Search Results - "SPASSOV, Danislav S"
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Binding Affinity Determination in Drug Design: Insights from Lock and Key, Induced Fit, Conformational Selection, and Inhibitor Trapping Models
Published in International journal of molecular sciences (28-06-2024)“…Binding affinity is a fundamental parameter in drug design, describing the strength of the interaction between a molecule and its target protein. Accurately…”
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Inhibitor Trapping in Kinases
Published in International journal of molecular sciences (01-03-2024)“…Recently, we identified a novel mechanism of enzyme inhibition in N-myristoyltransferases (NMTs), which we have named 'inhibitor trapping'. Inhibitor trapping…”
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Inhibitor Trapping in N-Myristoyltransferases as a Mechanism for Drug Potency
Published in International journal of molecular sciences (18-07-2023)“…Predicting inhibitor potency is critical in drug design and development, yet it has remained one of computational biology's biggest unresolved challenges…”
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Novel Hits for N-Myristoyltransferase Inhibition Discovered by Docking-Based Screening
Published in Molecules (Basel, Switzerland) (26-08-2022)“…N-myristoyltransferase (NMT) inhibitors that were initially developed for treatment of parasitic protozoan infections, including sleeping sickness, malaria,…”
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A role of salt bridges in mediating drug potency: A lesson from the N-myristoyltransferase inhibitors
Published in Frontiers in molecular biosciences (10-01-2023)“…The salt bridge is the strongest non-covalent interaction in nature and is known to participate in protein folding, protein-protein interactions, and molecular…”
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A Dimerization Function in the Intrinsically Disordered N-Terminal Region of Src
Published in Cell reports (Cambridge) (09-10-2018)“…The mode of regulation of Src kinases has been elucidated by crystallographic studies identifying conserved structured protein modules involved in an orderly…”
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Trask Loss Enhances Tumorigenic Growth by Liberating Integrin Signaling and Growth Factor Receptor Cross-Talk in Unanchored Cells
Published in Cancer research (Chicago, Ill.) (01-02-2013)“…The cell surface glycoprotein Trask/CDCP1 is phosphorylated during anchorage loss in epithelial cells in which it inhibits integrin clustering, outside-in…”
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Phosphorylation of Trask by Src Kinases Inhibits Integrin Clustering and Functions in Exclusion with Focal Adhesion Signaling
Published in Molecular and Cellular Biology (01-02-2011)“…Article Usage Stats Services MCB Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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Phosphorylation of the src Epithelial Substrate Trask Is Tightly Regulated in Normal Epithelia but Widespread in Many Human Epithelial Cancers
Published in Clinical cancer research (01-04-2009)“…Purpose: The frequently elevated activities of the c-src and c-yes products in human epithelial tumors suggest that these activated tyrosine kinases have…”
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The structural features of Trask that mediate its anti-adhesive functions
Published in PloS one (29-04-2011)“…Trask/CDCP1 is a transmembrane protein with a large extracellular and small intracellular domains. The intracellular domain (ICD) undergoes tyrosine…”
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Trask phosphorylation defines the reverse mode of a phosphotyrosine signaling switch that underlies cell anchorage state
Published in Cell cycle (Georgetown, Tex.) (15-04-2011)“…Phosphotyrosine signaling in anchored epithelial cells constitutes a spacially ordained signaling program that largely functions to promote integrin-linked…”
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Cloning and comparative sequence analysis of PUM1 and PUM2 genes, human members of the Pumilio family of RNA-binding proteins
Published in Gene (16-10-2002)“…Drosophila gene Pumilio (Pum) is a founder member of an evolutionarily conserved family of RNA-binding proteins that are present from yeast to mammals, and act…”
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CD318 is a ligand for CD6
Published in Proceedings of the National Academy of Sciences - PNAS (15-08-2017)“…It has been proposed that CD6, an important regulator of T cells, functions by interacting with its currently identified ligand, CD166, but studies performed…”
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Murine hematopoietic stem cells and multipotent progenitors express truncated intracellular form of c-kit receptor
Published in Stem cells and development (01-04-2008)“…The c-kit receptor plays a vital role in self-renewal and differentiation of hematopoietic stem cells (HSCs) and multipotent progenitors (MPPs). We have…”
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Proteomic Analysis of Src Family Kinase Phosphorylation States in Cancer Cells Suggests Deregulation of the Unique Domain
Published in Molecular cancer research (01-06-2021)“…The Src family kinases (SFK) are homologs of retroviral oncogenes, earning them the label of proto-oncogenes. Their functions are influenced by positive and…”
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Regulation of inside-out β1-integrin activation by CDCP1
Published in Oncogene (01-05-2018)“…Tumor metastasis depends on the dynamic regulation of cell adhesion through β1-integrin. The Cub-Domain Containing Protein-1, CDCP1, is a transmembrane…”
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A reversible SRC-relayed COX2 inflammatory program drives resistance to BRAF and EGFR inhibition in BRAFV600E colorectal tumors
Published in Nature cancer (01-02-2023)“…Abstract BRAF V600E mutation confers a poor prognosis in metastatic colorectal cancer (CRC) despite combinatorial targeted therapies based on the latest…”
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The PUF Family of RNA‐binding Proteins: Does Evolutionarily Conserved Structure Equal Conserved Function?
Published in IUBMB life (01-07-2003)“…Drosophila Pumilio ( Pum ) protein is a founder member of a novel family of RNA‐binding proteins, known as the PUF family. The PUF proteins constitute an…”
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The Transmembrane src Substrate Trask Is an Epithelial Protein that Signals during Anchorage Deprivation
Published in The American journal of pathology (01-05-2009)“…The roles of epithelial cells encompass both cellular- and tissue-level functions that involve numerous cell–cell and cell–matrix interactions, which…”
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Mouse Pum1 and Pum2 genes, members of the Pumilio family of RNA-binding proteins, show differential expression in fetal and adult hematopoietic stem cells and progenitors
Published in Blood cells, molecules, & diseases (2003)“…Self-renewal is the common functional property of all types of stem cells and is thought to be regulated by unknown conserved intrinsic and extrinsic molecular…”
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