Search Results - "Fulton, Mark G."

Structure of a reaction intermediate mimic in t6A biosynthesis bound in the active site of the TsaBD heterodimer from Escherichia coli by Kopina, Brett J, Missoury, Sophia, Collinet, Bruno, Fulton, Mark G, Cirio, Charles, van Tilbeurgh, Herman, Lauhon, Charles T

“…Abstract The tRNA modification N6-threonylcarbamoyladenosine (t6A) is universally conserved in all organisms. In bacteria, the biosynthesis of t6A requires…”
Get full text

Formal Total Synthesis of Pericoannosin A by Fulton, Mark G, Bertron, Jeanette L, Reed, Carson W, Lindsley, Craig W

“…A concise formal total synthesis of pericoannosin A, by the synthesis of an advanced intermediate of pericoannosin A, was achieved in eight steps from…”
Get full text

Structure-Activity Relationships, Pharmacokinetics, and Pharmacodynamics of the Kir6.2/SUR1-Specific Channel Opener VU0071063 by Kharade, Sujay V, Sanchez-Andres, Juan Vicente, Fulton, Mark G, Shelton, Elaine L, Blobaum, Anna L, Engers, Darren W, Hofmann, Christopher S, Dadi, Prasanna K, Lantier, Louise, Jacobson, David A, Lindsley, Craig W, Denton, Jerod S

“…Glucose-stimulated insulin secretion from pancreatic -cells is controlled by ATP-regulated potassium (K ) channels composed of Kir6.2 and sulfonylurea receptor…”
Get more information

Discovery and optimization of a novel CNS penetrant series of mGlu4 PAMs based on a 1,4-thiazepane core with in vivo efficacy in a preclinical Parkinsonian model by Kent, Caitlin N., Fulton, Mark G., Stillwell, Kaylee J., Dickerson, Jonathan W., Loch, Matthew T., Rodriguez, Alice L., Blobaum, Anna L., Boutaud, Olivier, Rook, Jerri L., Niswender, Colleen M., Conn, P. Jeffrey, Lindsley, Craig W.

“…[Display omitted] A high throughput screen (HTS) identified a novel, but weak (EC50 = 6.2 μM, 97% Glu Max) mGlu4 PAM chemotype based on a 1,4-thiazepane core,…”
Get full text

Synthesis and pharmacological evaluation of bivalent tethered ligands to target the mGlu2/4 heterodimeric receptor results in a compound with mGlu2/2 homodimer selectivity by Fulton, Mark G., Loch, Matthew T., Rodriguez, Alice L., Lin, Xin, Javitch, Jonathan A., Conn, P. Jeffrey, Niswender, Colleen M., Lindsley, Craig W.

“…[Display omitted] •Detailed SAR of tethered PAM ligands targeting the mGlu2/4 heterodimer.•When DCG-IV and L-AP4 agonists are combined, 14d can potentiate the…”
Get full text

Total synthesis of violaceimides A–E and consideration of the reported stereochemistry by Perry, Charles K., Fulton, Mark G., Lindsley, Craig W.

“…[Display omitted] •First total synthesis of violaceimides A–E.•Synthesis of unnatural diastereomers.•Consideration and revision of stereochemical assignment…”
Get full text

Total synthesis of natural (−)- and unnatural (+)-Melearoride A by Reed, Carson W., Fulton, Mark G., Nance, Kellie D., Lindsley, Craig W.

“…[Display omitted] •First total synthesis of (−)-Melearoride A.•Total synthesis of (+)-Melearoride A.•A concise 13 step synthesis from chiral pool starting…”
Get full text

Challenges in the Discovery and Optimization of MGLU2/4 Heterodimer Positive Allosteric Modulators and Total Synthesis of Epi- and Pericoannosin A by Fulton, Mark G

“…The metabotropic glutamate receptor 2/4 (mGlu2/4) heterodimer is a recently discovered receptor that displays unique pharmacology with respect to both mGlu2…”
Get full text

Synthesis and pharmacological evaluation of bivalent tethered ligands to target the mGlu 2/4 heterodimeric receptor results in a compound with mGlu 2/2 homodimer selectivity by Fulton, Mark G, Loch, Matthew T, Rodriguez, Alice L, Lin, Xin, Javitch, Jonathan A, Conn, P Jeffrey, Niswender, Colleen M, Lindsley, Craig W

“…This Letter details our ongoing efforts to develop selective positive allosteric modulators (PAMs) of the mGlu heterodimeric receptor that exists in the CNS…”
Get full text

Discovery and optimization of a novel CNS penetrant series of mGlu 4 PAMs based on a 1,4-thiazepane core with in vivo efficacy in a preclinical Parkinsonian model by Kent, Caitlin N, Fulton, Mark G, Stillwell, Kaylee J, Dickerson, Jonathan W, Loch, Matthew T, Rodriguez, Alice L, Blobaum, Anna L, Boutaud, Olivier, Rook, Jerri L, Niswender, Colleen M, Conn, P Jeffrey, Lindsley, Craig W

“…A high throughput screen (HTS) identified a novel, but weak (EC  = 6.2 μM, 97% Glu Max) mGlu PAM chemotype based on a 1,4-thiazepane core, VU0544412. Reaction…”
Get full text