Experts and Doctors on substrate specificity in Dortmund, North Rhine Westphalia, Germany


Locale: Dortmund, North Rhine Westphalia, Germany
Topic: substrate specificity

Top Publications

  1. Alexandrov K, Simon I, Yurchenko V, Iakovenko A, Rostkova E, Scheidig A, et al. Characterization of the ternary complex between Rab7, REP-1 and Rab geranylgeranyl transferase. Eur J Biochem. 1999;265:160-70 pubmed
    ..Based on these experiments, we propose that RabGGTase recognizes the overall structure arising from the association of Rab and REP and then 'scans' the flexible C-terminus to position the proximal cysteines into the active site. ..
  2. Esser D, Bauer B, Wolthuis R, Wittinghofer A, Cool R, Bayer P. Structure determination of the Ras-binding domain of the Ral-specific guanine nucleotide exchange factor Rlf. Biochemistry. 1998;37:13453-62 pubmed
    ..Raf-RBD. However, comparison of the putatively interacting regions revealed structural differences which are proposed to be responsible for the different substrate affinities of Rlf-, RalGDS-, and Raf-RBD. ..
  3. Thomä N, Iakovenko A, Kalinin A, Waldmann H, Goody R, Alexandrov K. Allosteric regulation of substrate binding and product release in geranylgeranyltransferase type II. Biochemistry. 2001;40:268-74 pubmed
    ..In summary, these results demonstrate that GGpp acts as an allosteric activator that stabilizes the Rab7:REP-1:GGTase-II complex and triggers product release upon prenylation, preventing product inhibition of the enzyme. ..
  4. Clerc J, Groll M, Illich D, Bachmann A, Huber R, Schellenberg B, et al. Synthetic and structural studies on syringolin A and B reveal critical determinants of selectivity and potency of proteasome inhibition. Proc Natl Acad Sci U S A. 2009;106:6507-12 pubmed publisher
    ..In light of the medicinal relevance of proteasome inhibitors as anticancer compounds, the present findings may assist in the rational design and development of syrbactin-based chemotherapeutics. ..
  5. Walter N, Wentsch H, Bührmann M, Bauer S, Döring E, Mayer Wrangowski S, et al. Design, Synthesis, and Biological Evaluation of Novel Type I1/2 p38? MAP Kinase Inhibitors with Excellent Selectivity, High Potency, and Prolonged Target Residence Time by Interfering with the R-Spine. J Med Chem. 2017;60:8027-8054 pubmed publisher
    ..Moreover, microsomal studies showed convenient metabolic stability of the most potent, herein reported representatives. ..
  6. Venne A, Vögtle F, Meisinger C, Sickmann A, Zahedi R. Novel highly sensitive, specific, and straightforward strategy for comprehensive N-terminal proteomics reveals unknown substrates of the mitochondrial peptidase Icp55. J Proteome Res. 2013;12:3823-30 pubmed publisher
    ..Thus, ChaFRADIC is a powerful and practicable tool for protease and peptidase research, providing the sensitivity to characterize even samples that can be obtained only in small quantities. ..
  7. Primorac I, Musacchio A. Panta rhei: the APC/C at steady state. J Cell Biol. 2013;201:177-89 pubmed publisher
    ..Here, we review how these recent advancements are modifying our understanding of the APC/C. ..
  8. Bürger M, Zimmermann T, Kondoh Y, Stege P, Watanabe N, Osada H, et al. Crystal structure of the predicted phospholipase LYPLAL1 reveals unexpected functional plasticity despite close relationship to acyl protein thioesterases. J Lipid Res. 2012;53:43-50 pubmed publisher
    ..Furthermore, extensive screening efforts using chemical array technique revealed a first small molecule inhibitor of LYPLAL1. ..
  9. Subramanian S, Glitz P, Kipp H, Kinne R, Castaneda F. Protein kinase-A affects sorting and conformation of the sodium-dependent glucose co-transporter SGLT1. J Cell Biochem. 2009;106:444-52 pubmed publisher
    ..Thus, PKA-mediated phosphorylation of the transporter represents a further mechanism in the regulation of SGLT1-mediated glucose transport in epithelial cells, in addition to a change in surface membrane expression. ..

Scientific Experts

More Information


  1. Fricke I, Berken A. Molecular basis for the substrate specificity of plant guanine nucleotide exchange factors for ROP. FEBS Lett. 2009;583:75-80 pubmed publisher
    ..These data also provide first evidence for a function of the Rho insert in interactions with GEFs. ..
  2. Lammers M, Meyer S, Kühlmann D, Wittinghofer A. Specificity of interactions between mDia isoforms and Rho proteins. J Biol Chem. 2008;283:35236-46 pubmed publisher
    ..We also show that the F106H and H104F mutations drastically alter the affinities and thermodynamics of mDia interactions. ..
  3. Kurpiers T, Mootz H. Site-specific chemical modification of proteins with a prelabelled cysteine tag using the artificially split Mxe GyrA intein. Chembiochem. 2008;9:2317-25 pubmed publisher
    ..Our approach combines the benefits of the plethora of commercially available cysteine-reactive probes with a straightforward route for their site-specific incorporation even into complex and cysteine-rich proteins. ..
  4. Meyer S, Scrima A, Vers es W, Wittinghofer A. Crystal structures of the conserved tRNA-modifying enzyme GidA: implications for its interaction with MnmE and substrate. J Mol Biol. 2008;380:532-47 pubmed publisher
    ..We propose a model for the interaction between GidA and MnmE, which is supported by site-directed mutagenesis. Our data suggest that this interaction is modulated and potentially regulated by the switch function of the G domain of MnmE...
  5. Berken A, Thomas C, Wittinghofer A. A new family of RhoGEFs activates the Rop molecular switch in plants. Nature. 2005;436:1176-80 pubmed
    ..RopGEFs may represent the missing link in signal transduction from receptor kinases to Rops and their identification has implications for the evolution of the Rho molecular switch. ..
  6. Fedorov R, Hartmann E, Ghosh D, Schlichting I. Structural basis for the specificity of the nitric-oxide synthase inhibitors W1400 and Nomega-propyl-L-Arg for the inducible and neuronal isoforms. J Biol Chem. 2003;278:45818-25 pubmed
    ..This flexibility is determined by isoform-specific residues outside the active site. ..
  7. Ostermann N, Segura Peña D, Meier C, Veit T, Monnerjahn C, Konrad M, et al. Structures of human thymidylate kinase in complex with prodrugs: implications for the structure-based design of novel compounds. Biochemistry. 2003;42:2568-77 pubmed
    ..Our results show the drastic effects that slight modifications of the substrates exert on the enzyme's conformation and, hence, activity and suggest the type of substitutions that are compatible with efficient phosphorylation by TMPK. ..
  8. Dursina B, Thoma N, Sidorovitch V, Niculae A, Iakovenko A, Rak A, et al. Interaction of yeast Rab geranylgeranyl transferase with its protein and lipid substrates. Biochemistry. 2002;41:6805-16 pubmed
    ..Despite the ability to function in concert with yRabGGTase in vitro, expression of mammalian REP-1 could not complement deletion of MRS6 gene in S. cerevisiae in vivo. The implications of these findings are discussed. ..
  9. Weyand M, Schlichting I. Crystal structure of wild-type tryptophan synthase complexed with the natural substrate indole-3-glycerol phosphate. Biochemistry. 1999;38:16469-80 pubmed
    ..These findings form the structural basis for the information transfer from the alpha- to the beta-subunit and may explain the affinity increase of the beta-active site for serine upon IGP binding. ..