To help you keep up with the latest biotech industry developments, we've curated a list of outstanding 2024 journal articles that have generated substantial industry interest, as well as impactful articles recently cited in patents.

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Groundbreaking discoveries are often built upon layers of scientific research published in high-quality peer-reviewed journals. To keep you abreast of the latest biotech industry developments, we curated a list of outstanding journal articles that have generated substantial interest from industry researchers in biotech this year, along with a list of impactful articles cited in patents shortly after their publication.

Most read journal articles among top biotech companies in 2024

NMR Chemical Shifts of Trace Impurities: Industrially Preferred Solvents Used in Process and Green Chemistry (OA)
Nicholas R. Babij, Elizabeth O. McCusker, Gregory T. Whiteker*, Belgin Canturk, Nakyen Choy, Lawrence C. Creemer, Carl V. De Amicis, Nicole M. Hewlett, Peter L. Johnson, James A. Knobelsdorf, Fangzheng Li, Beth A. Lorsbach, Benjamin M. Nugent, Sarah J. Ryan, Michelle R. Smith, and Qiang Yang
DOI: 10.1021/acs.oprd.5b00417

Beyond Rule of Five and PROTACs in Modern Drug Discovery: Polarity Reducers, Chameleonicity, and the Evolving Physicochemical Landscape
Edward Price*, Manuel Weinheimer, Alexey Rivkin, Gary Jenkins, Marjoleen Nijsen, Philip B. Cox, and David DeGoey
DOI: 10.1021/acs.jmedchem.3c02332

Development of Orally Bioavailable Peptides Targeting an Intracellular Protein: From a Hit to a Clinical KRAS Inhibitor
Mikimasa Tanada*, Minoru Tamiya, Atsushi Matsuo, Aya Chiyoda, Koji Takano, Toshiya Ito, Machiko Irie, Tomoya Kotake, Ryuuichi Takeyama, Hatsuo Kawada, Ryuji Hayashi, Shiho Ishikawa, Kenichi Nomura, Noriyuki Furuichi, Yuya Morita, Mirai Kage, Satoshi Hashimoto, Keiji Nii, Hitoshi Sase, Kazuhiro Ohara, Atsushi Ohta, Shino Kuramoto, Yoshikazu Nishimura, Hitoshi Iikura*, and Takuya Shiraishi*
DOI: 10.1021/jacs.3c03886

Validation of a New Methodology to Create Oral Drugs beyond the Rule of 5 for Intracellular Tough Targets
Atsushi Ohta*, Mikimasa Tanada, Shojiro Shinohara, Yuya Morita, Kazuhiko Nakano, Yusuke Yamagishi, Ryusuke Takano, Shiori Kariyuki, Takeo Iida, Atsushi Matsuo, Kazuhisa Ozeki, Takashi Emura, Yuuji Sakurai, Koji Takano, Atsuko Higashida, Miki Kojima, Terushige Muraoka, Ryuuichi Takeyama, Tatsuya Kato, Kaori Kimura, Kotaro Ogawa, Kazuhiro Ohara, Shota Tanaka, Yasufumi Kikuchi, Nozomi Hisada, Ryuji Hayashi, Yoshikazu Nishimura, Kenichi Nomura, Tatsuhiko Tachibana, Machiko Irie, Hatsuo Kawada, Takuya Torizawa, Naoaki Murao, Tomoya Kotake, Masahiko Tanaka, Shiho Ishikawa, Taiji Miyake, Minoru Tamiya, Masako Arai, Aya Chiyoda, Sho Akai, Hitoshi Sase, Shino Kuramoto, Toshiya Ito, Takuya Shiraishi, Tetsuo Kojima, and Hitoshi Iikura*
DOI: 10.1021/jacs.3c07145

Transition-Metal-Free C–N Cross-Coupling Enabled by a Multifunctional Reagent
Patrick S. Fier* and Suhong Kim*
DOI: 10.1021/jacs.4c00871

MicroCycle: An Integrated and Automated Platform to Accelerate Drug Discovery
Cara E. Brocklehurst*, Eva Altmann, Corentin Bon, Holly Davis, David Dunstan, Peter Ertl, Carol Ginsburg-Moraff, Jonathan Grob, Daniel J. Gosling, Guillaume Lapointe, Alexander N. Marziale, Heinrich Mues, Marco Palmieri, Sophie Racine, Richard I. Robinson, Clayton Springer, Kian Tan, William Ulmer, and René Wyler
DOI: 10.1021/acs.jmedchem.3c02029

Balanced Permeability Index: A Multiparameter Index for Improved In Vitro Permeability
Dahlia R. Weiss, Javier L. Baylon, Ethan D. Evans, Anthony Paiva, Gerry Everlof, Jingfang Cutrone, and Fabio Broccatelli*
DOI: 10.1021/acsmedchemlett.3c00542

Late-Stage Saturation of Drug Molecules (OA)
De-Hai Liu, Philipp M. Pflüger, Andrew Outlaw, Lukas Lückemeier, Fuhao Zhang, Clinton Regan, Hamid Rashidi Nodeh, Tim Cernak*, Jiajia Ma*, and Frank Glorius*
DOI: 10.1021/jacs.4c00807

Formation of N-Nitrosamine Drug Substance Related Impurities in Medicines: A Regulatory Perspective on Risk Factors and Mitigation Strategies (OA)
Răzvan C. Cioc, Ciarán Joyce, Monika Mayr, and Robert N. Bream*
DOI: 10.1021/acs.oprd.3c00153

Emerging and Re-emerging Warheads for Targeted Covalent Inhibitors: An Update
Laura Hillebrand, Xiaojun Julia Liang, Ricardo A. M. Serafim, and Matthias Gehringer*
DOI: 10.1021/acs.jmedchem.3c01825

Discovery and Preclinical Pharmacology of NX-2127, an Orally Bioavailable Degrader of Bruton’s Tyrosine Kinase with Immunomodulatory Activity for the Treatment of Patients with B Cell Malignancies
Daniel W. Robbins, Mark A. Noviski, Ying Siow Tan, Zef A. Konst, Aileen Kelly, Paul Auger, Nivetha Brathaban, Robert Cass, Ming Liang Chan, Ganesh Cherala, Matthew C. Clifton, Stefan Gajewski, Timothy G. Ingallinera, Dane Karr, Daisuke Kato, Jun Ma, Jenny McKinnell, Joel McIntosh, Jeff Mihalic, Brent Murphy, Jaipal Reddy Panga, Ge Peng, Janine Powers, Luz Perez, Ryan Rountree, Austin Tenn-McClellan, Arthur T. Sands, Dahlia R. Weiss, Jeffrey Wu, Jordan Ye, Cristiana Guiducci, Gwenn Hansen, and Frederick Cohen*
DOI: 10.1021/acs.jmedchem.3c01007

Synthetic Approaches to the New Drugs Approved During 2022
Scott P. France, Erick A. Lindsey, Emma L. McInturff*, Simon Berritt, Daniel W. Carney, Jacob C. DeForest, Sarah J. Fink, Andrew C. Flick, Tony S. Gibson, Kaitlyn Gray, Amber M. Johnson, Carolyn A. Leverett, Yiyang Liu, Subham Mahapatra, and Rebecca B. Watson
DOI: 10.1021/acs.jmedchem.3c02374

Discovery of Potent, Orally Bioavailable, Tricyclic NLRP3 Inhibitors
Lushun Wang, Monica J. Bohmer, Jinhua Wang, Flore Nardella, Jaeson Calla, Mariana Laureano De Souza, Kyra A. Schindler, Lukas Montejo, Nimisha Mittal, Frances Rocamora, Mayland Treat, Jordan T. Charlton, Patrick K. Tumwebaze, Philip J. Rosenthal, Roland A. Cooper, Ratna Chakrabarti, Elizabeth A. Winzeler*, Debopam Chakrabarti*, and Nathanael S. Gray*
DOI: 10.1021/acs.jmedchem.3c02098

Recently published journal articles cited in patents

TCFH–NMI: Direct Access to N-Acyl Imidazoliums for Challenging Amide Bond Formations (OA)
Gregory L. Beutner*, Ian S. Young, Merrill L. Davies, Matthew R. Hickey, Hyunsoo Park, Jason M. Stevens, and Qingmei Ye
DOI: 10.1021/acs.orglett.8b01591

Amide Bond Bioisosteres: Strategies, Synthesis, and Successes
Shikha Kumari, Angelica V. Carmona, Amit K. Tiwari, and Paul C. Trippier*
DOI: 10.1021/acs.jmedchem.0c00530

An Organic Chemist’s Guide to N-Nitrosamines: Their Structure, Reactivity, and Role as Contaminants (OA)
Jessica C. Beard and Timothy M. Swager*
DOI: 10.1021/acs.joc.0c02774

Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα
Emily J. Hanan*, Marie-Gabrielle Braun, Robert A. Heald, Calum MacLeod, Connie Chan, Saundra Clausen, Kyle A. Edgar, Charles Eigenbrot, Richard Elliott, Nicholas Endres, Lori S. Friedman, Emily Gogol, Xiao-Hui Gu, Rebecca Hong Thibodeau, Philip S. Jackson, James R. Kiefer, Jamie D. Knight, Michelle Nannini, Raman Narukulla, Amanda Pace, Jodie Pang, Hans E. Purkey, Laurent Salphati, Deepak Sampath, Stephen Schmidt, Steve Sideris, Kyung Song, Swathi Sujatha-Bhaskar, Mark Ultsch, Heidi Wallweber, Jianfeng Xin, SiewKuen Yeap, Amy Young, Yu Zhong, and Steven T. Staben
DOI: 10.1021/acs.jmedchem.2c01422

Bioisosteres of the Phenyl Ring: Recent Strategic Applications in Lead Optimization and Drug Design
Murugaiah A. M. Subbaiah* and Nicholas A. Meanwell
DOI: 10.1021/acs.jmedchem.1c01215

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