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Five Members of a Novel Ca2+-binding Protein (CABP) Subfamily with Similarity to Calmodulin*
TLDR
Five members of a novel Ca2+-binding protein subfamily (CaBP), with 46–58% sequence similarity to calmodulin (CaM), were identified in the vertebrate retina, suggesting that these novel CaBPs are an important component of Ca2-mediated cellular signal transduction in the central nervous system where they may augment or substitute for CaM.
Missense mutations in the regulatory domain of PKC gamma: a new mechanism for dominant nonepisodic cerebellar ataxia.
TLDR
A nonepisodic autosomal dominant spinocerebellar ataxia not caused by a nucleotide repeat expansion is reported that is, to the authors' knowledge, the first such SCA and suggests that there may be a common pathway for PKC gamma-related and polyglutamine-related neurodegeneration.
Alternatively spliced isoforms of the human constitutive androstane receptor.
TLDR
Assays to assess function indicate that the variant proteins, when compared with the reference protein isoform, exhibit compromised activities with respect to DNA binding, transcriptional activation and coactivator recruitment.
Toxoplasma gondii calcium-dependent protein kinase 1 is a target for selective kinase inhibitors
TLDR
It is shown that TgCDPK1 is inhibited by low nanomolar levels of bumped kinase inhibitors (BKIs), compounds inactive against mammalian kinases, and T. gondii expressing a glycine to methionine gatekeeper mutant enzyme show significantly decreased sensitivity to BKIs.
Genomic-scale prioritization of drug targets: the TDR Targets database
TLDR
The development of the TDR Targets database is discussed, which encompasses extensive genetic, biochemical and pharmacological data related to tropical disease pathogens, as well as computationally predicted druggability for potential targets and compound desirability information, and aims to facilitate the identification and prioritization of candidate drug targets for pathogens.
Glycolysis as a target for the design of new anti-trypanosome drugs.
TLDR
Structural- and catalytic mechanism-based approaches are applied to design compounds that inhibit the glycolytic enzymes of the parasites without affecting the corresponding proteins of the human host.
Reengineering CCA-adding enzymes to function as (U,G)- or dCdCdA-adding enzymes or poly(C,A) and poly(U,G) polymerases
TLDR
The specificity of both class I and II enzymes may be dictated by an intricate network of hydrogen bonds involving the protein, incoming nucleotide, and 3′ end of the tRNA, suggests that the evolutionary diversity of the nucleotidyltransferase family may be explained.
Rod and cone visual cycle consequences of a null mutation in the 11-cis-retinol dehydrogenase gene in man
TLDR
In vivo visual consequences of this null mutation showed complex kinetics of dark adaptation of rod and cone resensitization and the causative novel RDH5 mutation, Arg157Trp, that replaces an amino acid residue conserved among short-chain alcohol dehydrogenases.
Crystal structure of glycosomal glyceraldehyde-3-phosphate dehydrogenase from Leishmania mexicana: implications for structure-based drug design and a new position for the inorganic phosphate binding
TLDR
The structure of glycosomal glyceraldehyde-3-phosphate dehydrogenase (GAPDH) from the trypanosomatid parasite Leishmania mexicana has been determined by X-ray crystallography and will be used as a basis for structure-based drug design targeted against trypano-based GAPDHs.
Structure-based exploration of the ganglioside GM1 binding sites of Escherichia coli heat-labile enterotoxin and cholera toxin for the discovery of receptor antagonists.
TLDR
Careful analysis of binding data and comparison with crystal structures led to the derivation of correlations between the structure and affinity of the galactose derivatives, which will be used in the design of a second round of LT and CT receptor antagonists.
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