Zobrazeno 1 - 10
of 124
pro vyhledávání: '"Mark G. Bock"'
Autor:
David Harrison, Mark G. Bock, John R. Doedens, Christopher A. Gabel, M. Katharine Holloway, Arwel Lewis, Jane Scanlon, Andrew Sharpe, Iain D. Simpson, Pamela Smolak, Grant Wishart, Alan P. Watt
Publikováno v:
ACS Medicinal Chemistry Letters. 13:1321-1328
The NLRP3 inflammasome is a multiprotein complex that facilitates activation and release of the proinflammatory cytokines interleukin-1β (IL-1β) and IL-18 in response to infection or endogenous stimuli. It can be inappropriately activated by a rang
Autor:
Shreyas Deshpande, Rashmi Talwar, Ganesh Navinchandra Gote, Jayasagar Gundu, Rupali Vyawahare, Shashikant Pawar, Akshaya Wagh, Talha Khan, Anil Kalia, Venkata P. Palle, Usha Dhayagude, M. K. Singh, Pradeep Patil, Ganesh Chaure, Praveen Kumar Gupta, Amit Das, Vijay Kanoje, Sharad Sharma, Vidya Ramdas, Vinod Patil, Rajesh Yeshodharan, Prashant B. Nigade, Dipak Modi, Dnyaneshwar Warude, Dilip Pandey, Jagadeesh Daler, Mahammad Azhar, Arun Nayak, Sneha Joshi, Sudipto Das, Rajender Kumar Kamboj, Javed S Shaikh, Maneesh Mehta, Deepak Sahebrao Walke, Rajesh V. Gupta, Himani Pareek, Kumar V S Nemmani, Parag Joshi, Mahip Verma, Vinod Mali, Laxmikant Datrange, Santosh Parkale, Rajesh Loriya, Vaibhav Kalhapure, Geetika Sharma, Ravindra R. Pal, Sagar Budhe, Gautam Agarwal, Sachin Suravase, Sagar Darekar, Mark G. Bock, Advait Arun Joshi, Moloy Banerjee, Smita Bhoskar, Amitesh Kishore, Dhananjay Bakhle
Publikováno v:
Journal of Medicinal Chemistry. 63:6107-6133
Voltage-gated sodium channel NaV1.7 is a genetically validated target for pain. Identification of NaV1.7 inhibitors with all of the desired properties to develop as an oral therapeutic for pain has been a major challenge. Herein, we report systematic
Autor:
Vidya, Ramdas, Rashmi, Talwar, Vijay, Kanoje, Rajesh M, Loriya, Moloy, Banerjee, Pradeep, Patil, Advait Arun, Joshi, Laxmikant, Datrange, Amit Kumar, Das, Deepak Sahebrao, Walke, Vaibhav, Kalhapure, Talha, Khan, Ganesh, Gote, Usha, Dhayagude, Shreyas, Deshpande, Javed, Shaikh, Ganesh, Chaure, Ravindra R, Pal, Santosh, Parkale, Sachin, Suravase, Smita, Bhoskar, Rajesh V, Gupta, Anil, Kalia, Rajesh, Yeshodharan, Mahammad, Azhar, Jagadeesh, Daler, Vinod, Mali, Geetika, Sharma, Amitesh, Kishore, Rupali, Vyawahare, Gautam, Agarwal, Himani, Pareek, Sagar, Budhe, Arun, Nayak, Dnyaneshwar, Warude, Praveen Kumar, Gupta, Parag, Joshi, Sneha, Joshi, Sagar, Darekar, Dilip, Pandey, Akshaya, Wagh, Prashant B, Nigade, Maneesh, Mehta, Vinod, Patil, Dipak, Modi, Shashikant, Pawar, Mahip, Verma, Minakshi, Singh, Sudipto, Das, Jayasagar, Gundu, Kumar, Nemmani, Mark G, Bock, Sharad, Sharma, Dhananjay, Bakhle, Rajender Kumar, Kamboj, Venkata P, Palle
Publikováno v:
Journal of medicinal chemistry. 63(11)
Voltage-gated sodium channel Na
Autor:
Dominik Feuerbach, Xuechun Zhang, Karin Briner, Charles R. Yang, Mark G. Bock, Bharat Lagu, Yves Auberson, Troxler Thomas J, Wang Tielin, Mark Perrone
Publikováno v:
ChemMedChem. 14:1226-1226
Autor:
Douglas J. Pettibone, Mark G. Bock, Scott D. Kuduk, Cuyue Tang, Thomayant Prueksaritanont, Kathy L. Murphy, Richard W. Ransom, Samson M. Jolly, Duane R. Reiss, Neville J. Anthony, Vera Bodmer-Narkevitch, Victoria Cofre
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7011-7014
A new class of indazole-derived bradykinin B1 antagonists and their structure–activity relationships (SAR) is reported. A number of compounds were found to have low-nanomolar affinity for the human B1 receptor and possess acceptable P-gp and pharma
Autor:
Duane R. Reiss, Ronald K. Chang, Scott D. Kuduk, Kathy L. Murphy, Douglas J. Pettibone, Thomayant Prueksaritanont, Robert M. DiPardo, Cuyue Tang, Mark G. Bock, Christina N. Di Marco, Richard W. Ransom
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5107-5110
A series of carbo- and heterocyclic α-hydroxy amide-derived bradykinin B1 antagonists was prepared and evaluated. A 4,4-difluorocyclohexyl α-hydroxy amide was incorporated along with a 2-methyl tetrazole in lieu of an oxadiazole to afford a suitabl
Autor:
Christina N. Di Marco, Frédéric Poignant, Yuhsin Kuo, Kristie Strong-Basalyga, Roy Eisenhandler, Conrad E. Raab, Thomayant Prueksaritanont, Nathan X. Yu, Edward J. Carlini, Alisha Norcross, Karen Richards, Tom Rushmore, Stacey L. Polsky-Fisher, Mark G. Bock, Bennett Ma, Clay B. Frederick, Brian A. Carr, Cuyue Tang, Scott D. Kuduk
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 325:935-946
After oral treatment (once daily) for 4 weeks with the potent bradykinin B(1) receptor antagonist methyl 3-chloro-3'-fluoro-4'-{(1R)-1-[({1-[(trifluoroacetyl)amino]cyclopropyl}carbonyl)-amino]ethyl}-1,1'-biphenyl-2-carboxylate (MK-0686), rhesus monke
Autor:
Jacquelynn J. Cook, Rodney A. Bednar, Thomayant Prueksaritanont, Yvonne M. Leonard, Michael R. Wood, Qin Mei, Richard W. Ransom, Ronald K. Chang, Emily D. Adarayn, Robert M. DiPardo, Jian Yu, Audrey A. Wallace, Wei Lemaire, Scott D. Kuduk, Kathy L. Murphy, G. R. Sitko, Scott D. Mosser, Christina N. Di Marco, Mark G. Bock, Frank C. Clayton, Bang-Lin Wan, Kathy M. Schirripa, Marie A. Holahan, Roger M. Freidinger, Dennis L. Bohn, Douglas J. Pettibone, Raymond S.L. Chang, Cuyue Tang, June J. Kim
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:716-720
Antagonism of the bradykinin B1 receptor represents a potential treatment for chronic pain and inflammation. Novel antagonists incorporating α-hydroxy amides were designed that display low-nanomolar affinity for the human bradykinin B1 receptor and
Autor:
J. Fred Hess, Kathy M. Schirripa, Robert M. DiPardo, Christina N. Di Marco, Kathy L. Murphy, C. Meacham Harrell, Nova Sain, Jenny Wai, Marie A. Holahan, Douglas J. Pettibone, Ronald K. Chang, Mark G. Bock, Richard W. Ransom, June J. Kim, Jacquelynn J. Cook, Duane R. Reiss, Mark O. Urban, Cuyue Tang, Scott D. Kuduk, Thomayant Prueksaritanont, Michael R. Wood
Publikováno v:
Journal of Medicinal Chemistry. 50:272-282
A series of biphenylaminocyclopropane carboxamide based bradykinin B1 receptor antagonists has been developed that possesses good pharmacokinetic properties and is CNS penetrant. Discovery that the replacement of the trifluoropropionamide in the lead
Autor:
J. Fred Hess, Kathryn L. Murphy, Mark G. Bock, Rick W. Ransom, Dai-Shi Su, Douglas J. Pettibone, Tsing-Bau Chen, R. S. L. Chang, Sookhee Ha, Pat J. Hey
Publikováno v:
Biochemistry. 45:14355-14361
We report the critical residues for the interaction of the kinins with human bradykinin receptor 1 (B1) using site-directed mutagenesis in conjunction with molecular modeling of the binding modes of the kinins in the homology model of the B1 receptor