Keywords: Conformation (9)

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Advanced Organic Chemistry, Spring 2007
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Advanced Organic Chemistry, Spring 2007

Application of structure and theory to the study of organic reaction mechanisms: ... (more)

Application of structure and theory to the study of organic reaction mechanisms: stereochemical features including conformation and stereoelectronic effects; reaction dynamics, isotope effects and molecular orbital theory applied to pericyclic and photochemical reactions; and special reactive intermediates including carbenes, carbanions, and free radicals. (less)

Subject:
Science and Technology
Material Type:
Assessments
Full Course
Homework and Assignments
Lecture Notes
Syllabi
Provider:
M.I.T.
Provider Set:
MIT OpenCourseWare
Author:
Movassaghi, Mohammad
Arrestin Times for Developing Antipsychotics and {beta}-Blockers
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Arrestin Times for Developing Antipsychotics and {beta}-Blockers

Heterotrimeric guanine nucleotide–binding protein (G protein)–coupled receptors (GPCRs) are the largest group ... (more)

Heterotrimeric guanine nucleotide–binding protein (G protein)–coupled receptors (GPCRs) are the largest group of structurally related proteins encoded by the human genome. As signal effectors and allosteric regulators, GPCRs dynamically recruit not only specific heterotrimeric G proteins but also the cytosolic scaffold proteins, β-arrestin 1 and 2, which were originally thought only to serve as negative regulators of GPCR signaling. Although about half of currently available therapeutics target GPCR function, usually at the ligand-binding, orthosteric site, evidence suggests that β-arrestins may be therapeutic targets themselves. Indeed, a hitherto undiscovered action of various antipsychotics is to inhibit the ability of the dopamine D2 receptor to engage β-arrestin 2 and activate glycogen synthase kinase 3, which may be a target for developing therapeutics for schizophrenia. Also, certain β-antagonists (blockers) used to treat heart failure, such as carvedilol, have the added effect of promoting activation of extracellular signal-regulated kinase through β-arrestin. It seems likely that the structure of β-arrestins allows them to detect different types and conformational states of GPCRs and to respond in functionally distinct fashions by using separate cohorts of signaling proteins, thus generating additional possibilities for therapeutic intervention. (less)

Subject:
Life Science
Material Type:
Activities and Labs
Images and Illustrations
Instructional Material
Reference
Provider:
BiosciEdNet (BEN): Digital Library Portal for Teaching and Learning in the Biological Sciences
Provider Set:
BiosciEdNet (BEN): Digital Library Portal for Teaching and Learning in the Biological Sciences
Author:
Miles D. Houslay (University of Glasgow;Faculty of Biomedical and Life Sciences REV)
Assignment 1: Visualization and Ranking of Protein Conformations
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Assignment 1: Visualization and Ranking of Protein Conformations

This assigment introduces students to the visualization software VMD and allows them ... (more)

This assigment introduces students to the visualization software VMD and allows them to get familiar with protein structures. Students are required to visualize protein conformations and understand the differences between structures based on their geometry. Students will rank the provided conformations based on their geometric differences. (less)

Subject:
Science and Technology
Material Type:
Readings
Syllabi
Provider:
Rice University
Provider Set:
Connexions
Author:
Lydia E. Kavraki
Conformational Display: A Role for Switch Polymorphism in the Superfamily of Regulatory GTPases
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Conformational Display: A Role for Switch Polymorphism in the Superfamily of Regulatory GTPases

Regulating signal transduction is serious business. If signals are improperly controlled, aberrant ... (more)

Regulating signal transduction is serious business. If signals are improperly controlled, aberrant proliferation or inappropriate cell death may result. The Ras superfamily of small guanosine triphosphatases (GTPases) and the heterotrimeric G proteins require GTP binding into their active sites for subsequent activation. Hydrolysis of GTP to GDP precedes, and is a requirement for, inactivation. However, the changes in conformation that accompany GTP or GDP binding are now becoming fully appreciated. Sprang discusses the importance of conformation in the activation of GTPases and heterotrimeric G proteins, and the possibility that these proteins exist in several different conformations. Thus, rather than a simplistic on/off two-conformation model, these signaling proteins exist in several differing conformations that may be related to activation and effector protein binding. (less)

Subject:
Life Science
Material Type:
Activities and Labs
Images and Illustrations
Instructional Material
Reference
Provider:
BiosciEdNet (BEN): Digital Library Portal for Teaching and Learning in the Biological Sciences
Provider Set:
BiosciEdNet (BEN): Digital Library Portal for Teaching and Learning in the Biological Sciences
Author:
Stephen R. Sprang (Dallas;Howard Hughes Medical Institute and University of Texas Southwestern Medical Center REV)
Focus Issue: Series on Structural Biology
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Focus Issue: Series on Structural Biology

During the month of May, Science Signaling will publish research and commentary ... (more)

During the month of May, Science Signaling will publish research and commentary that use or describe the application of structural approaches to reveal the mechanisms underlying signaling molecules and events, to uncover how signaling molecules perform their biological functions or contribute to disease, and to highlight potentially fruitful avenues for drug design. (less)

Subject:
Life Science
Physics
Material Type:
Reference
Provider:
BiosciEdNet (BEN): Digital Library Portal for Teaching and Learning in the Biological Sciences
Provider Set:
BiosciEdNet (BEN): Digital Library Portal for Teaching and Learning in the Biological Sciences
Author:
Wei Wong (American Association for the Advancement of Science;Associate Editor of Science Signaling REV)
Focus Issue: The Protein Dynamics of Cell Signaling
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Focus Issue: The Protein Dynamics of Cell Signaling

Science Signaling complements the Science special issue on protein dynamics (http://www.sciencemag.org/sciext/proteindynamics/) with ... (more)

Science Signaling complements the Science special issue on protein dynamics (http://www.sciencemag.org/sciext/proteindynamics/) with several articles that highlight the dynamic nature of proteins involved in signal transduction. Not only are conformational changes in proteins important for transducing signaling information, proteins also move within the cell and interact with various partners to trigger the appropriate cellular response. Examples of each of these types of protein dynamics are highlighted in this issue. (less)

Subject:
Life Science
Material Type:
Reference
Provider:
BiosciEdNet (BEN): Digital Library Portal for Teaching and Learning in the Biological Sciences
Provider Set:
BiosciEdNet (BEN): Digital Library Portal for Teaching and Learning in the Biological Sciences
Author:
Nancy R. Gough (American Association for the Advancement of Science;Editor of Science Signaling REV)
Wei Wong (American Association for the Advancement of Science;Associate Editor of Science Signaling REV)
Protein Kinase Activation Loop Autophosphorylation in Cis: Overcoming a Catch-22 Situation
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Protein Kinase Activation Loop Autophosphorylation in Cis: Overcoming a Catch-22 Situation

Autophosphorylation of the activation loop in cis is an underappreciated and poorly ... (more)

Autophosphorylation of the activation loop in cis is an underappreciated and poorly understood mode of activation of protein kinases. Here, I describe four examples of protein kinases that are activated in this way, concentrating on their biochemical properties and how their autophosphorylation in cis is achieved. (less)

Subject:
Life Science
Material Type:
Activities and Labs
Data
Images and Illustrations
Instructional Material
Reference
Provider:
BiosciEdNet (BEN): Digital Library Portal for Teaching and Learning in the Biological Sciences
Provider Set:
BiosciEdNet (BEN): Digital Library Portal for Teaching and Learning in the Biological Sciences
Author:
Pamela A. Lochhead (UK;The Babraham Research Institute REV)
STRUCTURAL BIOLOGY: Evolutionary Chemistry: Getting There from Here
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STRUCTURAL BIOLOGY: Evolutionary Chemistry: Getting There from Here

Access to the article is free, however registration and sign-in are required. ... (more)

Access to the article is free, however registration and sign-in are required. What takes place when the antibodies in the immune system evolve to become highly specific for certain antigens? In this issue, Wedemayer et al. have captured the x-ray crystallographic images of antibody molecules before and after they evolve into high-affinity binders for their ligand. In his Perspective, Joyce explains the apparent Lamarckian nature of this process, in which the shape of the mature binding site resembles the one induced in the original germ line antibody by the ligand. (less)

Subject:
Life Science
Material Type:
Activities and Labs
Images and Illustrations
Instructional Material
Reference
Provider:
BiosciEdNet (BEN): Digital Library Portal for Teaching and Learning in the Biological Sciences
Provider Set:
BiosciEdNet (BEN): Digital Library Portal for Teaching and Learning in the Biological Sciences
Author:
Gerald F. Joyce (The Scripps Research Institute;Departments of Chemistry and Molecular Biology)
2002 llaF ,gnivloS melborP gnireenignE dna sretupmoC ot noitcudortnI

2002 llaF ,gnivloS melborP gnireenignE dna sretupmoC ot noitcudortnI

.desu si egaugnal gnimmargorp avaJ ehT .gninnalp dna ,tnemeganam ,ecneics ,gnireenigne ni ... (more)

.desu si egaugnal gnimmargorp avaJ ehT .gninnalp dna ,tnemeganam ,ecneics ,gnireenigne ni smelborp gnivlos rof seuqinhcet gnipoleved no si sisahpmE .scipot decnavda detceles dna scihparg retupmoc ,gnihcraes dna gnitros ,serutcurts atad ,sdohtem laciremun ,secafretni resu lacihparg ,stpecnoc gnimmargorp revoc smelborp gnimmargorp ylkeeW .esruoc eht fo sucof eht si tnempoleved dna ngised erawtfos detneiro-tcejbO .snoitacilppa cifitneics dna gnireenigne rof sdohtem lanoitatupmoc dna tnempoleved erawtfos latnemadnuf stneserp esruoc sihT (less)