Search Results - "Joy, Stephen T."

Allostery in the dynamic coactivator domain KIX occurs through minor conformational micro-states by Peiffer, Amanda L, Garlick, Julie M, Joy, Stephen T, Mapp, Anna K, Brooks, 3rd, Charles L

“…The coactivator KIX of CBP uses two binding surfaces to recognize multiple activators and exhibits allostery in ternary complex formation…”
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A Dual-Site Inhibitor of CBP/p300 KIX is a Selective and Effective Modulator of Myb by Joy, Stephen T., Henley, Madeleine J., De Salle, Samantha N., Beyersdorf, Matthew S., Vock, Isaac W., Huldin, Allison J. L., Mapp, Anna K.

“…The protein–protein interaction between the KIX motif of the transcriptional coactivator CBP/p300 and the transcriptional activator Myb is a high-value target…”
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Covalent Targeting of Ras G12C by Rationally Designed Peptidomimetics by Yoo, Daniel Y, Hauser, Andrew D, Joy, Stephen T, Bar-Sagi, Dafna, Arora, Paramjit S

“…Protein-protein interactions (PPIs) play a critical role in fundamental biological processes. Competitive inhibition of these interfaces requires compounds…”
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Inhibition of CREB Binding and Function with a Dual-Targeting Ligand by Liu, Yejun, Joy, Stephen T., Henley, Madeleine J., Croskey, Ayza, Yates, Joel A., Merajver, Sofia D., Mapp, Anna K.

“…CBP/p300 is a master transcriptional coactivator that regulates gene activation by interacting with multiple transcriptional activators. Dysregulation of…”
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The melanocortin-3 receptor is a pharmacological target for the regulation of anorexia by Sweeney, Patrick, Bedenbaugh, Michelle N, Maldonado, Jose, Pan, Pauline, Fowler, Katelyn, Williams, Savannah Y, Gimenez, Luis E, Ghamari-Langroudi, Masoud, Downing, Griffin, Gui, Yijun, Hadley, Colleen K, Joy, Stephen T, Mapp, Anna K, Simerly, Richard B, Cone, Roger D

“…Ablation of hypothalamic AgRP (Agouti-related protein) neurons is known to lead to fatal anorexia, whereas their activation stimulates voracious feeding and…”
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C-H radiocyanation of bioactive molecules via sequential iodination/copper-mediated cross-coupling by Horikawa, Mami, Joy, Stephen T, Sharninghausen, Liam S, Shao, Xia, Mapp, Anna K, Scott, Peter J H, Sanford, Melanie S

“…This report describes a net C-H radiocyanation reaction for the transformation of electron rich (hetero)aromatic substrates into CN-labeled products…”
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Copper-Mediated Radiocyanation of Unprotected Amino Acids and Peptides by Sharninghausen, Liam S, Preshlock, Sean, Joy, Stephen T, Horikawa, Mami, Shao, Xia, Winton, Wade P, Stauff, Jenelle, Kaur, Tanpreet, Koeppe, Robert A, Mapp, Anna K, Scott, Peter J. H, Sanford, Melanie S

“…This report describes a copper-mediated radiocyanation of aryl halides that is applicable to complex molecules. This transformation tolerates an exceptionally…”
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An optimal hydrogen-bond surrogate for α-helices by Joy, Stephen T, Arora, Paramjit S

“…Substitution of a main chain i → i + 4 hydrogen bond with a covalent bond can nucleate and stabilize the α-helical conformation in peptides. Herein we describe…”
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Nucleation Effects in Peptide Foldamers by Patgiri, Anupam, Joy, Stephen T, Arora, Paramjit S

“…Oligomers composed of β3-amino acid residues and a mixture of α- and β3-residues have emerged as proteolytically stable structural mimics of α-helices. An…”
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Subthreshold activation of the melanocortin system causes generalized sensitization to anorectic agents in mice by Dahir, Naima S, Gui, Yijun, Wu, Yanan, Sweeney, Patrick R, Rouault, Alix Aj, Williams, Savannah Y, Gimenez, Luis E, Sawyer, Tomi K, Joy, Stephen T, Mapp, Anna K, Cone, Roger D

“…The melanocortin-3 receptor (MC3R) regulates GABA release from agouti-related protein (AgRP) nerve terminals and thus tonically suppresses multiple circuits…”
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Garcinolic Acid Distinguishes Between GACKIX Domains and Modulates Interaction Networks by Breen, Meghan E, Joy, Stephen T, Baruti, Omari J, Beyersdorf, Matthew S, Henley, Madeleine J, De Salle, Samantha N, Ycas, Peter D, Croskey, Ayza, Cierpicki, Tomasz, Pomerantz, William C K, Mapp, Anna K

“…Natural products are often uniquely suited to modulate protein-protein interactions (PPIs) due to their architectural and functional group complexity relative…”
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Dynamic Phenylalanine Clamp Interactions Define Single-Channel Polypeptide Translocation through the Anthrax Toxin Protective Antigen Channel by Ghosal, Koyel, Colby, Jennifer M., Das, Debasis, Joy, Stephen T., Arora, Paramjit S., Krantz, Bryan A.

“…Anthrax toxin is an intracellularly acting toxin where sufficient detail is known about the structure of its channel, allowing for molecular investigations of…”
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Profiling small molecule inhibitors against helix-receptor interactions: the Bcl-2 family inhibitor BH3I-1 potently inhibits p53/hDM2 by Porter, Jason R, Helmers, Mark R, Wang, Ping, Furman, Jennifer L, Joy, Stephen T, Arora, Paramjit S, Ghosh, Indraneel

“…We validate a practical methodology for the rapid profiling of small molecule inhibitors of protein-protein interactions. We find that a well known BH3 family…”
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An Orthosteric Inhibitor of the RAS–SOS Interaction by Nickerson, Seth, Joy, Stephen T., Arora, Paramjit S., Bar-Sagi, Dafna

“…Rat sarcoma (RAS) proteins are signaling nodes that transduce extracellular cues into precise alterations in cellular physiology by engaging effector pathways…”
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C-H radiocyanation of bioactive molecules sequential iodination/copper-mediated cross-coupling by Horikawa, Mami, Joy, Stephen T, Sharninghausen, Liam S, Shao, Xia, Mapp, Anna K, Scott, Peter J. H, Sanford, Melanie S

“…This report describes a net C-H radiocyanation reaction for the transformation of electron rich (hetero)aromatic substrates into 11 CN-labeled products…”
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Abstract B46: Stabilized helices targeting the RAS-SOS interaction as inhibitors of RAS-dependent cancer cell growth by Nickerson, Seth, Joy, Stephen T., Arora, Paramjit S., Bar-Sagi, Dafna

“…Accumulating evidence supports an essential role for wild-type RAS isoforms in oncogenic RAS-driven tumorigenesis. Recently, we demonstrated that allosteric…”
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