Results 111 to 120 of about 9,317 (205)

Advances in Therapeutic Antibody Discovery and Development Targeting G Protein‐Coupled Receptors

Pharmacology Research &Perspectives, Volume 14, Issue 1, February 2026.
ABSTRACT G protein‐coupled receptors (GPCRs) are integral to numerous biological processes and are associated with various diseases across all therapeutic areas. Consequently, GPCRs present substantial potential for antibody‐based therapies. This review offers an overview of the therapeutic GPCR‐antibody target landscape and examines the diversity ...
Catherine J. Hutchings, Serbülent Ünsal, Mathieu Rappas, Matthew Barnes, Maria Waldhoer, Ben Holland, Martin Culka   +6 more
wiley   +1 more source

Chemical Tuning Enhances Both Potency Toward Nrf2 and In Vitro Therapeutic Index of Triterpenoids [PDF]

, 2017
The transcription factor Nrf2 protects against a number of experimental pathologies, and is a promising therapeutic target. The clinical investigation of a potent Nrf2-inducing agent, the triterpenoid (TP) bardoxolone methyl (BARD), was recently halted ...
Copple, Ian M., Dinkova-Kostova, Albena T., Goldring, Christopher E., Honda, Tadashi, Kratschmar, Denise V., Lister, Adam, Odermatt, Alex, Park, B. Kevin, Shelton, Luke M., Walsh, Joanne   +9 more
core  

Characterizing the Lanthanide‐Binding Tag Grafted at Calmodulin Site 1: Affinity, Selectivity, and Coordination Properties

European Journal of Inorganic Chemistry, Volume 29, Issue 3, January 21, 2026.
Lanthanide affinity and selectivity in proteins remain poorly understood. Engineering calmodulin with a lanthanide‐binding tag at Site 1 boosts affinity from nanomolar (isolated LBTs) to picomolar dissociation constants, comparable to lanmodulin but with distinct selectivity.
Catherine Berthomieu, Manon Martin, Jean Aupiais, Tiffanie Barré, Loïc Daronnat, Jérémy Pansier, Nicolas Brémond, David Lemaire, Atul Thawari, Martin Levier, Laurence Berthon, Sandrine Sauge‐Merle   +11 more
wiley   +1 more source

The in vivo proconvulsant effects of corticotropin releasing hormone in the developing rat are independent of ionotropic glutamate receptor activation. [PDF]

, 1998
Corticotropin releasing hormone (CRH) produces age-dependent limbic seizures in the infant rat. Both the phenotype and the neuroanatomic matrix of CRH-induced seizures resemble the seizures induced by the rigid glutamate analogue, kainic acid (KA), and ...
Baram, TZ, Brunson, KL, Schultz, L
core   +1 more source

Optically pure, structural and fluorescent analogues of a dimeric Y4 receptor agonist derived by an olefin metathesis approach [PDF]

, 2016
The dimeric peptide 1 (BVD-74D, as a diastereomeric mixture) is a potent and selective Neuropeptide Y Y4 receptor agonist. It represents a valuable candidate in developing traceable ligands for pharmacological studies of Y4 receptors, and as a lead ...
Briddon S., Gehlert D. R., Marleen Groenen, Mengjie Liu, Michel M. C., Nicholas D. Holliday, Philip E. Thompson, Rachel R. Richardson, Schober D. A., Simon J. Mountford, Uhe A. M.   +10 more
core   +2 more sources

Should NS5A inhibitors serve as the scaffold for all-oral anti-HCV combination therapies?

Hepatic Medicine: Evidence and Research, 2015
Sujit V Janardhan, Nancy S Reau Center for Liver Diseases, Section of Gastroenterology, Hepatology, and Nutrition, Department of Medicine, University of Chicago, Chicago, IL, USA Abstract: Chronic hepatitis C virus (HCV) infection represents a global ...
Janardhan SV, Reau NS
doaj  

The primary mechanism for highly potent inhibition of HIV-1 maturation by lenacapavir.

PLoS Pathogens
Lenacapavir (LEN) is a highly potent, long-acting antiretroviral medication for treating people infected with muti-drug-resistant HIV-1 phenotypes. The inhibitor targets multifaceted functions of the viral capsid protein (CA) during HIV-1 replication ...
Szu-Wei Huang, Lorenzo Briganti, Arun S Annamalai, Juliet Greenwood, Nikoloz Shkriabai, Reed Haney, Michael L Armstrong, Michael F Wempe, Satya Prakash Singh, Ashwanth C Francis, Alan N Engelman, Mamuka Kvaratskhelia   +11 more
doaj   +1 more source

Long‐Circulating Nanobody Confers Durable Prophylaxis against Severe Acute Respiratory Syndrome Coronavirus 2 Omicron Infection

Advanced NanoBiomed Research
Breakthrough infections in vaccinated population and continuous emergence of severe acute respiratory syndrome coronavirus 2 (SARS‐CoV‐2) variants make it imperative to develop more efficacious medical countermeasures.
Geetha Jyothi Vaskuri, Gang Ye, Fan Bu, Dong Yang, Colleen B. Jonsson, Hailey Turner‐Hubbard, Sydney Winecke, Alise Mendoza, Fang Li, Chalet Tan   +9 more
doaj   +1 more source

Discovery of potent KRASG12D inhibitors disrupting RAS-Raf interaction to block activation

Results in Chemistry
The proteins encoded by the KRAS gene belong to the RAS family, with activating KRAS mutations strongly implicated in oncogenesis. The hard-to-target nature of KRAS proteins stems from their unique structural biology: a highly conserved spherical surface
Zhaoyang Li, Junru Liu, Yingying Yan, Xiujuan Shi, Benlong Cao, Yue Wang, Fuxun Huang, Jingtong Feng, Qingqiang Yao, Bo Liu, Xinmei Yang   +10 more
doaj   +1 more source

An Antiherpesviral Host-Directed Strategy Based on CDK7 Covalently Binding Drugs: Target-Selective, Picomolar-Dose, Cross-Virus Reactivity

Pharmaceutics
The repertoire of currently available antiviral drugs spans therapeutic applications against a number of important human pathogens distributed worldwide. These include cases of the pandemic severe acute respiratory coronavirus type 2 (SARS-CoV-2 or COVID-
DongHoon Yu, Sabrina Wagner, Martin Schütz, Yeejin Jeon, Mooyoung Seo, Jaeseung Kim, Nadine Brückner, Jintawee Kicuntod, Julia Tillmanns, Christina Wangen, Friedrich Hahn, Benedikt B. Kaufer, Frank Neipel, Jan Eickhoff, Bert Klebl, Kiyean Nam, Manfred Marschall   +16 more
doaj   +1 more source