Results 91 to 100 of about 10,733 (194)

In Vitro Drug Metabolism by Human Carboxylesterase 1: Focus on Angiotensin-Converting Enzyme Inhibitors [PDF]

, 2020
Carboxylesterase 1 (CES1) is the major hydrolase in human liver. The enzyme is involved in the metabolism of several important therapeutic agents, drugs of abuse, and endogenous compounds.
Kristian Linnet, Ragnar Thomsen, Henrik B Rasmussen   +2 more
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Abstract 2575: Activation of antibody drug conjugate MDX-1203 by human carboxylesterase [PDF]

, 2010
MDX-1203 is a human anti-CD70 antibody conjugated to a DNA alkylating cytotoxic Drug A. Drug A is an enzyme-activated prodrug that requires cleavage of its peptide linker and removal of an ester-linked protecting group for cytotoxic activity.
Tim Chen, Bilal Sufi, Allen Zhang, Janette Sung, Sanjeev Gangwar, David Passmore, Brian Lee, Charlie Cong, Adam Salles, Vangipuram S. Rangan, Shrikant Deshpande, Chetana Rao, Alice Stevens, Daniel Tengco, Mary Huber, Barbara Aguilar, Dan Derwin   +16 more
core   +1 more source

Two CES1 Gene Mutations Lead to Dysfunctional Carboxylesterase 1 Activity in Man: Clinical Significance and Molecular Basis [PDF]

, 2008
The human carboxylesterase 1 (CES1) gene encodes for the enzyme carboxylesterase 1, a serine esterase governing both metabolic deactivation and activation of numerous therapeutic agents.
Wang, Jun-Sheng, Youngblood, Geri L., Johnson, Julie A., Malcolm, Robert, Markowitz, John S., Patrick, Kennerly S., Langaee, Taimour Y., DeVane, C. Lindsay, Sweet, Douglas H., Zhu, Hao-Jie, Donovan, Jennifer L., Yuan, Hong-Jie   +11 more
core   +1 more source

In silico prediction of human carboxylesterase-1 (hCES1) metabolism combining docking analyses and MD simulations [PDF]

, 2010
Metabolic problems lead to numerous failures during clinical trials, and much effort is now devoted in developing in silico models predicting metabolic stability and metabolites.
G. Vistoli, A. Pedretti, Vistoli, G., Pedretti, A., Mazzolari, A., A. Mazzolari, Testa, B., B. Testa   +7 more
core   +1 more source

Dammarenediol II enhances etoposide‐induced apoptosis by targeting O‐GlcNAc transferase and Akt/GSK3β/mTOR signaling in liver cancer

Molecular Oncology, Volume 20, Issue 6, Page 1591-1611, June 2026.
Etoposide induces DNA damage, activating p53‐dependent apoptosis via caspase‐3/7, which cleaves PARP1. Dammarenediol II enhances this apoptotic pathway by suppressing O‐GlcNAc transferase activity, further decreasing O‐GlcNAcylation. The reduction in O‐GlcNAc levels boosts p53‐driven apoptosis and influences the Akt/GSK3β/mTOR signaling pathway ...
Jaehoon Lee, Byung‐Cheol Han, Gi‐Bang Koo, Jihye Park, Mijin Kwon, Young Bin Park, Jae‐Mun Choi, Seung‐Ho Lee, Sangho Roh   +8 more
wiley   +1 more source

Insights into human carboxylesterase 2 stability and activity in vivo and in vitro [PDF]

, 2012
Dissertation to obtain a Master Degree in BiotechnologyDue to its role in ester containing xenobiotics metabolization, such as the activation of pro-drugs, carboxylesterase 2 (CES2) has become an attractive enzyme, with potential applications in the ...
Ferreira, Pedro Garcia
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Understanding and Overcoming Antibody‐Drug Conjugate Resistance: Biological Mechanisms and Emerging Analytical Frameworks in Breast Cancer

Advanced Science, Volume 13, Issue 35, 24 June 2026.
Antibody–drug conjugates (ADCs) transform breast cancer therapy, yet resistance limits their durability. Emerging evidence reveals that ADC failure is not solely tumor‐intrinsic but shaped by dynamic tumor–microenvironment interactions that alter drug delivery, processing, and response.
Minji Seo, Jangsoon Lee, Naoto T. Ueno
wiley   +1 more source

Development and preclinical testing of a naloxone prodrug depot for extended protection against opioid overdose

Nature Communications
The opioid crisis, driven by synthetic opioids like fentanyl, demands innovative solutions. The opioid antidote naloxone has a short action ( ~ 1 hour), requiring repeated doses.
Hala Aldawod, Arjun D. Patel, Rasha Emara, Dengpan Liang, Joshua S. Ho, Toufiq Ul Amin, Md Tariqul Haque Tuhin, Abdulmalek Balgoname, Avishan Kiani, Jumana M. Ajlouny, Melanie A. Felmlee, Miki S. Park, Bhaskara R. Jasti, William K. Chan, James A. Uchizono, Mamoun M. Alhamadsheh   +15 more
doaj   +1 more source

Molecular Profiling of Genes Associated With Methylphenidate Pathway Therapy and Discovery of New Variants in Amazonian Amerindian Populations

American Journal of Medical Genetics Part B: Neuropsychiatric Genetics, Volume 201, Issue 4, Page 291-299, June 2026.
ABSTRACT In Attention Deficit Hyperactivity Disorder (ADHD), methylphenidate is one of the most widely used drugs, in which patient response significantly impacts prognosis. This study aimed to characterize the molecular profile of 10 genes associated with methylphenidate therapy.
Aline Pasquini Santos, Tatiane Carinta de Souza, Kaio Evandro Cardoso Aguiar, Ana Caroline Alves da Costa, Natasha Monte, Juliana Carla Gomes Rodrigues, Giovanna Gilioli da Costa Nunes, Rita de Cássia Calderaro Coelho, Ândrea Ribeiro‐dos‐Santos, André Maurício Ribeiro dos Santos, Sandro José de Souza, Sidney Emanuel Batista dos Santos, Rommel Mario Rodriguez Burbano, Marianne Rodrigues Fernandes, Ney Pereira Carneiro dos Santos   +14 more
wiley   +1 more source

Human salivary esterases : a biochemical study of carboxylesterase and thio-esterase in human saliva with special reference to their inhibition by dental materials [PDF]

, 1980
Electrophoretic and gel chromatographic techniques have been developed in order to obtain partially purified esterases from small amounts of human saliva. These techniques permit the characterization of salivary esterase regarding substrate and inhibitor
Lindqvist, Lennart,
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