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Thiruvananthapuram, India

Kumar A.B.,Kerala University | Sanders K.L.,University of Adelaide | George S.,Chemical Biology Group | Murphy J.C.,Field Museum of Natural History
Systematics and Biodiversity | Year: 2012

The Kerala mud snake, Enhydris dussumierii Duméril, Bibron & Duméril, has long been known only from syntypes collected in the nineteenth century, but more recent specimens have provided the opportunity for molecular work. Using Bayesian phylogenetic analysis of 2200 base pairs of cytb, 16S, and c-mos, we recovered the Kerala mud snake as the sister species to the Chinese mud snake, Enhydris chinensis (Chinese-Vietnamese endemic). The DNA results establish the position of dussumierii and chinensis as separate from the Enhydris clade, and together they form the sister group to most of the other fanged homalopsids ((Bitia+Cantoria) + (Erpeton+Gerarda+Fordonia) + (Myron+Pseudoferania) + (Enhydris punctata) + (Homalopsis+Enhydris bocourti) + (Cerberus)). Here we resurrect Ferania Gray for Enhydris sieboldii Gray, establish a new genus for the E. chinensis clade (bennettii+chinensis), and apply the generic replacement name Dieurostus Berg to E. dussumierii Duméril, Bibron & Duméril. A biogeographic scenario is proposed based on the ecology, distribution and salt tolerance of the species composing a hypothesized (not supported with molecular evidence) Asian coastal lineage that is distributed from Pakistan's Indus River delta to temperate coastal China. © 2012 The Natural History Museum. Source

Liu Q.,Dana-Farber Cancer Institute | Liu Q.,Harvard University | Sabnis Y.,Computational Chemistry | Sabnis Y.,UCB Pharma | And 7 more authors.
Chemistry and Biology | Year: 2013

Protein kinases are a large family of approximately 530 highly conserved enzymes that transfer a γ-phosphate group from ATP to a variety of amino acid residues, such as tyrosine, serine, and threonine, that serves as a ubiquitous mechanism for cellular signal transduction. The clinical success of a number of kinase-directed drugs and the frequent observation of disease causing mutations in protein kinases suggest that a large number of kinases may represent therapeutically relevant targets. To date, the majority of clinical and preclinical kinase inhibitors are ATP competitive, noncovalent inhibitors that achieve selectivity through recognition of unique features of particular protein kinases. Recently, there has been renewed interest in the development of irreversible inhibitors that form covalent bonds with cysteine or other nucleophilic residues in the ATP-binding pocket. Irreversible kinase inhibitors have a number of potential advantages including prolonged pharmacodynamics, suitability for rational design, high potency, and ability to validate pharmacological specificity through mutation of the reactive cysteine residue. Here, we review recent efforts to develop cysteine-targeted irreversible protein kinase inhibitors and discuss their modes of recognizing the ATP-binding pocket and their biological activity profiles. In addition, we provided an informatics assessment of the potential "kinase cysteinome" and discuss strategies for the efficient development of new covalent inhibitors. © 2013 Elsevier Ltd. Source

Rana P.,Pfizer | Naven R.,Pfizer | Narayanan A.,Chemical Biology Group | Will Y.,Pfizer | Jones L.H.,Chemical Biology Group
MedChemComm | Year: 2013

Focussed screening of known redox cyclers, and structurally related compounds, was performed using a horseradish peroxidase-phenol red (hydrogen peroxide) assay. A cell viability assay was then used to further understand structure-based toxicity. Pyrimidotriazinediones were confirmed as structural alerts and new redox cycling motifs were identified. © 2013 The Royal Society of Chemistry. Source

Beal D.M.,Chemical Biology Group | Beal D.M.,University of Kent | Albrow V.E.,Chemical Biology Group | Burslem G.,Chemical Biology Group | And 7 more authors.
Organic and Biomolecular Chemistry | Year: 2012

A heterotrifunctional template was developed that utilizes thiol-maleimide and click chemistries (both copper-free and copper-mediated) to effect sequential biomolecule conjugations in a one-pot process. The breadth of compatible substrates was illustrated through highly efficient conjugations of protein, peptide, sugar, lipid, fluoroalkane, biotin and fluorophore molecules. This template should be useful for the creation of chemically-enhanced/enabled biotherapeutics, especially through the expression of discontinuous (and heterogeneous) epitopes. Source

Reshmy V.,Chemical Biology Group | Kumar K.S.,Chemical Biology Group | George S.,Chemical Biology Group
Research Journal of Biotechnology | Year: 2011

Esculentins constitute the most potent antimicrobial peptides from frog skin. The present study describes the successful isolation of 3 novel esculentin -2 peptides from the skin secretion of Indian bronzed frog Hylarana temporalis. The deduced open reading frames encoding the biosynthetic precursors of each esculentin consisted of 76 amino acid residues. Precursors of these novel peptides, named esculentin-2TEa, esculentin-2TEb and esculentin-2TEc, from H.temporalis showed 12 amino acid differences than the nearest homologous peptide reported so far. This forms the first report of escuelentin peptides from Hylarana temporalis, endemic to India and Srilanka. Source

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