Results 31 to 40 of about 423,855 (249)

Rationale-Based Engineering of a Potent Long-Acting FGF21 Analog for the Treatment of Type 2 Diabetes. [PDF]

PLoS ONE, 2012
Fibroblast growth factor 21 (FGF21) is a promising drug candidate for the treatment of type 2 diabetes. However, the use of wild type native FGF21 is challenging due to several limitations.
Randy Hecht, Yue-Sheng Li, Jeonghoon Sun, Ed Belouski, Michael Hall, Todd Hager, Junming Yie, Wei Wang, Dwight Winters, Stephen Smith, Chris Spahr, Lei-Ting Tam, Zhongnan Shen, Shanaka Stanislaus, Narumol Chinookoswong, Yvonne Lau, Allen Sickmier, Mark Leo Michaels, Thomas Boone, Murielle M Véniant, Jing Xu   +20 more
doaj   +1 more source

Engineered Human Heavy-Chain Ferritin with Half-Life Extension and Tumor Targeting by PAS and RGDK Peptide Functionalization

Pharmaceutics, 2021
Ferritin, one of the most investigated protein nanocages, is considered as a promising drug carrier because of its advantageous stability and safety.
Shuang Yin, Yan Wang, Bingyang Zhang, Yiran Qu, Yongdong Liu, Sheng Dai, Yao Zhang, Yingli Wang, Jingxiu Bi   +8 more
doaj   +1 more source

Modulation of Homer1 EVH1 domain internal dynamics by putative autism‐associated mutations

FEBS Letters, EarlyView.
The putative autism‐associated M65I and S97L variants of the EVH1 domain of the postsynaptic scaffold protein Homer1 do not exhibit substantial changes in their overall structure or partner binding. Both of them, but especially the M65I variant, show altered internal dynamics relative to the wild‐type domain on the μs‐ms timescale, indicated by the ...
Fanni Farkas, Brigitta Maruzs, Zsófia E. Kálmán, Tomas Klumpler, Gyula Batta, Bálint Péterfia, Zoltán Gáspári   +6 more
wiley   +1 more source

Studies on some properties and the half-life of lactate dehydrogenase-linked immunoglobulin complexes forming experimently in vitro.

SEIBUTSU BUTSURI KAGAKU, 1993
臨床上しばしば見られる酵素結合免疫グロブリンのモデル実験としてヒト精製乳酸脱水酵素 (LD) A4およびB4とそれらの抗ヒトLDモノクローナル抗体 (MoAb) 複合体を作製し, これらの若干の特性を調べた. その結果, LD-LD MoAb 複合体の特性は臨床上発見される E-Ig複合体の抗体の性質と類似し, その電気泳動上での移動度もよく一致していた. 本研究では特にLD結合免疫グロブリン複合体形成に関与すると思われる各 MoAbの糖鎖部分について注目し, 各 MoAb を各種グリコシダーゼで処理し, ヒト精製125IラベルLDアイソザイムと結合させた. こうして実験的に作製したLD-LD MoAb 複合体を家兎腹腔中へ注射した.
Miura, Masakazu, Sakai, Hiroshi, Sakagishi, Yoshikatsu, Komoda, Tsugikazu   +3 more
openaire   +2 more sources

From mice to humans—divergent strategies for intestinal homeostasis and regeneration

FEBS Letters, EarlyView.
Recent advances such as organoid genome editing, xenotransplantation, imaging, and whole‐genome sequencing have enabled direct studies of human intestinal stem cells (ISCs). These studies reveal species‐specific features, including slower ISC proliferation, distinct injury responses, slower somatic mutation accumulation in humans, and an inverse ...
Keiko Ishikawa, Shinya Sugimoto, Toshiro Sato   +2 more
wiley   +1 more source

Effects of a recombinant humanized anti‐cocaine monoclonal antibody on the metabolism and distribution of cocaine in vitro and in mice

Pharmacology Research & Perspectives, 2022
The anti‐cocaine monoclonal antibody, h2E2, is a candidate for treating cocaine‐use disorder. h2E2 binds to and sequesters cocaine in the plasma compartment, effectively decreasing cocaine concentrations in the brains of rats and mice.
Mackenzie E. Turner, Hanna N. Wetzel, Dakota B. Zinani, Christopher A. Crutchfield, Andrew B. Norman   +4 more
doaj   +1 more source

A Peptide-Based HIV-1 Fusion Inhibitor with Two Tail-Anchors and Palmitic Acid Exhibits Substantially Improved In Vitro and Ex Vivo Anti-HIV-1 Activity and Prolonged In Vivo Half-Life [PDF]

Molecules, 2019
Enfuvirtide (T20) is the first U.S. FDA-approved HIV fusion inhibitor-based anti-HIV drug. Its clinical application is limited because of its low potency and short half-life. We previously reported that peptide HP23-E6-IDL, containing both N- and C-terminal anchor-tails, exhibited stronger potency and a better resistance profile than T20.
Shan Su, Giselle Rasquinha, Lanying Du, Qian Wang, Wei Xu, Weihua Li, Lu Lu, Shibo Jiang   +7 more
openaire   +3 more sources

Investigating transcription factor dynamics in health and disease using FRAP

FEBS Letters, EarlyView.
FRAP analysis of GFP‐tagged transcription factors reveals how molecular mobility and target engagement change in response to drug treatment. By combining live‐cell imaging, quantitative model fitting, and statistical analysis, this approach uncovers transcription factor dynamics linked to disease mechanisms, providing a powerful framework for ...
Kannan Govindaraj, Carolina Vazquez Garzon, Jose Joaquin Velasco, Janine N. Post   +3 more
wiley   +1 more source

Development of [18F]-PSS223 as a PET Tracer for Imaging of Metabotropic Glutamate Receptor Subtype 5 (mGluR5)

CHIMIA, 2012
Involvement of metabotropic glutamate receptor subtype 5 (mGluR5) in physiological and pathophysiological processes in the brain has been demonstrated, and hence mGluR5 has emerged as an important drug target. [11C]-ABP688 is clinically the most
Selena Milicevic Sephton, Patrick Dennler, Dominique S. Leutwiler, Linjing Mu, Roger Schibli, Stefanie D. Krämer, Simon M. Ametamey   +6 more
doaj   +1 more source

PEGylation Extends Circulation Half-Life While Preserving In Vitro and In Vivo Activity of Tissue Inhibitor of Metalloproteinases-1 (TIMP-1)

PLoS ONE, 2012
Excess proteolytic activity of matrix metalloproteinases (MMPs) contributes to the development of arthritis, cardiovascular diseases and cancer progression, implicating these enzymes as therapeutic targets. While many small molecule inhibitors of MMPs have been developed, clinical uses have been limited, in part by toxicity and off-target effects ...
Jyotica Batra, Jessica Robinson, Christine Mehner, Alexandra Hockla, Erin Miller, Derek C Radisky, Evette S Radisky   +6 more
openaire   +4 more sources