Search Results - "Sjodin, P."

RNA-modifying proteins as anticancer drug targets by Boriack-Sjodin, P. Ann, Ribich, Scott, Copeland, Robert A.

“…Covalent modifications of RNA — mediated by RNA-modifying proteins (RMPs) — affect RNA stability and translation to proteins, and some of these RMPs have been…”
Get full text

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia by Daigle, Scott R., Olhava, Edward J., Therkelsen, Carly A., Basavapathruni, Aravind, Jin, Lei, Boriack-Sjodin, P. Ann, Allain, Christina J., Klaus, Christine R., Raimondi, Alejandra, Scott, Margaret Porter, Waters, Nigel J., Chesworth, Richard, Moyer, Mikel P., Copeland, Robert A., Richon, Victoria M., Pollock, Roy M.

“…Rearrangements of the MLL gene define a genetically distinct subset of acute leukemias with poor prognosis. Current treatment options are of limited…”
Get full text

Protein Methyltransferases: A Distinct, Diverse, and Dynamic Family of Enzymes by Boriack-Sjodin, P. Ann, Swinger, Kerren K

“…Methyltransferase proteins make up a superfamily of enzymes that add one or more methyl groups to substrates that include protein, DNA, RNA, and small…”
Get full text

Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation by Thomenius, Michael J, Totman, Jennifer, Harvey, Darren, Mitchell, Lorna H, Riera, Thomas V, Cosmopoulos, Kat, Grassian, Alexandra R, Klaus, Christine, Foley, Megan, Admirand, Elizabeth A, Jahic, Haris, Majer, Christina, Wigle, Tim, Jacques, Suzanne L, Gureasko, Jodi, Brach, Dorothy, Lingaraj, Trupti, West, Kip, Smith, Sherri, Rioux, Nathalie, Waters, Nigel J, Tang, Cuyue, Raimondi, Alejandra, Munchhof, Michael, Mills, James E, Ribich, Scott, Porter Scott, Margaret, Kuntz, Kevin W, Janzen, William P, Moyer, Mikel, Smith, Jesse J, Chesworth, Richard, Copeland, Robert A, Boriack-Sjodin, P Ann

“…A key challenge in the development of precision medicine is defining the phenotypic consequences of pharmacological modulation of specific target…”
Get full text

A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models by Chan-Penebre, Elayne, Kuplast, Kristy G, Majer, Christina R, Boriack-Sjodin, P Ann, Wigle, Tim J, Johnston, L Danielle, Rioux, Nathalie, Munchhof, Michael J, Jin, Lei, Jacques, Suzanne L, West, Kip A, Lingaraj, Trupti, Stickland, Kimberly, Ribich, Scott A, Raimondi, Alejandra, Scott, Margaret Porter, Waters, Nigel J, Pollock, Roy M, Smith, Jesse J, Barbash, Olena, Pappalardi, Melissa, Ho, Thau F, Nurse, Kelvin, Oza, Khyati P, Gallagher, Kathleen T, Kruger, Ryan, Moyer, Mikel P, Copeland, Robert A, Chesworth, Richard, Duncan, Kenneth W

“…Protein methyltransferase PRMT5 symmetrically dimethylates arginine residues in proteins, including histones, and has been associated with tumorigenesis. The…”
Get full text

Identification of a peptide inhibitor for the histone methyltransferase WHSC1 by Morrison, Michael J, Boriack-Sjodin, P Ann, Swinger, Kerren K, Wigle, Tim J, Sadalge, Dipti, Kuntz, Kevin W, Scott, Margaret Porter, Janzen, William P, Chesworth, Richard, Duncan, Kenneth W, Harvey, Darren M, Lampe, John W, Mitchell, Lorna H, Copeland, Robert A

“…WHSC1 is a histone methyltransferase that is responsible for mono- and dimethylation of lysine 36 on histone H3 and has been implicated as a driver in a…”
Get full text

The Elements of Translational Chemical Biology by Copeland, Robert A, Boriack-Sjodin, P Ann

“…A causal relationship between target activity modulation by small molecules and phenotypic consequence is the cornerstone of chemical biology and drug…”
Get more information

Crystal structures of the DExH‐box RNA helicase DHX9 by Young-Tae, Lee, E Allen Sickmier, Grigoriu, Simina, Castro, Jennifer, Boriack-Sjodin, P Ann

“…DHX9 is a DExH‐box RNA helicase with versatile functions in transcription, translation, RNA processing and regulation of DNA replication. DHX9 has recently…”
Get full text

Pyrrolamide DNA Gyrase Inhibitors: Fragment-Based Nuclear Magnetic Resonance Screening To Identify Antibacterial Agents by Eakin, Ann E, Green, Oluyinka, Hales, Neil, Walkup, Grant K, Bist, Shanta, Singh, Alok, Mullen, George, Bryant, Joanna, Embrey, Kevin, Gao, Ning, Breeze, Alex, Timms, Dave, Andrews, Beth, Uria-Nickelsen, Maria, Demeritt, Julie, Loch, James T., III, Hull, Ken, Blodgett, April, Illingworth, Ruth N, Prince, Bryan, Boriack-Sjodin, P. Ann, Hauck, Sheila, MacPherson, Lawrence J, Ni, Haihong, Sherer, Brian

“…DNA gyrase is an essential enzyme in bacteria, and its inhibition results in the disruption of DNA synthesis and, subsequently, cell death. The pyrrolamides…”
Get full text

Discovery of a novel azaindole class of antibacterial agents targeting the ATPase domains of DNA gyrase and Topoisomerase IV by Manchester, John I., Dussault, Daemian D., Rose, Jonathan A., Boriack-Sjodin, P. Ann, Uria-Nickelsen, Maria, Ioannidis, Georgine, Bist, Shanta, Fleming, Paul, Hull, Kenneth G.

“…We present the discovery and optimization of a novel series of bacterial topoisomerase inhibitors. Starting from a virtual screening hit, activity was…”
Get full text

The structural basis of the activation of Ras by Sos by Boriack-Sjodin, P. Ann, Margarit, S. Mariana, Bar-Sagi, Dafna, Kuriyan, John

“…The crystal structure of human H-Ras complexed with the Ras guanine-nucleotide-exchange-factor region of the Son of sevenless (Sos) protein has been determined…”
Get full text

A Potent, Selective, Small-Molecule Inhibitor of DHX9 Abrogates Proliferation of Microsatellite Instable Cancers with Deficient Mismatch Repair by Castro, Jennifer, Daniels, Matthew H., Brennan, David, Johnston, Brian, Gotur, Deepali, Lee, Young-Tae, Knockenhauer, Kevin E., Lu, Chuang, Wu, Jie, Nayak, Sunaina, Collins, Cindy, Bansal, Rishabh, Buker, Shane M., Case, April, Liu, Julie, Yao, Shihua, Sparling, Brian A., Sickmier, E. Allen, Silver, Serena J., Blakemore, Stephen J., Boriack-Sjodin, P. Ann, Duncan, Kenneth W., Ribich, Scott, Copeland, Robert A.

“…DHX9 is a multifunctional DExH-box RNA helicase with important roles in the regulation of transcription, translation, and maintenance of genome stability…”
Get full text

CARM1 Preferentially Methylates H3R17 over H3R26 through a Random Kinetic Mechanism by Jacques, Suzanne L, Aquino, Katrina P, Gureasko, Jodi, Boriack-Sjodin, P. Ann, Porter Scott, Margaret, Copeland, Robert A, Riera, Thomas V

“…CARM1 is a type I arginine methyltransferase involved in the regulation of transcription, pre-mRNA splicing, cell cycle progression, and the DNA damage…”
Get full text

Fragment-to-Hit-to-Lead Discovery of a Novel Pyridylurea Scaffold of ATP Competitive Dual Targeting Type II Topoisomerase Inhibiting Antibacterial Agents by Basarab, Gregory S, Manchester, John I, Bist, Shanta, Boriack-Sjodin, P. Ann, Dangel, Brian, Illingworth, Ruth, Sherer, Brian A, Sriram, Shubha, Uria-Nickelsen, Maria, Eakin, Ann E

“…The discovery and optimization of a new class of bacterial topoisomerase (DNA gyrase and topoisomerase IV) inhibitors binding in the ATP domain are described…”
Get full text

Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666 by Duncan, Kenneth W, Rioux, Nathalie, Boriack-Sjodin, P. Ann, Munchhof, Michael J, Reiter, Lawrence A, Majer, Christina R, Jin, Lei, Johnston, L. Danielle, Chan-Penebre, Elayne, Kuplast, Kristy G, Porter Scott, Margaret, Pollock, Roy M, Waters, Nigel J, Smith, Jesse J, Moyer, Mikel P, Copeland, Robert A, Chesworth, Richard

“…The recent publication of a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) provides the scientific community with in vivo-active tool…”
Get full text

Affinity enhancement of an in vivo matured therapeutic antibody using structure‐based computational design by Clark, Louis A., Boriack‐Sjodin, P. Ann, Eldredge, John, Fitch, Christopher, Friedman, Bethany, Hanf, Karl J.M., Jarpe, Matthew, Liparoto, Stefano F., Li, You, Lugovskoy, Alexey, Miller, Stephan, Rushe, Mia, Sherman, Woody, Simon, Kenneth, Van Vlijmen, Herman

“…Improving the affinity of a high‐affinity protein–protein interaction is a challenging problem that has practical applications in the development of…”
Get full text

Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound by Mitchell, Lorna H., Drew, Allison E., Ribich, Scott A., Rioux, Nathalie, Swinger, Kerren K., Jacques, Suzanne L., Lingaraj, Trupti, Boriack-Sjodin, P. Ann, Waters, Nigel J., Wigle, Tim J., Moradei, Oscar, Jin, Lei, Riera, Tom, Porter-Scott, Margaret, Moyer, Mikel P., Smith, Jesse J., Chesworth, Richard, Copeland, Robert A.

“…A novel aryl pyrazole series of arginine methyltransferase inhibitors has been identified. Synthesis of analogues within this series yielded the first potent,…”
Get full text

Enzyme-Inhibitor Interactions and a Simple, Rapid Method for Determining Inhibition Modality by Buker, Shane M, Boriack-Sjodin, P Ann, Copeland, Robert A

“…Contemporary chemical biology and drug discovery are increasingly focused on the discovery of inhibitory molecules that interact with enzyme targets in…”
Get more information

Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor by Basavapathruni, Aravind, Olhava, Edward J., Daigle, Scott R., Therkelsen, Carly A., Jin, Lei, Boriack-Sjodin, P. Ann, Allain, Christina J., Klaus, Christine R., Raimondi, Alejandra, Scott, Margaret Porter, Dovletoglou, Angelos, Richon, Victoria M., Pollock, Roy M., Copeland, Robert A., Moyer, Mikel P., Chesworth, Richard, Pearson, Paul G., Waters, Nigel J.

“…ABSTRACT…”
Get full text

Structural Insights into Ternary Complex Formation of Human CARM1 with Various Substrates by Boriack-Sjodin, P. Ann, Jin, Lei, Jacques, Suzanne L, Drew, Allison, Sneeringer, Chris, Scott, Margaret Porter, Moyer, Mikel P, Ribich, Scott, Moradei, Oscar, Copeland, Robert A

“…Coactivator-associated arginine methyltransferase 1 (CARM1) is a protein arginine N-methyltransferase (PRMT) enzyme that has been implicated in a variety of…”
Get full text