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Title | Tumor Targeting with Novel 6-Substituted Pyrrolo [2,3-d] Pyrimidine Antifolates with Heteroatom Bridge Substitutions via Cellular Uptake by Folate Receptor alpha and the Proton-Coupled Folate Transporter and Inhibition of de Novo Purine Nucleotide Biosynthesis. |
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Journal, issue, pages | J. Med. Chem., Vol. 59, Page 7856-7876, Year 2016 |
Publish date | Mar 25, 2016 (structure data deposition date) |
![]() | Golani, L.K. / Wallace-Povirk, A. / Deis, S.M. / Wong, J. / Ke, J. / Gu, X. / Raghavan, S. / Wilson, M.R. / Li, X. / Polin, L. ...Golani, L.K. / Wallace-Povirk, A. / Deis, S.M. / Wong, J. / Ke, J. / Gu, X. / Raghavan, S. / Wilson, M.R. / Li, X. / Polin, L. / de Waal, P.W. / White, K. / Kushner, J. / O'Connor, C. / Hou, Z. / Xu, H.E. / Melcher, K. / Dann, C.E. / Matherly, L.H. / Gangjee, A. |
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Methods | X-ray diffraction |
Resolution | 2.1 - 3.6 Å |
Structure data | ![]() PDB-5izq: ![]() PDB-5j9f: |
Chemicals | ![]() ChemComp-83A: ![]() ChemComp-GAR: ![]() ChemComp-HOH: |
Source |
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![]() | SIGNALING PROTEIN / Folate receptor alpha / antifolate / tumor targeting / 2-Amino-4-oxo-6-substituted pyrrolo[2 / 3-d]pyrimidine / ligase/ligase inhibitor / gar transformylase / ligase-ligase inhibitor complex |