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Dimerization of the EphA1 Receptor Tyrosine Kinase Transmembrane Domain: Insights into the Mechanism of Receptor Activation

17.10.2014 | Matthieu Chavent; Alan P. Chetwynd; Phillip J. Stansfeld; Mark S. P. Sansom, Biochemistry, 2014

EphA1 is a receptor tyrosine kinase (RTK) that plays a key role in developmental processes, including guidance of the migration of axons and cells in the nervous system. EphA1, in common with other RTKs, contains an N-terminal extracellular domain, a single transmembrane (TM) α-helix, and a ...


Increasing Efficiency in Protein–Protein Coupling: Subunit-Directed Acetylation and Phase-Directed CuAAC (“Click Coupling”) in the Formation of Hemoglobin Bis-Tetramers

17.10.2014 | Aizhou Wang; Ronald Kluger, Biochemistry, 2014

Cross-linked human hemoglobins have been evaluated for clinical use as circulating oxygen carriers. However, their induction of vasoactivity was sufficiently problematic to lead to the cessation of clinical trials. The source of vasoactivity is likely to be endothelial extravasation causing the ...


n-Alkylboronic Acid Inhibitors Reveal Determinants of Ligand Specificity in the Quorum-Quenching and Siderophore Biosynthetic Enzyme PvdQ

17.10.2014 | Kenneth D. Clevenger; Rui Wu; Dali Liu; Walter Fast, Biochemistry, 2014

The enzyme PvdQ (E.C. from Pseudomonas aeruginosa is an N-terminal nucleophile hydrolase that catalyzes the removal of an N-myristyl substituent from a biosynthetic precursor of the iron-chelating siderophore pyoverdine. Inhibitors of pyoverdine biosynthesis are potential antibiotics ...


Polyglutamine Amyloid Core Boundaries and Flanking Domain Dynamics in Huntingtin Fragment Fibrils Determined by Solid-State Nuclear Magnetic Resonance

16.10.2014 | Cody L. Hoop; Hsiang-Kai Lin; Karunakar Kar; Zhipeng Hou; Michelle A. Poirier; Ronald Wetzel; Patrick C. A. van der Wel, Biochemistry, 2014

In Huntington’s disease, expansion of a polyglutamine (polyQ) domain in the huntingtin (htt) protein leads to misfolding and aggregation. There is much interest in the molecular features that distinguish monomeric, oligomeric, and fibrillar species that populate the aggregation pathway and likely ...


Activation of BNGR-A24 by Direct Interaction with Tachykinin-Related Peptides from the Silkworm Bombyx mori Leads to the Gq- and Gs-Coupled Signaling Cascades

16.10.2014 | Xiaobai He; Jiashu Zang; Xiangmei Li; Jiajie Shao; Huipeng Yang; Jingwen Yang; Haishan Huang; Linjie Chen; Liangen S ..., Biochemistry, 2014

Tachykinins constitute one of the largest peptide families in the animal kingdom and exert their diverse actions via G protein-coupled receptors (GPCRs). In this study, the Bombyx tachykinin-related peptides (TKRPs) were identified as specific endogenous ligands for the Bombyx neuropeptide GPCR ...


Clotting of Mammalian Fibrinogens by Papain: A Re-examination

15.10.2014 | Russell F. Doolittle, Biochemistry, 2014

Papain has long been known to cause the gelation of mammalian fibrinogens. It has also been reported that papain-fibrin is insoluble in dispersing solvents like strong urea or sodium bromide solutions, similar to what is observed with thrombin-generated clots in the presence of factor XIIIa and ...


Binding Hotspots of BAZ2B Bromodomain: Histone Interaction Revealed by Solution NMR Driven Docking

15.10.2014 | Fleur M. Ferguson; David M. Dias; João P. G. L. M. Rodrigues; Hans Wienk; Rolf Boelens; Alexandre M. J. J. Bonvin; C ..., Biochemistry, 2014

Bromodomains are epigenetic reader domains, which have come under increasing scrutiny both from academic and pharmaceutical research groups. Effective targeting of the BAZ2B bromodomain by small molecule inhibitors has been recently reported, but no structural information is yet available on the ...


Covalent Small Molecule Inhibitors of Ca2+-Bound S100B

14.10.2014 | Michael C. Cavalier; Adam D. Pierce; Paul T. Wilder; Milad J. Alasady; Kira G. Hartman; David B. Neau; Timothy L. Fo ..., Biochemistry, 2014

Elevated levels of the tumor marker S100B are observed in malignant melanoma, and this EF-hand-containing protein was shown to directly bind wild-type (wt) p53 in a Ca2+-dependent manner, dissociate the p53 tetramer, and inhibit its tumor suppression functions. Likewise, inhibiting S100B with ...


Flexible Docking-Based Molecular Dynamics/Steered Molecular Dynamics Calculations of Protein–Protein Contacts in a Complex of Cytochrome P450 1A2 with Cytochrome b5

14.10.2014 | Petr Jeřábek; Jan Florián; Marie Stiborová; Václav Martínek, Biochemistry, 2014

Formation of transient complexes of cytochrome P450 (P450) with another protein of the endoplasmic reticulum membrane, cytochrome b5 (cyt b5), dictates the catalytic activities of several P450s. Therefore, we examined formation and binding modes of the complex of human P450 1A2 with cyt b5. ...


Phenylalanine Binding Is Linked to Dimerization of the Regulatory Domain of Phenylalanine Hydroxylase

13.10.2014 | Shengnan Zhang; Kenneth M. Roberts; Paul F. Fitzpatrick, Biochemistry, 2014

Biochemistry DOI: 10.1021/bi501109s


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