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2. Novel advances in biotransformation and bioactivation research – 2020 year in review

Author

Khojasteh, S Cyrus, Argikar, Upendra A, Driscoll, James P, Heck, Carley JS, King, Lloyd, Jackson, Klarissa D, Jian, Wenying, Kalgutkar, Amit S, Miller, Grover P, Kramlinger, Valerie, Rietjens, Ivonne MCM, Teitelbaum, Aaron M, Wang, Kai, Wei, Cong, Johnson, Benjamin M, Shu, Yue-Zhong, Zhuo, Xiaoliang, Meanwell, Nicholas A, Cerny, Matthew A, Obach, R Scott, Sharma, Raman, Spracklin, Douglas K, Walker, Gregory S, Goracci, Laura, Desantis, Jenny, Valeri, Aurora, Castellani, Beatrice, Eleuteri, Michela, Cruciani, Gabriele, Lall, Manjinder S, Bassyouni, Asser, Bradow, James, Brown, Maria, Bundesmann, Mark, Chen, Jinshan, Ciszewski, Gregory, Hagen, Anne E, Hyek, Dennis, Jenkinson, Stephen, Liu, Bo, Pan, Senliang, Reilly, Usa, Sach, Neal, Smaltz, Daniel J, Starr, Jeremy, Wagenaar, Melissa, de Bruyn Kops, Christina, Sicho, Martin, Mazzolari, Angelica, Kirchmair, Johannes, Korprasertthaworn, Porntipa, Chau, Nuy, Nair, Pramod C, Rowland, Andrew, Miners, John O, Wrobleski, Stephen T, Moslin, Ryan, Lin, Shuqun, Zhang, Yanlei, Spergel, Steven, Kempson, James, Tokarski, John S, Strnad, Joann, Zupa-Fernandez, Adriana, Cheng, Lihong, Shuster, David, Gillooly, Kathleen, Yang, Xiaoxia, Heimrich, Elizabeth, McIntyre, Kim W, Chaudhry, Charu, Khan, Javed, Ruzanov, Max, Tredup, Jeffrey, Mulligan, Dawn, Xie, Dianlin, Sun, Huadong, Huang, Christine, D'Arienzo, Celia, Aranibar, Nelly, Chiney, Manoj, Chimalakonda, Anjaneya, Pitts, William J, Lombardo, Louis, Carter, Percy H, Burke, James R, Weinstein, David S, Li, Jing, Liu, Ju, Enders, Jennifer, Arciprete, Michael, Tran, Chris, Aluri, Krishna, Guan, Li-Hua, O'Shea, Jonathan, Bisbe, Anna, Charisse, Klaus, Zlatev, Ivan, Najarian, Diana, Xu, Yuanxin, Kim, Jaeah, El Zahar, Noha M, Bartlett, Michael G, Katyayan, Kishore, Yi, Ping, Monk, Scott, Cassidy, Kenneth, Takahashi, Ryan H, Grandner, Jessica M, Bobba, Sudheer, Liu, Yanzhou, Beroza, Paul, Zhang, Donglu, Ma, Shuguang, Post, Noah, Yu, Rosie, Greenlee, Sarah, Gaus, Hans, Hurh, Eunju, Matson, John, Wang, Yanfeng, Tajima, Yuya, Toyoda, Takeshi, Hirayama, Yuichiro, Matsushita, Kohei, Yamada, Takanori, Ogawa, Kumiko, Watanabe, Kenji, Takamura-Enya, Takeji, Totsuka, Yukari, Wakabayashi, Keiji, Miyoshi, Noriyuki, Zhang, Jiayin, Chan, Chi-Kong, Ham, Yat-Hing, Chan, Wan, Schleiff, Mary Alexandra, Flynn, Noah R, Payakachat, Sasin, Schleiff, Benjamin Mark, Pinson, Anna O, Province, Dennis W, Swamidass, S Joshua, Boysen, Gunnar, Nardone-White, Dasean T, Bissada, Jennifer E, Abouda, Arsany A, Zhang, Zhuming, Connolly, Peter J, Lim, Heng Keang, Pande, Vineet, Meerpoel, Lieven, Teleha, Christopher, Branch, Jonathan R, Ondrus, Janine, Hickson, Ian, Bush, Tammy, Luistro, Leopoldo, Packman, Kathryn, Bischoff, James R, Ibrahim, Salam, Parrett, Christopher, Chong, Yolanda, Gottardis, Marco M, Bignan, Gilles, Mulder, Teresa, Bobba, Sudder, Johnson, Kevin M, Wang, Wei, Zhang, Chenghong, Cai, Jingwei, Choo, Edna F, Crawford, James J, Landry, Matthew L, Chen, Huifen, Kenny, Jane R, Lee, Wendy, Young, Wendy B, Geib, Timon, Thulasingam, Madhuranayaki, Haeggstrom, Jesper Z, Sleno, Lekha, Monroe, James J, Tanis, Keith Q, Podtelezhnikov, Alexei A, Nguyen, Truyen, Machotka, Sam V, Lynch, Donna, Evers, Raymond, Palamanda, Jairam, Miller, Randy R, Pippert, Todd, Cabalu, Tamara D, Johnson, Timothy E, Aslamkhan, Amy G, Kang, Wen, Tamburino, Alex M, Mitra, Kaushik, Agrawal, Nancy GB, and Sistare, Frank D

Subjects
METABOLISM, Toxicology, 030226 pharmacology & pharmacy, 03 medical and health sciences, nonp450 enzymes, 0302 clinical medicine, p450 enzymes, Biotransformation, INTRINSIC CLEARANCE, Political science, MASS-BALANCE, Humans, Pharmacology (medical), Pharmacology & Pharmacy, P450 Enzymes, General Pharmacology, Toxicology and Pharmaceutics, ANTISENSE OLIGONUCLEOTIDE, Toxicologie, VLAG, ARISTOLOCHIC ACID, Drug metabolism, Science & Technology, WIMEK, bioactivation, IDENTIFICATION, Year in review, IN-VITRO, NONHEPATOTOXIC DRUGS, Drug metabolizing enzymes, Drug development, 030220 oncology & carcinogenesis, COVALENT BINDING DATA, Engineering ethics, biotransformation, LIVER-MICROSOMES, Life Sciences & Biomedicine
Abstract

This annual review is the sixth of its kind since 2016 (see references). Our objective is to explore and share articles which we deem influential and significant in the field of biotransformation and bioactivation. These fields are constantly evolving with new molecular structures and discoveries of corresponding pathways for metabolism that impact relevant drug development with respect to efficacy and safety. Based on the selected articles, we created three sections: (1) drug design, (2) metabolites and drug metabolizing enzymes, and (3) bioactivation and safety (Table 1). Unlike in years past, more biotransformation experts have joined and contributed to this effort while striving to maintain a balance of authors from academic and industry settings.[Table: see text]. ispartof: DRUG METABOLISM REVIEWS vol:53 issue:3 pages:384-433 ispartof: location:England status: published

Published
2021

4. Late-Stage Lead Diversification Coupled with Quantitative Nuclear Magnetic Resonance Spectroscopy to Identify New Structure–Activity Relationship Vectors at Nanomole-Scale Synthesis: Application to Loratadine, a Human Histamine H1 Receptor Inverse Agonist

Author

Lall, Manjinder S., primary, Bassyouni, Asser, additional, Bradow, James, additional, Brown, Maria, additional, Bundesmann, Mark, additional, Chen, Jinshan, additional, Ciszewski, Gregory, additional, Hagen, Anne E., additional, Hyek, Dennis, additional, Jenkinson, Stephen, additional, Liu, Bo, additional, Obach, R. Scott, additional, Pan, Senliang, additional, Reilly, Usa, additional, Sach, Neal, additional, Smaltz, Daniel J., additional, Spracklin, Douglas K., additional, Starr, Jeremy, additional, Wagenaar, Melissa, additional, and Walker, Gregory S., additional

Published
2020
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5. Late-Stage Lead Diversification Coupled with Quantitative Nuclear Magnetic Resonance Spectroscopy to Identify New Structure–Activity Relationship Vectors at Nanomole-Scale Synthesis: Application to Loratadine, a Human Histamine H1...

Author

Lall, Manjinder S., Bassyouni, Asser, Bradow, James, Brown, Maria, Bundesmann, Mark, Chen, Jinshan, Ciszewski, Gregory, Hagen, Anne E., Hyek, Dennis, Jenkinson, Stephen, Liu, Bo, Obach, R. Scott, Pan, Senliang, Reilly, Usa, Sach, Neal, Smaltz, Daniel J., Spracklin, Douglas K., Starr, Jeremy, Wagenaar, Melissa, and Walker, Gregory S.

Published
2020
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7. Strain-Release Heteroatom Functionalization: Development, Scope, and Stereospecificity

Author

Lopchuk, Justin M., primary, Fjelbye, Kasper, additional, Kawamata, Yu, additional, Malins, Lara R., additional, Pan, Chung-Mao, additional, Gianatassio, Ryan, additional, Wang, Jie, additional, Prieto, Liher, additional, Bradow, James, additional, Brandt, Thomas A., additional, Collins, Michael R., additional, Elleraas, Jeff, additional, Ewanicki, Jason, additional, Farrell, William, additional, Fadeyi, Olugbeminiyi O., additional, Gallego, Gary M., additional, Mousseau, James J., additional, Oliver, Robert, additional, Sach, Neal W., additional, Smith, Jason K., additional, Spangler, Jillian E., additional, Zhu, Huichin, additional, Zhu, Jinjiang, additional, and Baran, Phil S., additional

Published
2017
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8. Late-Stage Lead Diversification Coupled with Quantitative Nuclear Magnetic Resonance Spectroscopy to Identify New Structure–Activity Relationship Vectors at Nanomole-Scale Synthesis: Application to Loratadine, a Human Histamine H1Receptor Inverse Agonist

Author

Lall, Manjinder S., Bassyouni, Asser, Bradow, James, Brown, Maria, Bundesmann, Mark, Chen, Jinshan, Ciszewski, Gregory, Hagen, Anne E., Hyek, Dennis, Jenkinson, Stephen, Liu, Bo, Obach, R. Scott, Pan, Senliang, Reilly, Usa, Sach, Neal, Smaltz, Daniel J., Spracklin, Douglas K., Starr, Jeremy, Wagenaar, Melissa, and Walker, Gregory S.

Abstract

An experimental approach is described for late-stage lead diversification of frontrunner drug candidates using nanomole-scale amounts of lead compounds for structure–activity relationship development. The process utilizes C–H bond activation methods to explore chemical space by transforming candidates into newly functionalized leads. A key to success is the utilization of microcryoprobe nuclear magnetic resonance (NMR) spectroscopy, which permits the use of low amounts of lead compounds (1–5 μmol). The approach delivers multiple analogues from a single lead at nanomole-scale amounts as DMSO-d6stock solutions with a known structure and concentration for in vitropharmacology and absorption, distribution, metabolism, and excretion testing. To demonstrate the feasibility of this approach, we have used the antihistamine agent loratadine (1). Twenty-six analogues of loratadine were isolated and fully characterized by NMR. Informative SAR analogues were identified, which display potent affinity for the human histamine H1receptor and improved metabolic stability.

Published
2020
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12. Accounting for deferred charges - Is more guidance needed?

Author

Bradow, James R.

Subjects
Cost accounting -- Standards, Financial statements -- Methods, Assets (Accounting) -- Valuation, Accounting -- Standards, Banking, finance and accounting industries, Business, Business, general, Financial Accounting Standards Board -- Standards
Abstract

The Financial Accounting Standards Board needs to provide more specific guidance in the area of accounting for deferred charges. The present standards, stipulated in Statement of Financial Accounting Concepts No. 6, are too vague to consistently determine whether an incurred cost meets the definition of an asset. Two types of uncertainty prevent costs from being shown as assets: uncertainty about whether an asset exists, and uncertainty about determining the value of the asset.

Published
1987

15. Late-Stage Lead Diversification Coupled with Quantitative Nuclear Magnetic Resonance Spectroscopy to Identify New Structure-Activity Relationship Vectors at Nanomole-Scale Synthesis: Application to Loratadine, a Human Histamine H 1 Receptor Inverse Agonist.

Author

Lall MS, Bassyouni A, Bradow J, Brown M, Bundesmann M, Chen J, Ciszewski G, Hagen AE, Hyek D, Jenkinson S, Liu B, Obach RS, Pan S, Reilly U, Sach N, Smaltz DJ, Spracklin DK, Starr J, Wagenaar M, and Walker GS

Subjects
Animals, Chromatography, High Pressure Liquid, Cytochrome P-450 Enzyme System genetics, Cytochrome P-450 Enzyme System metabolism, Dimethyl Sulfoxide chemistry, Dogs, Drug Discovery methods, Histamine H1 Antagonists, Non-Sedating chemistry, Histamine H1 Antagonists, Non-Sedating pharmacology, Humans, Hydrogen Bonding, Inactivation, Metabolic, Loratadine chemistry, Magnetic Resonance Spectroscopy, Metalloporphyrins chemistry, Metalloporphyrins metabolism, Microsomes, Liver drug effects, Microsomes, Liver metabolism, Rabbits, Recombinant Proteins genetics, Recombinant Proteins metabolism, Tandem Mass Spectrometry, Tissue Distribution, Loratadine analogs & derivatives, Loratadine pharmacokinetics, Structure-Activity Relationship
Abstract

An experimental approach is described for late-stage lead diversification of frontrunner drug candidates using nanomole-scale amounts of lead compounds for structure-activity relationship development. The process utilizes C-H bond activation methods to explore chemical space by transforming candidates into newly functionalized leads. A key to success is the utilization of microcryoprobe nuclear magnetic resonance (NMR) spectroscopy, which permits the use of low amounts of lead compounds (1-5 μmol). The approach delivers multiple analogues from a single lead at nanomole-scale amounts as DMSO- d 6 stock solutions with a known structure and concentration for in vitro pharmacology and absorption, distribution, metabolism, and excretion testing. To demonstrate the feasibility of this approach, we have used the antihistamine agent loratadine ( 1 ). Twenty-six analogues of loratadine were isolated and fully characterized by NMR. Informative SAR analogues were identified, which display potent affinity for the human histamine H 1 receptor and improved metabolic stability.

Published
2020
Full Text
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