Search Results - "Madhu, Chintala"

Antithrombotic Effects of the Novel Small-Molecule Factor XIa Inhibitor Milvexian in a Rabbit Arteriovenous Shunt Model of Venous Thrombosis by Wang, Xinkang, Li, Qiu, Du, Fuyong, Shukla, Neetu, Nawrocki, Andrea R, Chintala, Madhu

“…Factor XIa (FXIa) is an emerging therapeutic target, and FXIa inhibition is a promising mechanism to improve therapeutic index over current anticoagulants…”
Get full text

Basic and Translational Research on Proteinase-Activated Receptors: Antagonism of the Proteinase-Activated Receptor 1 for Thrombin, a Novel Approach to Antiplatelet Therapy for Atherothrombotic Disease by Chintala, Madhu, Shimizu, Kenji, Ogawa, Masami, Yamaguchi, Hiroya, Doi, Masaki, Jensen, Peder

“…Atherothrombotic disease is a leading public health problem. Although current antiplatelet agents, such as aspirin and adenosine diphosphate (ADP)-receptor…”
Get full text

Discovery of Potent Orally Active Thrombin Receptor (Protease Activated Receptor 1) Antagonists as Novel Antithrombotic Agents by Chackalamannil, Samuel, Xia, Yan, Greenlee, William J, Clasby, Martin, Doller, Darìo, Tsai, Hsingan, Asberom, Theodros, Czarniecki, Michael, Ahn, Ho-Sam, Boykow, George, Foster, Carolyn, Agans-Fantuzzi, Jacqueline, Bryant, Matthew, Lau, Janice, Chintala, Madhu

“…Structurally novel thrombin receptor (protease activated receptor 1, PAR-1) antagonists based on the natural product himbacine are described. The prototypical…”
Get full text

Cardiac Expression of Factor X Mediates Cardiac Hypertrophy and Fibrosis in Pressure Overload by Guo, Xinji, Kolpakov, Mikhail A, Hooshdaran, Bahman, Schappell, William, Wang, Tao, Eguchi, Satoru, Elliott, Katherine J, Tilley, Douglas G, Rao, A Koneti, Andrade-Gordon, Patricia, Bunce, Matthew, Madhu, Chintala, Houser, Steven R, Sabri, Abdelkarim

“…Activated factor X is a key component of the coagulation cascade, but whether it directly regulates pathological cardiac remodeling is unclear. In mice…”
Get full text

Inhibition of Protease-activated Receptor 1 Ameliorates Intestinal Radiation Mucositis in a Preclinical Rat Model by Wang, Junru, MD, PhD, Kulkarni, Ashwini, MS, Chintala, Madhu, PhD, Fink, Louis M., MD, Hauer-Jensen, Martin, MD, PhD

“…Purpose To determine, using a specific small-molecule inhibitor of protease-activated receptor 1 (PAR1) signaling, whether the beneficial effect of thrombin…”
Get full text

RETRACTED: Cardiac Expression of Factor X Mediates Cardiac Hypertrophy and Fibrosis in Pressure Overload by Guo, Xinji, Kolpakov, Mikhail A., Hooshdaran, Bahman, Schappell, William, Wang, Tao, Eguchi, Satoru, Elliott, Katherine J., Tilley, Douglas G., Rao, A. Koneti, Andrade-Gordon, Patricia, Bunce, Matthew, Madhu, Chintala, Houser, Steven R., Sabri, Abdelkarim

Get full text

Discovery of SCH 900271, a Potent Nicotinic Acid Receptor Agonist for the Treatment of Dyslipidemia by Palani, Anandan, Rao, Ashwin U, Chen, Xiao, Huang, Xianhai, Su, Jing, Tang, Haiqun, Huang, Ying, Qin, Jun, Xiao, Dong, Degrado, Sylvia, Sofolarides, Michael, Zhu, Xiaohong, Liu, Zhidan, McKittrick, Brian, Zhou, Wei, Aslanian, Robert, Greenlee, William J, Senior, Mary, Cheewatrakoolpong, Boonlert, Zhang, Hongtao, Farley, Constance, Cook, John, Kurowski, Stan, Li, Qiu, van Heek, Margaret, Wang, Gangfeng, Hsieh, Yunsheng, Li, Fangbiao, Greenfeder, Scott, Chintala, Madhu

“…Structure-guided optimization of a series of C-5 alkyl substituents led to the discovery of a potent nicotinic acid receptor agonist SCH 900271 (33) with an…”
Get full text

Metabolism-Based Identification of a Potent Thrombin Receptor Antagonist by Clasby, Martin C, Chackalamannil, Samuel, Czarniecki, Michael, Doller, Dario, Eagen, Keith, Greenlee, William, Kao, Grace, Lin, Yan, Tsai, Hsingan, Xia, Yan, Ahn, Ho-Sam, Agans-Fantuzzi, Jacqueline, Boykow, George, Chintala, Madhu, Foster, Carolyn, Smith-Torhan, April, Alton, Kevin, Bryant, Matthew, Hsieh, Yunsheng, Lau, Janice, Palamanda, Jairam

“…The metabolism of our prototypical thrombin receptor antagonist 1, K i = 2.7 nM, was studied and three major metabolites (2, 4, and 5) were found. The…”
Get full text

Molecular identification and characterization of the platelet ADP receptor targeted by thienopyridine antithrombotic drugs by Foster, C J, Prosser, D M, Agans, J M, Zhai, Y, Smith, M D, Lachowicz, J E, Zhang, F L, Gustafson, E, Monsma, Jr, F J, Wiekowski, M T, Abbondanzo, S J, Cook, D N, Bayne, M L, Lira, S A, Chintala, M S

“…ADP plays a critical role in modulating thrombosis and hemostasis. ADP initiates platelet aggregation by simultaneous activation of two G protein-coupled…”
Get full text

Himbacine derived thrombin receptor antagonists: Discovery of a new tricyclic core by Clasby, Martin C., Chackalamannil, Samuel, Czarniecki, Michael, Doller, Darío, Eagen, Keith, Greenlee, William J., Lin, Yan, Tagat, Jayaram R., Tsai, Hsingan, Xia, Yan, Ahn, Ho-Sam, Agans-Fantuzzi, Jacqueline, Boykow, George, Chintala, Madhu, Hsieh, Yunsheng, McPhail, Andrew T.

“…The synthesis and biological activity of a novel series of thrombin receptor antagonists is described. This series of compounds showed excellent in vitro and…”
Get full text

The anticoagulant effects of milvexian, a novel small molecule FXIa inhibitor, are neutralized by aPCC and rFVIIa in human plasma and whole blood in vitro by Bunce, Matthew, Devine, Zheng Huang, Chintala, Madhu

Get full text

FEIBA® and Novoseven® Neutralize the Anticoagulant Effects of a Novel Small Molecule FXIa Inhibitor BMS-986177/JNJ-70033093 in Human Plasma and Whole Blood in Vitro by Bunce, Matthew W, Huang Devine, Zheng, Chintala, Madhu

“…Background: FXIa inhibition is a promising antithrombotic drug target. BMS-986177/JNJ-70033093 (BMS-177/JNJ-3093) is a novel small molecular inhibitor of FXIa…”
Get full text

Evidence for the Presence of a Proteinase-Activated Receptor Distinct From the Thrombin Receptor in Vascular Endothelial Cells by Hwa, Joyce J, Ghibaudi, Lorraine, Williams, Patricia, Chintala, Madhu, Zhang, Rumin, Chatterjee, Meeta, Sybertz, Edmund

“…The thrombin receptor was the first cloned G protein-coupled receptor reported to be activated by proteolytic cleavage of its extracellular amino terminus. A…”
Get full text

Abstract 521: Pharmacological Profile of JNJ-64179375: a Novel, Long Acting Exosite-1 Thrombin Inhibitor by Huang Devine, Zheng, Li, Qiu, Chintala, Madhu

“…Abstract only Background: Thrombin is a key serine protease involved in hemostasis and thrombosis by mediating the conversion of soluble fibrinogen to…”
Get full text

Measuring the Anticoagulation Effects of Exosite I Thrombin Inhibitors: Utility and Limitations of Clotting Assays, Thromboelastography, and Calibrated Automated Thrombography by Bunce, Matthew, Huang Devine, Zheng, Chintala, Madhu

“…The ability to anticoagulate patients at elevated risk for thrombosis without inducing a bleeding diathesis remains an unmet need of patient care both in a…”
Get full text

JNJ-64179375 Inhibits Exosite I-Mediated Thrombin Activity While Preserving Exosite II and Active Site Function in Vitro by Bunce, Matthew, Chintala, Madhu, Krishnaswamy, Sriram, Bradford, Harlan N

“…Anticoagulation requires a careful balance to achieve antithrombotic efficacy without disrupting normal hemostasis. Although current generation direct oral…”
Get full text

Preferential Inhibition of Fibrin Mediated Thrombosis in Rodent Models By JNJ-9375, a Novel exosite1 Thrombin Inhibitor by Chintala, Madhu, Li, Qiu, Huang Devine, Zheng, Bunce, Matthew

“…We have previously reported an improved therapeutic index (TI) for JNJ-9375 vs apixaban in rat and cynomolgus monkey models of venous thrombosis and bleeding…”
Get full text

S1B3-6 A new approach to antiplatelet treatment with a PAR-1 antagonist in patients with atherosclerosis by Kenji Shimizu, Masami Ogawa, Hiroya Yamaguchi, Junpei Shibata, Pader Jensen, Madhu Chintala

Get full text

Translational PK/PD and model-informed development of JNJ-67842125, a F ab reversal agent for JNJ-64179375, a long-acting thrombin inhibitor by Ayyar, Vivaswath S, Jaiprasart, Pharavee, Geist, Brian, Huang Devine, Zheng, Case, Martin, Hazra, Anasuya, Hsu, Chyi-Hung, Chintala, Madhu, Wang, Weirong

“…Antigen-binding fragment (F ) reversal agents (RAs) were developed to reverse, in situations of bleeding emergency, the anticoagulant activity of JNJ-64179375…”
Get full text

Pharmacological Profile of JNJ-64179375: A Novel, Long-Acting Exosite-1 Thrombin Inhibitor by Huang Devine, Zheng, Du, Fuyong, Li, Qiu, Bunce, Matthew, Lacy, Eilyn R, Chintala, Madhu

“…JNJ-64179375 (JNJ-9375) is a recombinant human IgG4 monoclonal antibody engineered to mimic an IgA antibody that was identified in a patient who exhibited…”
Get more information