Search Results - "Teresk, Martin"

Thermodynamic and Structural Effects of Conformational Constraints in Protein−Ligand Interactions. Entropic Paradoxy Associated with Ligand Preorganization by DeLorbe, John E, Clements, John H, Teresk, Martin G, Benfield, Aaron P, Plake, Hilary R, Millspaugh, Laura E, Martin, Stephen F

“…Succinate- and cyclopropane-derived phosphotyrosine (pY) replacements were incorporated into a series of Grb2 SH2 binding ligands wherein the pY+1 residue was…”
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Deficiencies in Traditional Oral Dosage Forms and the Emergence of Controlled-Release Powder Manufacturing by Teresk, Martin G., Berkland, Cory J., Dormer, Nathan H.

“…The importance of providing safe and effective delayed- and extended-release oral formulations that can replace products requiring multiple administrations has…”
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Ligand Preorganization May Be Accompanied by Entropic Penalties in Protein-Ligand Interactions by Benfield, Aaron P., Teresk, Martin G., Plake, Hilary R., DeLorbe, John E., Millspaugh, Laura E., Martin, Stephen F.

“…Fact or fiction? It is generally assumed that preorganization of a flexible ligand in the 3D shape it adopts when bound to a macromolecular receptor will…”
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Evaluation of solution oxygenation requirements for azonitrile-based oxidative forced degradation studies of pharmaceutical compounds by Nelson, Eric D, Harmon, Paul A, Szymanik, Renee C, Teresk, Martin G, Li, Li, Seburg, Randal A, Reed, Robert A

“…AIBN and ACVA oxidative forced degradation models are examined for two drug molecules whose predominant oxidation chemistries arise from different reaction…”
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A phase 2 basket trial of ulixertinib (BVD-523) in combination with hydroxychloroquine in patients with advanced gastrointestinal malignancies harboring MAPK pathway mutations (BVD-523-HCQ) by Ko, Andrew H., Zalupski, Mark, Al-Rajabi, Raed Moh'd Taiseer, Matin, Khalid, Cohen, Deirdre Jill, Krishnamurthi, Smitha S., Kreider, Brent, Box, Jessica A., Emery, Caroline, Teresk, Martin, Varterasian, Mary Laura, Lee, Martin, Groover, Anna, Knoerzer, Deb, Shroff, Rachna T.

“…TPS4174 Background: RAS-induced signaling through the mitogen-activated protein kinase/extracellular signal-regulated kinase (MAPK/ERK) pathway plays an…”
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Abstract B085: Preclinical pharmacokinetic/pharmacodynamic (PK/PD) relationship demonstrated for BVD-723, a potent and selective phosphoinositide 3-kinase gamma (PI3Kγ) inhibitor by Knoerzer, Deborah, Teresk, Martin, Krutzik, Peter, O’Donnell, Erika, DeCrescenzo, Gary, Welsch, Dean, Emery, Caroline

“…Abstract The phosphoinositide 3-kinase (PI3K) family of enzymes play a pivotal role in controlling vital cellular functions, including proliferation, motility,…”
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Abstract 2693: Combining ulixertinib (ERK1/2 Inhibitor) with EGFR and BRAF inhibition yields significant efficacy in preclinical BRAF V600E mutant colorectal cancer models by Knoerzer, Deborah, Reddy, Anupama, Box, Jessica A., Groover, Anna, Kreider, Brent, Teresk, Martin, Emery, Caroline M.

“…Abstract The BRAFV600E mutation occurs in approximately 7% of colorectal cancer (CRC). BRAF plus EGFR inhibition (encorafenib with cetuximab) is an FDA…”
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Abstract 2692: The combination of ulixertinib (ERK1/2 Inhibitor) and KRASG12C inhibition demonstrates significant efficacy in preclinical models by Knoerzer, Deborah, Reddy, Anupama, Box, Jessica A., Groover, Anna, Kreider, Brent, Teresk, Martin, Emery, Caroline M.

“…Abstract Ulixertinib (BVD-523) is a first-in-class and best-in-class small molecule inhibitor of ERK1/2 currently being investigated in several oncology…”
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Design, synthesis & thermodynamic evaluation of conformationally-constrained pseudopeptides and synthetic approaches to sieboldine A by Teresk, Martin Gerald

“…A series of conformationally constrained and flexible pseudopeptides were prepared and their thermodynamic parameters on binding to the Grb2 SH2 domain were…”
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Ligand Preorganization May Be Accompanied by Entropic Penalties in Protein-Ligand Interactions by Benfield, Aaron P., Teresk, Martin G., Plake, Hilary R., DeLorbe, John E., Millspaugh, Laura E., Martin, Stephen F.

“…Fakt oder Fiktion? Es wird allgemein angenommen, dass die Präorganisation eines flexiblen Liganden zu der dreidimensionalen Form, die er bei der Bindung an…”
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Ligand Preorganization May Be Accompanied by Entropic Penalties in Protein–Ligand Interactions by Benfield, Aaron P., Teresk, Martin G., Plake, Hilary R., DeLorbe, John E., Millspaugh, Laura E., Martin, Stephen F.

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