James Schiemer

A covalent BTK ternary complex compatible with targeted protein degradation

James Schiemer, Andrew Maxwell, Reto Horst, Shenping Liu et autres

Targeted protein degradation using heterobifunctional chimeras holds the potential to expand target space and grow the druggable proteome. Most acutely, this provides an opportunity to target proteins that lack enzymatic activity or have otherwise proven intractable to small molecule inhibition. Limiting this …

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Backbone assignments of the cIAP1-Bir3 domain

Reto Horst, James Schiemer, Kim Fennell

Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes

James Schiemer, Reto Horst, Yilin Meng, Justin I. Montgomery et autres

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Ternary complex structure - BTK cIAP compound 15

Matthew F. Calabrese, James Schiemer

Ternary complex structure - BTK cIAP compound 17

Matthew F. Calabrese, James Schiemer

Structure of cIAP with compound 15

Matthew F. Calabrese, James Schiemer

HIV protease inhibitors block parasite signal peptide peptidases and prevent growth of Babesia microti parasites in erythrocytes

Christopher Schwake, Michael R. Baldwin, William W. Bachovchin, Shreeya Hegde et autres

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Human erythrocyte band 3 is a host receptor for Plasmodium falciparum glutamic acid–rich protein

Haifa Almukadi, Christopher Schwake, Maima M. Kaiser, Daniel Mayer et autres

Abstract Malaria remains a major global threat to human health and economic development. Microvascular lesions caused by Plasmodium falciparum–infected human erythrocytes/red blood cells are hallmarks of severe pathogenesis contributing to high mortality, particularly in children from sub-Saharan Africa. In this study, we …

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Delineating the role of cooperativity in the design of potent PROTACs for BTK

Adelajda Zorba, Chuong Nguyen, Yingrong Xu, Jeremy T. Starr et autres

Proteolysis targeting chimeras (PROTACs) are heterobifunctional small molecules that simultaneously bind to a target protein and an E3 ligase, thereby leading to ubiquitination and subsequent degradation of the target. They present an exciting opportunity to modulate proteins in a manner independent of …

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Gα13 Switch Region 2 Relieves Talin Autoinhibition to Activate Platelet αIIbβ3 Integrin

James Schiemer, Andrew Bohm, Glenn Merrill‐Skoloff, Robert Flaumenhaft et autres

Abstract Integrins function as bi-directional signaling transducers that regulate cell-cell and cell-matrix signals across the membrane. A key modulator of integrin activation is talin, a large cytoskeletal protein that exists in an autoinhibited state in quiescent cells. Due to the fundamental importance …

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Gα13 Switch Region 2 Relieves Talin Autoinhibition to Activate αIIbβ3 Integrin

James Schiemer, Andrew Bohm, Lin Li, Glenn Merrill‐Skoloff et autres

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Gα13 Switch Region 2 Binds to the Talin Head Domain and Activates αIIbβ3 Integrin in Human Platelets

Subhashini Srinivasan, James Schiemer, Xiaowei Zhang, Athar H. Chishti et autres

Even though GPCR signaling in human platelets is directly involved in hemostasis and thrombus formation, the sequence of events by which G protein activation leads to αIIbβ3 integrin activation (inside-out signaling) is not clearly defined. We previously demonstrated that a conformationally sensitive …

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