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Literature DB >> 22996816

Metal-bis(2-picolyl)amine complexes as state 1(T) inhibitors of activated Ras protein.

Ina C Rosnizeck¹, Michael Spoerner, Tobias Harsch, Sandra Kreitner, Daniel Filchtinski, Christian Herrmann, Daniel Engel, Burkhard König, Hans Robert Kalbitzer.

Abstract

Allosteric interactions: Metal(II) cyclens inhibit Ras-effector interactions by stabilizing a weak effector-binding state of Ras, state 1(T), and binding directly in the active site. The novel state (1T) inhibitor Zn(2+)-BPA (BPA = bis(2-picolyl)amine) binds outside the nucleotide binding pocket but nevertheless allosterically stabilizes state 1(T) and thus inhibits the Ras-Raf interaction.

Entities: Chemical Gene

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Year: 2012 PMID： 22996816 DOI： 10.1002/anie.201204148

Source DB: PubMed Journal: Angew Chem Int Ed Engl ISSN： 1433-7851 Impact factor: 15.336

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Cited

19 in total

Review 1. Drugging Ras GTPase: a comprehensive mechanistic and signaling structural view.

Authors: Shaoyong Lu; Hyunbum Jang; Shuo Gu; Jian Zhang; Ruth Nussinov
Journal: Chem Soc Rev Date: 2016-07-11 Impact factor: 54.564

2. High pressure ³¹P NMR spectroscopy on guanine nucleotides.

Authors: Michael Spoerner; Matthias Karl; Pedro Lopes; Marcus Hoering; Karoline Loeffel; Andrea Nuehs; Joseph Adelsberger; Werner Kremer; Hans Robert Kalbitzer
Journal: J Biomol NMR Date: 2016-12-23 Impact factor: 2.835

Review 3. The RAS-Effector Interaction as a Drug Target.

Authors: Adam B Keeton; E Alan Salter; Gary A Piazza
Journal: Cancer Res Date: 2017-01-06 Impact factor: 12.701

4. Pressure dependence of side chain ¹³C chemical shifts in model peptides Ac-Gly-Gly-Xxx-Ala-NH₂.

Authors: Markus Beck Erlach; Joerg Koehler; Edson Crusca; Claudia E Munte; Masatsune Kainosho; Werner Kremer; Hans Robert Kalbitzer
Journal: J Biomol NMR Date: 2017-09-14 Impact factor: 2.835

5. Binding hotspots on K-ras: consensus ligand binding sites and other reactive regions from probe-based molecular dynamics analysis.

Authors: Priyanka Prakash; John F Hancock; Alemayehu A Gorfe
Journal: Proteins Date: 2015-03-25

Metal-bis(2-picolyl)amine complexes as state 1(T) inhibitors of activated Ras protein.

Review 1. Drugging Ras GTPase: a comprehensive mechanistic and signaling structural view.

2. High pressure ³¹P NMR spectroscopy on guanine nucleotides.

Review 3. The RAS-Effector Interaction as a Drug Target.

4. Pressure dependence of side chain ¹³C chemical shifts in model peptides Ac-Gly-Gly-Xxx-Ala-NH₂.

5. Binding hotspots on K-ras: consensus ligand binding sites and other reactive regions from probe-based molecular dynamics analysis.

Review 6. Small-molecule modulation of Ras signaling.

Review 7. Lessons from computer simulations of Ras proteins in solution and in membrane.

8. Overview of simulation studies on the enzymatic activity and conformational dynamics of the GTPase Ras.

9. Pressure dependence of backbone chemical shifts in the model peptides Ac-Gly-Gly-Xxx-Ala-NH2.

10. Andrographolide derivatives inhibit guanine nucleotide exchange and abrogate oncogenic Ras function.

Metal-bis(2-picolyl)amine complexes as state 1(T) inhibitors of activated Ras protein.

Review 1. Drugging Ras GTPase: a comprehensive mechanistic and signaling structural view.

2. High pressure 31P NMR spectroscopy on guanine nucleotides.

Review 3. The RAS-Effector Interaction as a Drug Target.

4. Pressure dependence of side chain 13C chemical shifts in model peptides Ac-Gly-Gly-Xxx-Ala-NH2.

5. Binding hotspots on K-ras: consensus ligand binding sites and other reactive regions from probe-based molecular dynamics analysis.

Review 6. Small-molecule modulation of Ras signaling.

Review 7. Lessons from computer simulations of Ras proteins in solution and in membrane.

8. Overview of simulation studies on the enzymatic activity and conformational dynamics of the GTPase Ras.

9. Pressure dependence of backbone chemical shifts in the model peptides Ac-Gly-Gly-Xxx-Ala-NH2.

10. Andrographolide derivatives inhibit guanine nucleotide exchange and abrogate oncogenic Ras function.

2. High pressure ³¹P NMR spectroscopy on guanine nucleotides.

4. Pressure dependence of side chain ¹³C chemical shifts in model peptides Ac-Gly-Gly-Xxx-Ala-NH₂.