Search Results - "Bashore, Frances M"

Modulation of tau tubulin kinases (TTBK1 and TTBK2) impacts ciliogenesis by Bashore, Frances M., Marquez, Ariana B., Chaikuad, Apirat, Howell, Stefanie, Dunn, Andrea S., Beltran, Alvaro A., Smith, Jeffery L., Drewry, David H., Beltran, Adriana S., Axtman, Alison D.

“…Tau tubulin kinase 1 and 2 (TTBK1/2) are highly homologous kinases that are expressed and mediate disease-relevant pathways predominantly in the brain…”
Get full text

Characterization of covalent inhibitors that disrupt the interaction between the tandem SH2 domains of SYK and FCER1G phospho-ITAM by Bashore, Frances M, Katis, Vittorio L, Du, Yuhong, Sikdar, Arunima, Wang, Dongxue, Bradshaw, William J, Rygiel, Karolina A, Leisner, Tina M, Chalk, Rod, Mishra, Swati, Williams, C Andrew, Gileadi, Opher, Brennan, Paul E, Wiley, Jesse C, Gockley, Jake, Cary, Gregory A, Carter, Gregory W, Young, Jessica E, Pearce, Kenneth H, Fu, Haian, Axtman, Alison D

“…RNA sequencing and genetic data support spleen tyrosine kinase (SYK) and high affinity immunoglobulin epsilon receptor subunit gamma (FCER1G) as putative…”
Get full text

Discovery and characterization of a specific inhibitor of serine-threonine kinase cyclin-dependent kinase-like 5 (CDKL5) demonstrates role in hippocampal CA1 physiology by Castano, Anna, Silvestre, Margaux, Wells, Carrow I, Sanderson, Jennifer L, Ferrer, Carla A, Ong, Han Wee, Lang, Yi, Richardson, William, Silvaroli, Josie A, Bashore, Frances M, Smith, Jeffery L, Genereux, Isabelle M, Dempster, Kelvin, Drewry, David H, Pabla, Navlot S, Bullock, Alex N, Benke, Tim A, Ultanir, Sila K, Axtman, Alison D

“…Pathological loss-of-function mutations in cyclin-dependent kinase-like 5 ( ) cause CDKL5 deficiency disorder (CDD), a rare and severe neurodevelopmental…”
Get full text

Fused Tetrahydroquinolines Are Interfering with Your Assay by Bashore, Frances M, Annor-Gyamfi, Joel, Du, Yuhong, Katis, Vittorio, Nwogbo, Felix, Flax, Raymond G, Frye, Stephen V, Pearce, Kenneth H, Fu, Haian, Willson, Timothy M, Drewry, David H, Axtman, Alison D

“…Tricyclic tetrahydroquinolines (THQs) have been repeatedly reported as hits across a diverse range of high-throughput screening (HTS) campaigns. The activities…”
Get full text

PROTAC Linkerology Leads to an Optimized Bivalent Chemical Degrader of Polycomb Repressive Complex 2 (PRC2) Components by Bashore, Frances M., Foley, Caroline A., Ong, Han Wee, Rectenwald, Justin M., Hanley, Ronan P., Norris-Drouin, Jacqueline L., Cholensky, Stephanie H., Mills, Christine A., Pearce, Kenneth H., Herring, Laura E., Kireev, Dmitri, Frye, Stephen V., James, Lindsey I.

“…Bivalent chemical degraders, otherwise known as proteolysis-targeting chimeras (PROTACs), have proven to be an efficient strategy for targeting overexpressed…”
Get full text

Discovery of FERM domain protein–protein interaction inhibitors for MSN and CD44 as a potential therapeutic approach for Alzheimer’s disease by Du, Yuhong, Bradshaw, William J., Leisner, Tina M., Annor-Gyamfi, Joel K., Qian, Kun, Bashore, Frances M., Sikdar, Arunima, Nwogbo, Felix O., Ivanov, Andrey A., Frye, Stephen V., Gileadi, Opher, Brennan, Paul E., Levey, Allan I., Axtman, Alison D., Pearce, Kenneth H., Fu, Haian, Katis, Vittorio L.

“…Proteomic studies have identified moesin (MSN), a protein containing a four-point-one, ezrin, radixin, moesin (FERM) domain, and the receptor CD44 as hub…”
Get full text

Discovery and Characterization of a Chemical Probe for Cyclin-Dependent Kinase-Like 2 by Bashore, Frances M., Min, Sophia M., Chen, Xiangrong, Howell, Stefanie, Rinderle, Caroline H., Morel, Gabriel, Silvaroli, Josie A., Wells, Carrow I., Bunnell, Bruce A., Drewry, David H., Pabla, Navjot S., Ultanir, Sila K., Bullock, Alex N., Axtman, Alison D.

“…Acylaminoindazole-based inhibitors of CDKL2 were identified via analyses of cell-free binding and selectivity data. Compound 9 was selected as a CDKL2 chemical…”
Get full text

Discovery of a Potent and Selective Naphthyridine-Based Chemical Probe for Casein Kinase 2 by Davis-Gilbert, Zachary W., Krämer, Andreas, Dunford, James E., Howell, Stefanie, Senbabaoglu, Filiz, Wells, Carrow I., Bashore, Frances M., Havener, Tammy M., Smith, Jeffery L., Hossain, Mohammad A., Oppermann, Udo, Drewry, David H., Axtman, Alison D.

“…Naphthyridine-based inhibitors were synthesized to yield a potent and cell-active inhibitor of casein kinase 2 (CK2). Compound 2 selectively inhibits CK2α and…”
Get full text

Development of SYK NanoBRET cellular target engagement assays for gain–of–function variants by Jacob L. Capener, James D. Vasta, Vittorio L. Katis, Ani Michaud, Michael T. Beck, Sabrina C. D. Daglish, Sarit Cohen-Kedar, Sarit Cohen-Kedar, Efrat Shaham Barda, Efrat Shaham Barda, Stefanie Howell, Iris Dotan, Iris Dotan, Matthew B. Robers, Alison D. Axtman, Frances M. Bashore

“…Spleen tyrosine kinase (SYK) is a non-receptor tyrosine kinase that is activated by phosphorylation events downstream of FcR, B-cell and T-cell receptors,…”
Get full text

Efforts toward discovering inhibitors of the SYK SH2–FCER1γ interaction as potential Alzheimer’s disease chemical probes and therapeutics by Sikdar, Arunima, Bashore, Frances M., Katis, Vittorio, Bradshaw, William, Rygiel, Karolina, Du, Yuhong, Wang, Dongxue, Leisner, Tina, Hardy, Brian P., Kireev, Dmitri B., Pearce, Kenneth H., Fu, Haian, Frye, Stephen V., Axtman, Alison D.

“…Background Spleen associated tyrosine kinase (SYK) plays a potential role in several neurodegenerative conditions. To date, a few pharmacological inhibitors…”
Get full text

Characterization of covalent inhibitors that disrupt the interaction between the tandem SH2 domains of SYK and FCER1G phospho-ITAM by Frances M Bashore, Vittorio L Katis, Yuhong Du, Arunima Sikdar, Dongxue Wang, William J Bradshaw, Karolina A Rygiel, Tina M Leisner, Rod Chalk, Swati Mishra, C Andrew Williams, Opher Gileadi, Paul E Brennan, Jesse C Wiley, Jake Gockley, Gregory A Cary, Gregory W Carter, Jessica E Young, Kenneth H Pearce, Haian Fu, Emory-Sage-SGC TREAT-AD Center, Alison D Axtman

“…RNA sequencing and genetic data support spleen tyrosine kinase (SYK) and high affinity immunoglobulin epsilon receptor subunit gamma (FCER1G) as putative…”
Get full text