Search Results - "Bulfer, Stacie"

2.3 Å resolution cryo-EM structure of human p97 and mechanism of allosteric inhibition by Banerjee, Soojay, Bartesaghi, Alberto, Merk, Alan, Rao, Prashant, Bulfer, Stacie L., Yan, Yongzhao, Green, Neal, Mroczkowski, Barbara, Neitz, R. Jeffrey, Wipf, Peter, Falconieri, Veronica, Deshaies, Raymond J., Milne, Jacqueline L. S., Huryn, Donna, Arkin, Michelle, Subramaniam, Sriram

“…p97 is a hexameric AAA+ adenosine triphosphatase (ATPase) that is an attractive target for cancer drug development. We report cryo–electron microscopy…”
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Altered cofactor regulation with disease-associated p97/VCP mutations by Zhang, Xiaoyi, Gui, Lin, Zhang, Xiaoyan, Bulfer, Stacie L., Sanghez, Valentina, Wong, Daniel E., Lee, YouJin, Lehmann, Lynn, Lee, James Siho, Shih, Pei-Yin, Lin, Henry J., Iacovino, Michelina, Weihl, Conrad C., Arkin, Michelle R., Wang, Yanzhuang, Chou, Tsui-Fen

“…Dominant mutations in p97/VCP (valosin-containing protein) cause a rare multisystem degenerative disease with varied phenotypes that include inclusion body…”
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Specific inhibition of p97/VCP ATPase and kinetic analysis demonstrate interaction between D1 and D2 ATPase domains by Chou, Tsui-Fen, Bulfer, Stacie L, Weihl, Conrad C, Li, Kelin, Lis, Lev G, Walters, Michael A, Schoenen, Frank J, Lin, Henry J, Deshaies, Raymond J, Arkin, Michelle R

“…The p97 AAA (ATPase associated with diverse cellular activities), also called VCP (valosin-containing protein), is an important therapeutic target for cancer…”
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Discovery of vimseltinib (DCC-3014), a highly selective CSF1R switch-control kinase inhibitor, in clinical development for the treatment of Tenosynovial Giant Cell Tumor (TGCT) by Caldwell, Timothy M., Ahn, Yu Mi, Bulfer, Stacie L., Leary, Cynthia B., Hood, Molly M., Lu, Wei-Ping, Vogeti, Lakshminarayana, Vogeti, Subha, Kaufman, Michael D., Wise, Scott C., Le Bourdonnec, Bertrand, Smith, Bryan D., Flynn, Daniel L.

“…[Display omitted] Based on knowledge of kinase switch-control inhibition and using a combination of structure-based drug design and standard medicinal…”
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p97 Disease Mutations Modulate Nucleotide-Induced Conformation to Alter Protein–Protein Interactions by Bulfer, Stacie L, Chou, Tsui-Fen, Arkin, Michelle R

“…The AAA+ ATPase p97/VCP adopts at least three conformations that depend on the binding of ADP and ATP and alter the orientation of the N-terminal…”
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Discovery of acyl ureas as highly selective small molecule CSF1R kinase inhibitors by Caldwell, Timothy M., Kaufman, Michael D., Wise, Scott C., Mi Ahn, Yu, Hood, Molly M., Lu, Wei-Ping, Patt, William C., Samarakoon, Thiwanka, Vogeti, Lakshminarayana, Vogeti, Subha, Yates, Karen M., Bulfer, Stacie L., Le Bourdonnec, Bertrand, Smith, Bryan D., Flynn, Daniel L.

“…[Display omitted] Based on the structure of an early lead identified in Deciphera’s proprietary compound collection of switch control kinase inhibitors and…”
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Crystal structure of Saccharomyces cerevisiae Aro8, a putative α‐aminoadipate aminotransferase by Bulfer, Stacie L., Brunzelle, Joseph S., Trievel, Raymond C.

“…α‐Aminoadipate aminotransferase (AAA‐AT) catalyzes the amination of 2‐oxoadipate to α‐aminoadipate in the fourth step of the α‐aminoadipate pathway of lysine…”
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Structure–Activity Study of Bioisosteric Trifluoromethyl and Pentafluorosulfanyl Indole Inhibitors of the AAA ATPase p97 by Alverez, Celeste, Arkin, Michelle R, Bulfer, Stacie L, Colombo, Raffaele, Kovaliov, Marina, LaPorte, Matthew G, Lim, Chaemin, Liang, Mary, Moore, William J, Neitz, R. Jeffrey, Yan, Yongzhao, Yue, Zhizhou, Huryn, Donna M, Wipf, Peter

“…Exploratory SAR studies of a new phenyl indole chemotype for p97 inhibition revealed C-5 indole substituent effects in the ADPGlo assay that did not fully…”
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A threonine turnstile defines a dynamic amphiphilic binding motif in the AAA ATPase p97 allosteric binding site by Burnett, James C, Lim, Chaemin, Peyser, Brian D, Samankumara, Lalith P, Kovaliov, Marina, Colombo, Raffaele, Bulfer, Stacie L, LaPorte, Matthew G, Hermone, Ann R, McGrath, Connor F, Arkin, Michelle R, Gussio, Rick, Huryn, Donna M, Wipf, Peter

“…The turnstile motion of two neighboring threonines sets up a dynamic side chain interplay that can accommodate both polar and apolar ligands in a small…”
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Optimization of Phenyl Indole Inhibitors of the AAA+ ATPase p97 by LaPorte, Matthew G, Burnett, James C, Colombo, Raffaele, Bulfer, Stacie L, Alverez, Celeste, Chou, Tsui-Fen, Neitz, R. Jeffrey, Green, Neal, Moore, William J, Yue, Zhizhou, Li, Shan, Arkin, Michelle R, Wipf, Peter, Huryn, Donna M

“…Optimization of the side-chain of a phenyl indole scaffold identified from a high-throughput screening campaign for inhibitors of the AAA+ ATPase p97 is…”
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Structural Basis for l-Lysine Feedback Inhibition of Homocitrate Synthase by Bulfer, Stacie L., Scott, Erin M., Pillus, Lorraine, Trievel, Raymond C.

“…The α-aminoadipate pathway of lysine biosynthesis is modulated at the transcriptional and biochemical levels by feedback inhibition. The first enzyme in the…”
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Crystal structure of homoisocitrate dehydrogenase from Schizosaccharomyces pombe by Bulfer, Stacie L., Hendershot, Jenna M., Trievel, Raymond C.

“…Homoisocitrate dehydrogenase (HICDH) catalyzes the conversion of homoisocitrate to 2-oxoadipate, the third enzymatic step in the α-aminoadipate pathway by…”
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Allosteric Indole Amide Inhibitors of p97: Identification of a Novel Probe of the Ubiquitin Pathway by Alverez, Celeste, Bulfer, Stacie L, Chakrasali, Ramappa, Chimenti, Michael. S, Deshaies, Raymond J, Green, Neal, Kelly, Mark, LaPorte, Matthew G, Lewis, Taber S, Liang, Mary, Moore, William J, Neitz, R. Jeffrey, Peshkov, Vsevolod A, Walters, Michael A, Zhang, Feng, Arkin, Michelle R, Wipf, Peter, Huryn, Donna M

“…A high-throughput screen to discover inhibitors of p97 ATPase activity identified an indole amide that bound to an allosteric site of the protein. Medicinal…”
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Crystal Structure and Functional Analysis of Homocitrate Synthase, an Essential Enzyme in Lysine Biosynthesis by Bulfer, Stacie L., Scott, Erin M., Couture, Jean-François, Pillus, Lorraine, Trievel, Raymond C.

“…Homocitrate synthase (HCS) catalyzes the first and committed step in lysine biosynthesis in many fungi and certain Archaea and is a potential target for…”
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Crystal structure of Saccharomyces cerevisiae Aro8, a putative [alpha]-aminoadipate aminotransferase by Bulfer, Stacie L, Brunzelle, Joseph S, Trievel, Raymond C

“…[alpha]-Aminoadipate aminotransferase (AAA-AT) catalyzes the amination of 2-oxoadipate to [alpha]-aminoadipate in the fourth step of the [alpha]-aminoadipate…”
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A Fragment-Based Ligand Screen Against Part of a Large Protein Machine: The ND1 Domains of the AAA+ ATPase p97/VCP by Chimenti, Michael S, Bulfer, Stacie L, Neitz, R Jeffrey, Renslo, Adam R, Jacobson, Matthew P, James, Thomas L, Arkin, Michelle R, Kelly, Mark J S

“…The ubiquitous AAA+ ATPase p97 functions as a dynamic molecular machine driving several cellular processes. It is essential in regulating protein homeostasis,…”
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Application of a high-throughput fluorescent acetyltransferase assay to identify inhibitors of homocitrate synthase by Bulfer, Stacie L., McQuade, Thomas J., Larsen, Martha J., Trievel, Raymond C.

“…Homocitrate synthase (HCS) catalyzes the first step of l-lysine biosynthesis in fungi by condensing acetyl-coenzyme A and 2-oxoglutarate to form 3…”
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Ripretinib (DCC-2618) Is a Switch Control Kinase Inhibitor of a Broad Spectrum of Oncogenic and Drug-Resistant KIT and PDGFRA Variants by Smith, Bryan D., Kaufman, Michael D., Lu, Wei-Ping, Gupta, Anu, Leary, Cynthia B., Wise, Scott C., Rutkoski, Thomas J., Ahn, Yu Mi, Al-Ani, Gada, Bulfer, Stacie L., Caldwell, Timothy M., Chun, Lawrence, Ensinger, Carol L., Hood, Molly M., McKinley, Arin, Patt, William C., Ruiz-Soto, Rodrigo, Su, Ying, Telikepalli, Hanumaiah, Town, Ajia, Turner, Benjamin A., Vogeti, Lakshminarayana, Vogeti, Subha, Yates, Karen, Janku, Filip, Abdul Razak, Albiruni Ryan, Rosen, Oliver, Heinrich, Michael C., Flynn, Daniel L.

“…Ripretinib (DCC-2618) was designed to inhibit the full spectrum of mutant KIT and PDGFRA kinases found in cancers and myeloproliferative neoplasms,…”
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Abstract 3925: Inhibition of oncogenic and drug-resistant PDGFRA and KIT alterations by DCC-2618 by Smith, Bryan D., Kaufman, Michael D., Gupta, Anu, Leary, Cynthia B., Lu, Wei-ping, Bulfer, Stacie L., Al-Ani, Gada, Singh, Jarnail, Vogeti, Subha, Heinrich, Michael C., Flynn, Daniel L.

“…Abstract Introduction: Activating mutations and other genetic alterations in KIT and PDGFRA receptor tyrosine kinases have been identified in certain cancers…”
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Abstract B129: Preclinical studies with DCC-3116, an ULK kinase inhibitor designed to inhibit autophagy as a potential strategy to address mutant RAS cancers by Smith, Bryan D, Vogeti, Lakshminarayana, Gupta, Anu, Singh, Jarnail, Al-Ani, Gada, Bulfer, Stacie L, Caldwell, Timothy M, Timson, Mary J, Vogeti, Subha, Ahn, Yu Mi, Al-Hashimi, Hikmat, Crawley, Chase K, Heiniger, Cale L, Leary, Cynthia B, Proto, Justin T, Shen, Quanrong, Telikepalli, Hanumaiah, Yates, Karen, Lu, Wei-Ping, Flynn, Daniel L

“…Abstract Background: Cancer cells activate autophagy, a catabolic process to resupply nutrients and recycle damaged organelles, in order to survive stresses…”
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