Activation / Netrin mediated repulsion signals ... negative regulation of cortisol secretion / intestinal epithelial cell migration / microvillus organization / negative regulation of growth hormone secretion / genitalia development / multicellular organismal reproductive process / atrioventricular canal development / negative regulation of cell adhesion mediated by integrin / STAT5 Activation / Netrin mediated repulsion signals / positive regulation of hormone secretion / cerebellar cortex formation / regulation of protein export from nucleus / positive regulation of ossification / hormone metabolic process / Interleukin-37 signaling / negative regulation of chondrocyte differentiation / Signaling by Leptin / MET activates PTPN11 / Regulation of RUNX1 Expression and Activity / face morphogenesis / ERBB signaling pathway / Costimulation by the CD28 family / Signal regulatory protein family interactions / peptide hormone receptor binding / platelet formation / megakaryocyte development / negative regulation of type I interferon production / organ growth / triglyceride metabolic process / CTLA4 inhibitory signaling / Platelet sensitization by LDL / Interleukin-20 family signaling / PI-3K cascade:FGFR3 / Interleukin-6 signaling / STAT5 activation downstream of FLT3 ITD mutants / PI-3K cascade:FGFR2 / Prolactin receptor signaling / PI-3K cascade:FGFR4 / PI-3K cascade:FGFR1 / MAPK3 (ERK1) activation / PECAM1 interactions / MAPK1 (ERK2) activation / regulation of cell adhesion mediated by integrin / regulation of type I interferon-mediated signaling pathway / Bergmann glial cell differentiation / phosphoprotein phosphatase activity / inner ear development / neurotrophin TRK receptor signaling pathway / platelet-derived growth factor receptor signaling pathway / non-membrane spanning protein tyrosine phosphatase activity / RET signaling / peptidyl-tyrosine dephosphorylation / Interleukin-3, Interleukin-5 and GM-CSF signaling / Regulation of IFNA/IFNB signaling / PI3K Cascade / PD-1 signaling / regulation of protein-containing complex assembly / ephrin receptor signaling pathway / fibroblast growth factor receptor signaling pathway / GAB1 signalosome / Activated NTRK2 signals through FRS2 and FRS3 / negative regulation of insulin secretion / Regulation of IFNG signaling / positive regulation of insulin receptor signaling pathway / FRS-mediated FGFR3 signaling / Signaling by CSF3 (G-CSF) / Signaling by FLT3 ITD and TKD mutants / homeostasis of number of cells within a tissue / FRS-mediated FGFR2 signaling / FRS-mediated FGFR4 signaling / Tie2 Signaling / FRS-mediated FGFR1 signaling / cellular response to epidermal growth factor stimulus / GPVI-mediated activation cascade / cell adhesion molecule binding / T cell costimulation / FLT3 Signaling / positive regulation of interferon-beta production / hormone-mediated signaling pathway / phosphotyrosine residue binding / protein dephosphorylation / Downstream signal transduction / positive regulation of mitotic cell cycle / protein-tyrosine-phosphatase / protein tyrosine kinase binding / axonogenesis / Activation of IRF3, IRF7 mediated by TBK1, IKKε (IKBKE) / DNA damage checkpoint signaling / protein tyrosine phosphatase activity / integrin-mediated signaling pathway / positive regulation of glucose import / Negative regulation of FGFR3 signaling / Negative regulation of FGFR2 signaling / Negative regulation of FGFR4 signaling / Negative regulation of FGFR1 signaling / insulin receptor binding / Spry regulation of FGF signaling / brain development / epidermal growth factor receptor signaling pathway Similarity search - Function Protein-tyrosine phosphatase, non-receptor type-6, -11 / Protein tyrosine phosphatase, catalytic domain / PTP type protein phosphatase domain profile. / Protein-tyrosine phosphatase / Tyrosine-specific protein phosphatase, PTPase domain / Protein-tyrosine phosphatase, catalytic / Protein tyrosine phosphatase, catalytic domain motif / Tyrosine specific protein phosphatases active site. / Protein-tyrosine phosphatase, active site / Tyrosine-specific protein phosphatases domain ... Protein-tyrosine phosphatase, non-receptor type-6, -11 / Protein tyrosine phosphatase, catalytic domain / PTP type protein phosphatase domain profile. / Protein-tyrosine phosphatase / Tyrosine-specific protein phosphatase, PTPase domain / Protein-tyrosine phosphatase, catalytic / Protein tyrosine phosphatase, catalytic domain motif / Tyrosine specific protein phosphatases active site. / Protein-tyrosine phosphatase, active site / Tyrosine-specific protein phosphatases domain / Tyrosine specific protein phosphatases domain profile. / Protein-tyrosine phosphatase-like / SH2 domain / Src homology 2 (SH2) domain profile. / Src homology 2 domains / SH2 domain / SH2 domain superfamily Similarity search - Domain/homologyBiological species Homo sapiens (human)Method X-RAY DIFFRACTION / SYNCHROTRON / MOLECULAR REPLACEMENT / Resolution : 1.84 Å DetailsAuthors Tang, Y. / Nugyen, V. / Wilbur, J.D. Funding support 1items Details Hide detailsOrganization Grant number Country Other private
CitationJournal : J.Med.Chem. / Year : 2023Title : Identification of GDC-1971 (RLY-1971), a SHP2 Inhibitor Designed for the Treatment of Solid Tumors.Authors: Taylor, A.M. / Williams, B.R. / Giordanetto, F. / Kelley, E.H. / Lescarbeau, A. / Shortsleeves, K. / Tang, Y. / Walters, W.P. / Arrazate, A. / Bowman, C. / Brophy, E. / Chan, E.W. / ... Authors : Taylor, A.M. / Williams, B.R. / Giordanetto, F. / Kelley, E.H. / Lescarbeau, A. / Shortsleeves, K. / Tang, Y. / Walters, W.P. / Arrazate, A. / Bowman, C. / Brophy, E. / Chan, E.W. / Deshmukh, G. / Greisman, J.B. / Hunsaker, T.L. / Kipp, D.R. / Saenz Lopez-Larrocha, P. / Maddalo, D. / Martin, I.J. / Maragakis, P. / Merchant, M. / Murcko, M. / Nisonoff, H. / Nguyen, V. / Nguyen, V. / Orozco, O. / Owen, C. / Pierce, L. / Schmidt, M. / Shaw, D.E. / Smith, S. / Therrien, E. / Tran, J.C. / Watters, J. / Waters, N.J. / Wilbur, J. / Willmore, L. History Deposition Jun 15, 2023 Deposition site : RCSB / Processing site : RCSBRevision 1.0 Oct 11, 2023 Provider : repository / Type : Initial releaseRevision 1.1 Oct 25, 2023 Group : Database references / Category : citation / citation_authorItem : _citation.journal_volume / _citation.page_first ... _citation.journal_volume / _citation.page_first / _citation.page_last / _citation_author.identifier_ORCID
Show all Show less