Article
Chemistry, Medicinal
Guanglin Luo, Xiang-Jun Jiang, Ling Chen, Charles M. Conway, Michael Gulianello, Walter Kostich, Deborah Keavy, Laura J. Signor, Ping Chen, Carl Davis, Valerie J. Whiterock, Richard Schartman, Kimberly A. Widmann, John E. Macor, Gene M. Dubowchik
Summary: Researchers identified a series of high-affinity heterocycle derivatives as CGRP receptor antagonists, some of which showed good oral exposure and reduced time-dependent CYP3A4 inhibition. However, challenges remained in improving the oral bioavailability of these compounds.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Medicine, General & Internal
Jessica Ailani, Richard B. Lipton, Peter J. Goadsby, Hua Guo, Rosa Miceli, Lawrence Severt, Michelle Finnegan, Joel M. Trugman
Summary: Oral atogepant once daily was effective in reducing the number of migraine days and headache days over a period of 12 weeks, but may cause adverse events such as constipation and nausea. Longer and larger trials are needed to determine the effect and safety of atogepant for migraine prevention.
NEW ENGLAND JOURNAL OF MEDICINE
(2021)
Review
Medicine, General & Internal
Matilde Capi, Valerio De Angelis, Donatella De Bernardini, Ottavia De Luca, Fabiola Cipolla, Luana Lionetto, Maurizio Simmaco, Paolo Martelletti
Summary: The discovery of CGRP's role in migraine pathophysiology has led to the development of new drugs, showing potential to transform migraine management, although its exact position is yet to be determined.
JOURNAL OF CLINICAL MEDICINE
(2021)
Article
Multidisciplinary Sciences
Francesco De Logu, Romina Nassini, Alan Hegron, Lorenzo Landini, Dane D. Jensen, Rocco Latorre, Julia Ding, Matilde Marini, Daniel Souza Monteiro de Araujo, Paulina Ramirez-Garcia, Michael Whittaker, Jeffri Retamal, Mustafa Titiz, Alessandro Innocenti, Thomas P. Davis, Nicholas Veldhuis, Brian L. Schmidt, Nigel W. Bunnett, Pierangelo Geppetti
Summary: This study reveals that the CGRP-mediated neuronal/Schwann cell pathway mediates allodynia associated with neurogenic inflammation, contributing to the algesic action of CGRP in mice.
NATURE COMMUNICATIONS
(2022)
Review
Neurosciences
Chun-Pai Yang, Kuo-Ting Huang, Ching-Mao Chang, Cheng-Chia Yang, Shuu-Jiun Wang
Summary: This paper reviews the advances in new agents for acute therapy of migraine, including new formulations of sumatriptan, ditans, and CGRP receptor antagonists. These new drugs have expanded the options for migraine treatment and may change the treatment strategy for patients with migraine in the future.
Review
Physiology
Ambrish Kumar, Maelee Williamson, Andrew Hess, Donald J. DiPette, Jay D. Potts
Summary: Alpha-CGRP plays an important role in cardiovascular disease and migraines. Knock-out studies have shown that α-CGRP deficiency leads to higher mortality rates and cardiac damage in heart failure, while administration of α-CGRP improves cardiac function and protects the heart. In migraines, α-CGRP antagonists can reduce headache symptoms. Both agonists and antagonists of α-CGRP have clinical relevance in treating cardiovascular disease and migraine pain.
FRONTIERS IN PHYSIOLOGY
(2022)
Review
Medicine, General & Internal
Lars Edvinsson
Summary: Migraine is a common neurovascular disorder, affecting over 15% of the global population. Women are three times more likely to suffer from migraine compared to men. The underlying mechanisms of migraine are still largely unknown, but molecules such as CGRP play a crucial role in its pathophysiology.
JOURNAL OF INTERNAL MEDICINE
(2022)
Article
Clinical Neurology
J. Talbot, R. Stuckey, L. Crawford, S. Weatherby, S. Mullin
Summary: This study presented the outcomes of erenumab treatment in chronic migraine patients who had previously shown unsatisfactory response to onabotulinumtoxinA. The results showed significant improvements in pain, medication use, and quality of life over the 9-month treatment period.
JOURNAL OF HEADACHE AND PAIN
(2021)
Review
Biochemistry & Molecular Biology
Cinder Faith Cohen, Jueun Roh, Sang Hoon Lee, Chul-Kyu Park, Temugin Berta
Summary: Migraine is a neurovascular disorder affecting 12% of the global population. Research suggests that nociceptive neurons in the trigeminal ganglia play a crucial role in migraine pain signals. These neurons innervate the meninges and transmit pain signals to the thalamus. Targeting nociceptive neurons, which express transient receptor potential (TRP) channels, may be a promising approach for migraine treatment. This review discusses the role of nociceptive neurons, challenges with current drugs, and the potential of TRP channels, particularly TRPC4, as novel targets for migraine prevention and treatment.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Medicine, Research & Experimental
Dulanji K. Kuruppu, James M. North, Amy J. Kovacik, Yan Dong, Eric M. Pearlman, Susan L. Hutchinson
Summary: Galcanezumab demonstrates early onset of action, maintenance of effect, and gradual reduction of effect upon treatment cessation in both patients with episodic and chronic migraine.
ADVANCES IN THERAPY
(2021)
Review
Pharmacology & Pharmacy
Amber Lanae Martirosov, Christopher Giuliano, Macy Shupp, Sarah Channey, Pramodini B. Kale-Pradhan
Summary: This review examines the pharmacology, efficacy, and safety of intranasal zavegepant as an acute treatment for migraine with or without aura. The results show that zavegepant is more effective than placebo in relieving pain and symptoms, with a similar incidence of adverse effects. Zavegepant may be a convenient and useful treatment option for acute migraines.
ANNALS OF PHARMACOTHERAPY
(2023)
Article
Clinical Neurology
Francesca Puledda, Elisa Martins Silva, Kanokrat Suwanlaong, Peter J. Goadsby
Summary: Migraine is a common neurological disorder with complex neurobiology, affecting both central and peripheral nervous systems. Recent advancements in understanding its pathophysiology have led to the development of novel treatments, which are changing the clinical approach to the disease globally.
JOURNAL OF NEUROLOGY
(2023)
Review
Immunology
Sandhya Jinesh
Summary: Migraine is a common neurological disorder with a significant socio-economic impact. CGRP plays a key role in triggering migraines by causing vasodilation in extracerebral arteries. While there are various medications used for migraine prevention and treatment, targeted therapies are limited. CGRP receptor inhibitors have been developed as drugs for migraine therapy, and a risk-benefit comparison of different classes of these inhibitors is provided in this review article.
INFLAMMOPHARMACOLOGY
(2023)
Review
Pharmacology & Pharmacy
Jessica Barreto Ribeiro dos Santos, Michael Ruberson Ribeiro da Silva
Summary: This article reviews the chemistry, pharmacodynamics, pharmacokinetics, efficacy, safety, and tolerability profile of small molecule CGRP receptor antagonists for the preventive treatment of migraine. The study finds that atogepant and rimegepant are effective and safe for the preventive treatment of migraine in adults.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2022)
Article
Clinical Neurology
Justin L. Hoskin, Terry D. Fife
Summary: The CGRP medications appear to be a decent treatment option for vestibular migraine (VM), with most patients experiencing some level of symptom improvement.
FRONTIERS IN NEUROLOGY
(2022)
Article
Chemistry, Applied
Jeonghan Park, Jeffrey C. Moore, Feng Xu
ORGANIC PROCESS RESEARCH & DEVELOPMENT
(2016)
Article
Chemistry, Organic
Feng Xu, Yong-Li Zhong, Hongming Li, Ji Qi, Richard Desmond, Zhiguo J. Song, Jeonghan Park, Tao Wang, Matthew Truppo, Guy R. Humphrey, Rebecca T. Ruck
Article
Chemistry, Multidisciplinary
Feng Xu, Birgit Kosjek, Fabien L. Cabirol, Haibin Chen, Richard Desmond, Jeonghan Park, Anupam P. Gohel, Steven J. Collier, Derek J. Smith, Zhuqing Liu, Jacob M. Janey, John Y. L. Chung, Oscar Alvizo
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2018)
Article
Chemistry, Applied
Jianguo Yin, Mark Weisel, Yining Ji, Zhijian Liu, Jinchu Liu, Debra J. Wallace, Feng Xu, Benjamin D. Sherry, Nobuyoshi Yasuda
ORGANIC PROCESS RESEARCH & DEVELOPMENT
(2018)
Article
Chemistry, Medicinal
Tesfaye Biftu, Xiaoxia Qian, Ping Chen, Dennis Feng, Giovanna Scapin, Ying-Duo Gao, Jason Cox, Ranabir Sinha Roy, George Eiermann, Huabing He, Kathy Lyons, Gino Salituro, Sangita Patel, Alexander Petrov, Feng Xu, Shiyao Sherrie Xu, Bei Zhang, Charles Caldwell, Joseph K. Wu, Kathy Lyons, Ann E. Weber
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2013)
Article
Chemistry, Organic
Feng Xu, John Y. L. Chung, Jeffery C. Moore, Zhuqing Liu, Naoki Yoshikawa, R. Scott Hoerrner, Jaemoon Lee, Maksim Royzen, Ed Cleator, Andrew G. Gibson, Robert Dunn, Kevin M. Maloney, Mahbub Alam, Adrian Goodyear, Joseph Lynch, Nobuyashi Yasuda, Paul N. Devine
Article
Chemistry, Organic
Feng Xu, Michael J. Zacuto, Yoshinori Kohmura, Jon Rosen, Andrew Gibb, Mahbub Alam, Jeremy Scott, David Tschaen
Article
Chemistry, Applied
Naoki Yoshikawa, Feng Xu, Juan D. Arredondo, Takahiro Itoh
ORGANIC PROCESS RESEARCH & DEVELOPMENT
(2011)
Article
Chemistry, Organic
Feng Xu, Bryon Simmons, Tomoaki Maehara, Tohru Fukuyama
Article
Chemistry, Organic
Feng Xu, Jungchul Kim, Jacob Waldman, Tao Wang, Paul Devine
Article
Chemistry, Organic
John Y. L. Chung, Dongfang Meng, Michael Shevlin, Venugopal Gudipati, Qinghao Chen, Yizhou Liu, Yu-hong Lam, Aaron Dumas, Jeremy Scott, Qiang Tu, Feng Xu
JOURNAL OF ORGANIC CHEMISTRY
(2020)
Correction
Chemistry, Multidisciplinary
Karl B. Hansen, Yi Hsiao, Feng Xu, Nelo Rivera, Andrew Clausen, Michele Kubryk, Shane Krska, Thorsten Rosner, Bryon Simmons, Jaume Balsells, Nori Ikemoto, Yongkui Sun, Felix Spindler, Christophe Malan, Edward J. J. Grabowski, Joseph D. Armstrong
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2020)
Article
Chemistry, Applied
Jungchul Kim, Tetsuji Itoh, Feng Xu, Zachary E. X. Dance, Jacob H. Waldman, Debra J. Wallace, Feiyue Wu, Roman Kats-Kagan, Anil R. Ekkati, Andrew P. J. Brunskill, Feng Peng, Patrick S. Fier, Jennifer Obligacion, Benjamin D. Sherry, Zhijian Liu, Khateeta M. Emerson, Adam J. Fine, Anna Jenks, Marco Euclide Armenante
Summary: A robust manufacturing process has been developed for the synthesis of the potent beta-lactamase inhibitor relebactam, ensuring >99% purity with non-detectable levels of oligomers. The origin and control strategy of oligomer impurities formed during specific reaction steps have been thoroughly studied and addressed in the optimal manufacturing process.
ORGANIC PROCESS RESEARCH & DEVELOPMENT
(2021)
Article
Chemistry, Multidisciplinary
Tamas Benkovics, Feng Peng, Eric M. Phillips, Chihui An, Rachel S. Bade, Cheol K. Chung, Zachary E. X. Dance, Patrick S. Fier, Jacob H. Forstater, Zhijian Liu, Zhuqing Liu, Peter E. Maligres, Nicholas M. Marshall, Nastaran Salehi Marzijarani, John A. McIntosh, Steven P. Miller, Jeffrey C. Moore, Andrew J. Neel, Jennifer Obligacion, Weilan Pan, Michael T. Pirnot, Marc Poirier, Mikhail Reibarkh, Benjamin D. Sherry, Zhiguo Jake Song, Lushi Tan, Ben W. H. Turnbull, Deeptak Verma, Jacob H. Waldman, Lu Wang, Tao Wang, Matthew S. Winston, Feng Xu
Summary: As practitioners of organic chemistry strive to deliver efficient syntheses of complex natural products and drug candidates, enzyme-catalyzed reactions serve as a necessary and impressive tool. This article reports a highly selective synthesis of MK-1454 using enzyme-catalyzed cascade reactions to construct complex molecules.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2022)
Article
Chemistry, Applied
Andrew J. Neel, Zhuqing Liu, Tamas Benkovics, Lu Wang, Stephan M. Rummelt, Heather C. Johnson, Kevin M. Belyk, Feng Xu, Cheol K. Chung, David J. Lamberto, Ryan D. Cohen, Stephanus Axnanda, Zachary E. X. Dance
Summary: This study describes a novel synthetic approach to prepare 3 ' FG, involving aminocatalytic electrophilic fluorination and subsequent substrate-directed reduction. The key features of this method include the use of commercially available L-leucine amide as the fluorination catalyst, development of a highly stereoselective (>95:5) intramolecular hydride delivery, and the use of dispersive Raman spectroscopy to guide form control during crystallization.
ORGANIC PROCESS RESEARCH & DEVELOPMENT
(2023)