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From Collaborating Labs

Parmodulin, an Allosteric Inhibitor of Protease Activated Receptor 1 (PAR1) Protects Sickle Cell Mice from Thromboinflammation and Endothelial Dysfunction

Ramadas, N.; Lowder, K.; Mosnier, L. O.; Pawlinski, R.; Sparkenbaugh, E.

64th American Society of Hematology Annual Meeting, abstract #2364

Protease Activated Receptor-1 (PAR-1) Inhibition By Parmodulin 2, but Not Vorapaxar, Protects Sickle Cell Mice from Heme-Induced Acute Chest Syndrome

Lowder, K.; Ramadas, N.; Pawlinski, R.; Sparkenbaugh, E.

64th American Society of Hematology Annual Meeting, abstract #1046

Reversal of the renal hyperglycemic memory by targeting sustained tubular p21 expression.

Al-Dabet, M. M.; Shahzad, K.; Elwakiel, A.; Sulaj, A.; Kopf, S.; Bock, F.; Gadi, I.; Zimmermann, S.; Rana, R.; Krishnan, S.; Gupta, D.; Nazir, S.; Geffers, R.; Mertens, P.; Nawroth, P. P.; Griffin, J.; Dockendorff, C.; Kohli, S.*; Isermann, B.*

Nature Communications 2022, 13, 5062.

A Thrombin-PAR1/2 Feedback Loop Amplifies Thrombo-Inflammatory Endothelial Responses To The Viral RNA Analogue Poly(I:C).

Subramaniam, S.; Ogoti, Y.; Hernandez, I.; Zogg, M.; Botros, F.; Burns, R. T.; DeRousse, J. T.; Dockendorff, C.; Mackman, N.; Antoniak, S.; Fletcher, C.; Weiler, H.

Blood Advances 2021, 5, 2760–2774.

The Evolving Concept of Neuro-Thromboinflammation for Neurodegenerative Disorders and Neurotrauma: a Rationale for PAR1-Targeting Therapies.

Festoff, B. W.*; Dockendorff, C.

Biomolecules 2021, 11, 1558.

Synthesis and initial pharmacology of dual-targeting ligands for putative complexes of integrin αVβ3 and PAR2.

Majewski, M. W.; Gandhi, D. M.; Holyst, T.; Wang, Z.; Hernandez, I.; Rosas Jr., R.; Zhu, J.; Weiler, H.; Dockendorff, C.*

RSC Med. Chem. 2020, 11, 940–949.

The parmodulin NRD-21 is a biased allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability.

Gandhi, D. M.; Rosas, Jr., R.; Greve, E.; Kentala, K.; Diby, N. D.-R.; Snyder, V. A.; Stephans, A.; Yeung, T. H. W.; Subramaniam, S.; DiMilo, E.; Kurtenbach, K. E.; Arnold, L. A.; Weiler, H.; Dockendorff, C.*

Bioorg. Med. Chem. 2019, 27, 3788–3796.

Design and evaluation of heterobivalent PAR1–PAR2 ligands as antagonists of calcium mobilization.

Majewski, M. W.; Gandhi, D. M.; Rosas Jr., R.; Dockendorff, C.*

ACS Med. Chem. Lett. 2019, 10, 121–126.

Characterization of Protease-Activated Receptor (PAR) ligands: Parmodulins are reversible allosteric inhibitors of PAR1-driven calcium mobilization in endothelial cells.

Gandhi, D. M.; Majewski, M. W.; Rosas, Jr., R.; Kentala, K.; Foster, T. J.; Greve, E.; Dockendorff, C.*

Bioorg. Med. Chem. 2018, 26, 2514–2529.

PAR1 agonists stimulate APC-like endothelial cytoprotection and confer resistance to thromboinflammatory injury.

De Ceunynck, K.; Peters, C. G.; Jain, A.; Higgins, S. J.; Aisiku, O.; Fitch-Tewfik, J. L.; Chaudhry, S. A.; Dockendorff, C.; Parikh, S. M.; Ingber, D. E.; Flaumenhaft, R.*

Proc. Nat. Acad. Sci. USA 2018, 115, E982–E991.

Cytoprotective activated protein C ameliorates Nlrp3 inflammasome induced ischemia reperfusion 1 injury via mTORC1 inhibition.

Nazir, S.; Gadi, I.; Al-Dabet, M. M.; Elwakiel, A.; Kohli, S.; Ghosh, S.; Manoharan, J.; Ranjan, S.; Bock, F.; Braun-Dullaeus, R. C.; Esmon, C. T.; Huber, T. B.; Camerer, E.; Dockendorff, C.; Griffin, J. H.; Isermann, B.*; Shahzad, K.*

Blood 2017, 130, 2664–2677.

Parmodulins Inhibit Thrombus Formation Without Inducing Endothelial Injury Caused by Vorapaxar.

Aisiku, O.; Peters, C. G.; De Cuenynck, K.; Ghosh, C. C.; Dilks, J. R.; Fustolo-Gunnink, S. F.; Huang, M.; Dockendorff, C.; Parikh, S. M.; Flaumenhaft, R.*

Blood 2015, 125, 1976–1985.

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