Protein Targeting Compounds

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Protein Targeting Compounds

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Author : Thomas Böldicke
language : en
Publisher: Springer
Release Date : 2016-05-28

Protein Targeting Compounds written by Thomas Böldicke and has been published by Springer this book supported file pdf, txt, epub, kindle and other format this book has been release on 2016-05-28 with Medical categories.

This book presents an overview of the most relevant protein knockdown techniques. Readers will find a description of the generation and use of recombinant human antibodies, ER intrabodies and peptides as well as a description of the working mechanism and potential of the inhibitory action of each of these molecules. The book will also describe the selection and activity of a number of phosphatases, aptamers and allosteric modulators, focusing on A G protein coupled receptors. The book starts with a chapter on the in silico prediction of target-inhibitor interactions. Key aspects of this book are: - Selection strategies for monoclonal and recombinant human antibodies - Selection strategies for ER intrabodies, peptides and aptamers - Examples of the most efficient inhibitors and their applications in protein biochemistry and cell biology - Antibodies for cancer therapy and inhibitors of angiogenesis. The book will be of great interest to scientists and students working in the life sciences on all areas related to protein biology. The variety of methods to modulate the activities of specific proteins which are introduced here will be of great benefit to the reader who is interested in general protein research or to readers who have very specific protein related questions.

Protein Targeting With Small Molecules

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Author : Hiroyuki Osada
language : en
Publisher: John Wiley & Sons
Release Date : 2009-07-31

Protein Targeting With Small Molecules written by Hiroyuki Osada and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2009-07-31 with Science categories.

Discover the link between the latest chemical biology approaches and novel drug therapies! Protein Targeting with Small Molecules: Chemical Biology Techniques and Applications takes readers beyond the use of chemical biology in basic research, providing a highly relevant look at techniques that can address the challenges of biology and drug design and development. This indispensable bench companion features up-to-date coverage of advances in chemistry and assesses their impact on developing new therapeutics, making it ideal for chemical biologists and medicinal chemists who are developing small molecule drugs to target proteins and treat diseases. In addition, the book examines the full range of complex biological systems and their interrelationship with chemistry, from the interaction of biological response modifiers with proteins to the chemical biology of cell surface oligosaccharides. Distinguished by an overview of chemical biology that is reinforced and clarified by detailed examples and descriptions of techniques, Protein Targeting with Small Molecules: Chemical Biology Techniques and Applications: Introduces key technologies and methods of chemical biology designed to detect the interactions of small molecules and proteins Facilitates the discovery of small molecules that bind to proteins and describes the molecules' application in the investigation of biological processes Presents timely coverage of the development of fluorescent probes for small molecules, as well as the generation of small molecule ligands and inhibitors Reviews important techniques such as chemical genomics, target profiling, immobilization technology, detection methods, chemical inhibition, and structure-based targeting Offers a compelling synopsis of data that underscores the recent progress made in the area of targeting proteins by small molecules

Activity Based Protein Profiling

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Author : Benjamin F. Cravatt
language : en
Publisher: Springer
Release Date : 2019-01-25

Activity Based Protein Profiling written by Benjamin F. Cravatt and has been published by Springer this book supported file pdf, txt, epub, kindle and other format this book has been release on 2019-01-25 with Medical categories.

This volume provides a collection of contemporary perspectives on using activity-based protein profiling (ABPP) for biological discoveries in protein science, microbiology, and immunology. A common theme throughout is the special utility of ABPP to interrogate protein function and small-molecule interactions on a global scale in native biological systems. Each chapter showcases distinct advantages of ABPP applied to diverse protein classes and biological systems. As such, the book offers readers valuable insights into the basic principles of ABPP technology and how to apply this approach to biological questions ranging from the study of post-translational modifications to targeting bacterial effectors in host-pathogen interactions.

Molecular Biology Of The Cell

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Author : Bruce Alberts
language : en
Publisher:
Release Date : 2002

Molecular Biology Of The Cell written by Bruce Alberts and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2002 with Cytology categories.

Design And Synthesis Of Small Molecule Protein Protein Interaction Antagonists

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Author : Xu Han
language : en
Publisher:
Release Date : 2014

Design And Synthesis Of Small Molecule Protein Protein Interaction Antagonists written by Xu Han and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2014 with Calcium channels categories.

Protein-protein interactions play a crucial role in a wide range of biological processes. Research on the design and synthesis of small molecules to modulate these proteinprotein interactions can lead to new targets and drugs to modulate their function. In chapter one, we discuss the design and synthesis of small molecules to probe a proteinprotein interaction in a voltage-gated Ca2+ channel. Virtual screening identified a compound (BTT-3) that contained a 3,4-dihydro-3,4'-pyrazole core. This compound had modest biological activity when tested in a fluorescence polarization (FP) assay. The synthetic route to BTT-3 consisted of six steps. In addition, analogs of BTT-3 were made for a structure-activity study to establish the importance of a carboxylate moiety. We also synthesized a biotinylated benzophenone photo-affinity probe and linked it to BTT-3 to identify additional protein targets of the compound. In Chapter two, small-molecule antagonists targeting uPA-uPAR protein-protein interaction are presented. A total of 500 commercially-available compounds were previously identified by virtual screening and tested by a FP assay. Three classes of compounds were found with biological activity. The first class of compounds contains pyrrolidone core structures represented by IPR- 1110, the second class has a novel pyrrolo[3,4-c]pyrazole ring system, represented by xv IPR-1283 and the last series had compounds with a 1,2-disubstituted 1,2- dihydropyrrolo[3,4-b]indol-3(4H)-one core structure, represented by IPR-540. Each of these three compounds were synthesized and assessed by FP and ELISA assays. A binding mode of IPR-1110 with uPA was subsequently proposed. Based on this binding mode, another 61 IPR-1110 derivatives were synthesized by us to illustrate the SAR activity. Analogs of the other two series were also synthesized.

Targeting Protein Protein Interactions In Transcriptional Complexes As Potential Anti Cancer Therapy

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Author : Melanie Amber Blevins
language : en
Publisher:
Release Date : 2015

Targeting Protein Protein Interactions In Transcriptional Complexes As Potential Anti Cancer Therapy written by Melanie Amber Blevins and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2015 with categories.

It is widely accepted that the aberrant expression of developmental transcription factors in adult tissues can result in the misexpression of target genes and reactivation of developmental programs, thereby contributing to tumorigenesis and/or tumor progression. I propose that the disruption of the transcriptional activity of developmental transcriptional factors overexpressed in cancer can be an attractive mechanism for potential anti-cancer treatment. The approach through which I hope to disrupt transcription is through the inhibition of the protein-protein interactions between target transcriptional factors and their cofactors. To that end, I have chosen two separate transcriptional complexes each known to be misexpressed and play a causal role in cancer phenotypes: SIX1 and CtBP1. SIX1, a homeobox gene normally expressed during embryogenesis, requires the EYA family of co-activator proteins to activate transcription. CtBP1 is a co-repressor that binds to a conserved peptide motif found in multiple transcription factors (as well as the adenovirus E1A protein) to elicit its effect. Since single amino acid mutations have been shown to significantly disrupt each protein-protein interaction, I hypothesize that only a few residues play an important role in these interactions and that these residue interactions can be disrupted by small molecules leading to decreased protein-protein interactions. To identify small molecule inhibitors that target these complexes, I have developed an AlphaScreen assay to monitor the interaction between SIX1 and EYA2 or CtBP1 and E1A. In collaboration with the National Institute of Health Chemical Genomics Center (NCGC) using a high throughput screen, I have identified compounds that specifically inhibit either the CtBP-E1A or SIX1-EYA2 interactions. These compounds have been validated using secondary, specificity, and cell culture experiments. I plan to further determine the mechanism of action of these compounds through additional biophysical and structural techniques, such as crystallography and isothermal calorimetry. Concurrently, the NCGC is synthesizing a large number of analogues around the lead compounds to improve their potency and solubility, which may facilitate future efforts to characterize their mechanism of action and optimize the compounds. In addition, I am also developing a peptide-based inhibitor of CtBP and its transcription factor partners to inhibit CtBP-mediated tumorigenic and metastatic properties.

Computational Tools For The High Throughput Identification Of Protein Targeted Drugs And Probes

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Author : Rhiannon Lily Kamstra
language : en
Publisher:
Release Date : 2014

Computational Tools For The High Throughput Identification Of Protein Targeted Drugs And Probes written by Rhiannon Lily Kamstra and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2014 with Cancer categories.

"This thesis is comprised of three projects that are driven by a common theme, which is the use of computational tools in aiding molecular probe and drug design. In the first project, the feasibility of using molecular docking and scoring to estimate binding affinity for small molecules labelled covalently with fluorophores was tested using several proof-of-concept experiments. The high-throughput nature of computational screening applications such as Hierarchical Virtual Ligand Screening (HierVLS) necessitate that, in order to screen these labelled compounds, there must be an automated way to generate the associated structures virtually from large databases of base compounds and fluorophores. A script was developed in MOE software using scientific vector language (SVL) that could identify key reactive functional groups in both reactive fluorophores and target base compounds, and create the appropriate labelled structures for screening. The final fluorescence-labelled database numbers 14,862 compounds, each tagged with the ATTO680 fluorophore. In a subsequent project, the fluorescence-tagged library was screened against carbonic anhydrase 9 (CAIX), a protein implicated as a biomarker in several cancer types. This screening was accompanied by the screening of a validation set of known CAIX ligands and appropriately chosen decoys.

Trp Ion Channel Function In Sensory Transduction And Cellular Signaling Cascades

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Author : Wolfgang B. Liedtke, MD, PH.D.
language : en
Publisher: CRC Press
Release Date : 2006-09-29

Trp Ion Channel Function In Sensory Transduction And Cellular Signaling Cascades written by Wolfgang B. Liedtke, MD, PH.D. and has been published by CRC Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2006-09-29 with Medical categories.

Since the first TRP ion channel was discovered in Drosophila melanogaster in 1989, the progress made in this area of signaling research has yielded findings that offer the potential to dramatically impact human health and wellness. Involved in gateway activity for all five of our senses, TRP channels have been shown to respond to a wide range of st

Std Interchange

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Author :
language : en
Publisher:
Release Date : 1984

Std Interchange written by and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 1984 with Health education categories.

Biochemical Targets Of Plant Bioactive Compounds

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Author : Gideon Polya
language : en
Publisher: CRC Press
Release Date : 2003-05-15

Biochemical Targets Of Plant Bioactive Compounds written by Gideon Polya and has been published by CRC Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2003-05-15 with Science categories.

When introduced to the human body, bioactive metabolites produced by plants for self defense bind to particular biochemical targets, most notably to proteins involved in signaling by hormones and neurotransmitters. This, essentially, is the basis for the effects of herbal medicine. While herbal medicine preparations may act by complex synergistic interactions, molecular explanations of herbal medicine efficacy and side effects ultimately require definition of the biochemical targets of individual plant bioactive constituents. Biochemical Targets of Plant Bioactive Compounds is a comprehensive and user-friendly reference guide to biochemical targets of plant defensive compounds. With 500 pages of tables, it presents a mine of succinctly summarized information relating to bioactive compound structures, plant sources, biochemical targets and physiological effects that can be readily accessed via chemical compound, plant genus, plant common name and subject indexes. With introductory chapters providing reviews of the structural diversity of plant defensive compounds and biochemistry, this book is an invaluable reference for biomedical professionals in the fields of alternative/complementary medicine, natural product chemistry, toxicology, pharmacology, and botany.