2j9m
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CRYSTAL STRUCTURE OF CDK2 IN COMPLEX WITH MACROCYCLIC AMINOPYRIMIDINE
OverviewOverview
X-ray structures from CDK2-aminopyrimidine inhibitor complexes led to the, idea to stabilize the active conformation of aminopyrimidine inhibitors by, incorporating the recognition site into a macrocyclic framework. A modular, synthesis approach that relies on a new late-stage macrocyclization, protocol that enables fast and efficient synthesis of macrocyclic, aminopyrimidines was developed. A set of structurally diverse derivatives, was prepared. Macrocyclic aminopyrimidines were shown to be multitarget, inhibitors of CDK1/2 and VEGF-RTKs. In addition, potent antiproliferative, activities toward various human tumor cells and a human tumor xenograft, model were demonstrated.
About this StructureAbout this Structure
2J9M is a Single protein structure of sequence from Homo sapiens with PY8 as ligand. Active as Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 Structure known Active Site: AC1. Full crystallographic information is available from OCA.
ReferenceReference
Macrocyclic Aminopyrimidines as Multitarget CDK and VEGF-R Inhibitors with Potent Antiproliferative Activities., Lucking U, Siemeister G, Schafer M, Briem H, Kruger M, Lienau P, Jautelat R, ChemMedChem. 2007 Jan 15;2(1):63-77. PMID:17131463
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- Homo sapiens
- Non-specific serine/threonine protein kinase
- Single protein
- Briem, H.
- Jautelat, R.
- Krueger, M.
- Lienau, P.
- Luecking, U.
- Schaefer, M.
- Siemeister, G.
- PY8
- Arylamine n-acetyltransferase
- Atp-binding
- Cell cycle
- Cell division
- Drug metabolism
- Isoniazid
- Kinase
- Mitosis
- Mycobacteria
- Nat
- Nucleotide-binding
- Phosphorylation
- Polymorphism
- Serine-threonine protein kinase
- Serine/threonine-protein kinase
- Transferase