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David H. Hackos
Researcher at Genentech
Publications - 40
Citations - 1973
David H. Hackos is an academic researcher from Genentech. The author has contributed to research in topics: Biology & Medicine. The author has an hindex of 19, co-authored 34 publications receiving 1491 citations.
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Journal ArticleDOI
Pannexin-1 Is Required for ATP Release during Apoptosis but Not for Inflammasome Activation
Yan Qu,Shahram Misaghi,Kim Newton,Laurie L. Gilmour,Salina Louie,James E. Cupp,George R. Dubyak,David H. Hackos,Vishva M. Dixit +8 more
TL;DR: Thymocytes lacking pannexin-1, but not the P2X7R purinergic receptor, were defective in their uptake of the nucleic acid dye YO-PRO-1 during early apoptosis, consistent with pannexIn-1 liberating ATP and other yet to be defined “find me” signals necessary for macrophage recruitment to apoptotic cells.
Journal ArticleDOI
Structural basis of Nav1.7 inhibition by an isoform-selective small-molecule antagonist.
Shivani Ahuja,Susmith Mukund,Lunbin Deng,Kuldip Khakh,Elaine Chang,Hoangdung Ho,Stephanie Shriver,Clint Young,Sophia Lin,J. P. Johnson,Ping Wu,Jun Li,Mary Coons,Christine Tam,Bobby Brillantes,Honorio Sampang,Kyle Mortara,Krista K. Bowman,Kevin R Clark,Alberto Estevez,Zhiwei Xie,Henry Verschoof,Michael Edward Grimwood,Christoph Martin Dehnhardt,Jean-Christophe Andrez,Thilo Focken,Daniel P. Sutherlin,Brian Safina,Melissa A. Starovasnik,Daniel F. Ortwine,Yvonne Franke,Charles J. Cohen,David H. Hackos,Christopher M. Koth,Jian Payandeh +34 more
TL;DR: A novel protein-engineering strategy is devised that overcomes the technical complexities of producing full-length human Nav channels and demonstrates how this important new class of gating modifier engages VSD4 to inhibit Nav channel activity through a “voltage-sensor trapping” mechanism.
Journal ArticleDOI
Positive Allosteric Modulators of GluN2A-Containing NMDARs with Distinct Modes of Action and Impacts on Circuit Function
David H. Hackos,Patrick J. Lupardus,Teddy Grand,Yelin Chen,Tzu-Ming Wang,Paul Reynen,Amy Gustafson,Heidi J.A. Wallweber,Matthew Volgraf,Benjamin D. Sellers,Jacob Schwarz,Pierre Paoletti,Morgan Sheng,Qiang Zhou,Jesse E. Hanson +14 more
TL;DR: The identification of a new NMDAR modulatory site and characterization of GluN2A-selective PAMs provide powerful molecular tools to dissect N MDAR function and demonstrate the feasibility of a therapeutically desirable type of NMD AR enhancement.
Journal ArticleDOI
TRPA1 as a drug target—promise and challenges
Jun Chen,David H. Hackos +1 more
TL;DR: The recent progress, unsettled issues, and challenges in TRPA1 research and drug discovery are reviewed.
Journal ArticleDOI
Structural basis of α-scorpion toxin action on Nav channels
Thomas Clairfeuille,Alexander Cloake,Alexander Cloake,Daniel T. Infield,José P. Llongueras,Christopher P. Arthur,Zhong Rong Li,Yuwen Jian,Marie-France Martin-Eauclaire,Pierre E. Bougis,Claudio Ciferri,Christopher A. Ahern,Frank Bosmans,David H. Hackos,Alexis Rohou,Jian Payandeh +15 more
TL;DR: Structures reveal how activation of voltage-gated sodium channels causes conformational changes in a voltage-sensor domain, leading to fast inactivation, and pharmacological trapping of VSD4 reveals state-dependent interactions of gating charges from the S4 helix and S4-S5 linker.