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A Left‐Handed Solution to Peptide Inhibition of the p53–MDM2 Interaction

10.05.2010 | Liu, Min; Pazgier, Marzena; Li, Changqing; Yuan, Weirong; Li, Chong; Lu, Wuyuan, Angewandte Chemie International Edition, 2010

Throwing tumors a left-hook punch: The oncoprotein MDM2 negatively regulates the activity and stability of the tumor suppressor protein p53, and is an important molecular target for anticancer therapy. Mirror-image phage display identifies a high-affinity D-peptide ligand of MDM2 (see structure) ...


Porphyrin “Lego Block” Strategy To Construct Directly meso–β Doubly Linked Porphyrin Rings

10.05.2010 | Song, Jianxin; Aratani, Naoki; Kim, Pyosang; Kim, Dongho; Shinokubo, Hiroshi; Osuka, Atsuhiro, Angewandte Chemie International Edition, 2010

Clicking together: The Suzuki-Miyaura coupling of [beta],[beta][prime]-diborylated porphyrin blocks and meso,meso[prime]-dibrominated porphyrin blocks is used for the construction of directly meso-[beta] doubly linked porphyrin rings including two tetraporphyrin rings, hexaporphyrin rings, and a ...


Tetrazine Phototriggers: Probes for Peptide Dynamics

10.05.2010 | Tucker, Matthew J.; Courter, Joel R.; Chen, Jianxin; Atasoylu, Onur; Smith III, Amos B.; Hochst ..., Angewandte Chemie International Edition, 2010

Surrender your secrets, peptides! Of several 3,6-disubstituted tetrazines examined as phototriggers for the investigation of peptide dynamics, the most useful candidates were disulfenyl tetrazines. The thiocyanate fragments resulting from photolysis (see scheme) were detected by ultrafast ...


Directed Orthogonal Self‐Assembly of Homochiral Coordination Polymers for Heterogeneous Enantioselective Hydrogenation

10.05.2010 | Yu, Liting; Wang, Zheng; Wu, Jiang; Tu, Shujiang; Ding, Kuiling, Angewandte Chemie International Edition, 2010

Three in one: Orthogonal coordination of FeII and RhI with a single heteroditopic ligand results in the formation of self-supported heterogeneous chiral catalysts (see scheme). The compounds are highly active, enantioselective, and reusable in the heterogeneous asymmetric hydrogenation of various ...


Halomethane Biosynthesis: Structure of a SAM‐Dependent Halide Methyltransferase from Arabidopsis thaliana

10.05.2010 | Schmidberger, Jason W.; James, Agata B.; Edwards, Robert; Naismith, James H.; O'Hagan, David, Angewandte Chemie International Edition, 2010

It's a gas! The structure of the halomethane-producing halo/thiocyanate methyltransferase enzyme from plants has been determined. The halide ion and the methyl group of S-adenosyl-L-methionine (SAM) are modeled into the active site (see picture; chloride: green sphere; SAM: C green, O red, S ...


Fully Synthetic Vaccines Consisting of Tumor‐Associated MUC1 Glycopeptides and a Lipopeptide Ligand of the Toll‐like Receptor 2

10.05.2010 | Kaiser, Anton; Gaidzik, Nikola; Becker, Torsten; Menge, Clara; Groh, Kai; Cai, Hui; Li, Yan‐Mei; Gerlitzki, B ..., Angewandte Chemie International Edition, 2010

Fragment condensation of a protected Pam3Cys lipopeptide with unprotected tumor-associated MUC1 glycopeptides opens the way to vaccine candidates like A. These vaccines elicit selective immune responses in mice although they lack an immunodominant carrier protein. In principle, such vaccines are ...


Trapping a Difluorocarbene-Platinum Fragment by Base Coordination

06.05.2010 | Sonia Martínez-Salvador, Babil Menjón, Juan Forniés, Antonio Martín, Isabel Usón, Angewandte Chemie International Edition, 2010

Caught in the act: Evidence for the intermediacy of difluorocarbene-platinum species along the acidic degradation of Pt[bond]CF3 bonds was gained by trapping a base-stabilized Pt[double bond]CF2 moiety (see scheme). Attack of an N nucleophile (py*) to the highly electrophilic and extremely ...


Highly Enantioselective Conjugate Addition of Thioglycolate to Chalcones Catalyzed by Lanthanum: Low Catalyst Loading and Remarkable Chiral Amplification

06.05.2010 | Yonghai Hui, Jun Jiang, Wentao Wang, Weiliang Chen, Yunfei Cai, Lili Lin, Xiaohua Liu, Xiaoming Feng, Angewandte Chemie International Edition, 2010

Ramping it up: The titled reaction has been developed using a chiral N,N[prime]-dioxide-LaIII complex as the catalyst. The reaction proceeded with high yield and enantioselectivity. Remarkably, a high asymmetric amplification was observed, as 98 % ee was achieved using 1 mol % L/La(OTf)3 in which ...


Highly Active Chiral Ruthenium-Based Metathesis Catalysts through a Monosubstitution in the N-Heterocyclic Carbene

05.05.2010 | Sascha Tiede, Anke Berger, David Schlesiger, Daniel Rost, Anja Lühl, Siegfried Blechert, Angewandte Chemie International Edition, 2010

One handed is very efficient, not only for fiddler crabs, but also for chiral ruthenium metathesis (pre)catalysts that contain a monosubstituted carbon center in the N-heterocyclic ligand. In their Communication (DOI: ) S. Blechert and co-workers show that the combination of ligands results in ...


Self-Assembly of Thermally Responsive Amphiphilic Diblock Copolypeptides into Spherical Micellar Nanoparticles

05.05.2010 | Wookhyun Kim, Julie Thévenot, Emmanuel Ibarboure, Sébastien Lecommandoux, Elliot L. Chaikof, Angewandte Chemie International Edition, 2010

Stable micellar structures were synthesized containing cysteine residues at the diblock interface to stabilize micellar structure (see picture). Self-assembly of these copolypeptides affords a new class of protein nanoparticles with potential applications in drug-delivery and bioimaging.


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