One-pot thiol–amine bioconjugation to maleimides: simultaneous stabilisation and dual functionalisation

Maleimide chemistry is widely used in the site-selective modification of proteins. However, hydrolysis of the resultant thiosuccinimides is required to provide robust stability to the bioconjugates. Herein, we present an alternative approach that affords simultaneous stabilisation and dual functionalisation in a one pot fashion. By consecutive conjugation of a thiol and an amine to dibromomaleimides, we show that aminothiomaleimides can be generated extremely efficiently. Furthermore, the amine serves to deactivate the electrophilicity of the maleimide, precluding further reactivity and hence generating stable conjugates. We have applied this conjugation strategy to peptides and proteins to generate stabilised trifunctional conjugates. We propose that this stabilisation-dual modification strategy could have widespread use in the generation of diverse conjugates.

An alternative approach to maleimide conjugate stabilisation is presented, by the consecutive addition of a thiol and an amine to dibromomaleimides. The amine serves to simultaneously deactivate the maleimide and enable dual functionalisation.     

Successive-minima-type inequalities

We show analogues of Minkowski's theorem on successive minima, where the volume is replaced by the lattice point enumerator. We further give analogous results to some recent theorems by Kannan and Lovász on covering minima.     

Geometric realizations for Dyck's regular map on a surface of genus 3

Klein's and Dyck's regular maps on Riemann surfaces of genus 3 were one impetus for the theory of regular maps, automorphic functions, and algebraic curves. Recently a polyhedral realization inE ³ of Klein's map was discovered [18], thereby underlining the strong analogy to the icosahedron. In this paper we show that Dyck's map can be realized inE ³ as a polyhedron of Kepler-Poinsot-type, i.e., with maximal symmetry and minimal self-intersections. Furthermore some closely related polyhedra and a Kepler-Poinsot-type realization of Sherk's regular map of genus 5 are discussed.     

Mirroring doubly excited resonances in argon

New features are revealed in the low-energy photoionization spectrum of Ar by critically combining high photon resolution and differential photoelectron spectroscopic techniques. Two LS-forbidden doubly excited resonances are seen in the 3p(-1)(3/2, 1/2) partial cross sections which exhibit mirroring profiles, resulting in complete cancellation in the total photoionization cross section, as was predicted by Liu and Starace [Phys. Rev. A 59, R1731 (1999)]. These results demonstrate that a new class of weakly spin-orbit induced, mirroring resonances should be observable in partial, but not in total, collisional cross sections involving atoms, molecules, and solids in general.     

Polyhedral 2-manifolds inE 3 with unusually large genus

An equivelar polyhedral 2-manifold in the class ?_p,q is one embedded inE ³ in which every face is a convexp-gon and every vertex isq-valent. In this paper, examples are constructed, to show that each of the classes ?_3,q (q≧7), ?_4,q (q≧5) and ?_p,4 (p≧5) contains infinitely many distinct combinatorial types. As particular examples, there are polyhedral 2-manifolds with 576 vertices and genus 577, and with 4096 faces and genus 4097. A modification of one construction shows that there is a constantk, such that for eachg≧2, there exists a closed polyhedral 2-manifold inE ³ of genusg with at mostkg/logg vertices.     

Untere Schranken für zwei diophantische Approximations-Funktionen

Ohne Zusammenfassung     

Symmetrisierung an Unterräumen

Ohne Zusammenfassung     

On finite multiple packings

Dedicated to Professor Dr. August Florian on the occasion of his sixtieth birthday     

Analytische Fortsetzung durch ein Limitierungsverfahren

Ohne ZusammenfassungHerrn Prof. Dr. Ernst Mohr zum 60. Geburtstag