Results 121 to 130 of about 131,409 (188)

Natural Products Inspired Scaffold Diversification Leads to Unnatural Molecular Warhead and Covalent Strategy to Modulating Protein Function through Electrophilic Bromine Transfer

Advanced Science, EarlyView.
We report a new thiolate‐reactive α,α‐gem‐dibromo lactam warhead that activates transcription factor Nrf2 and demonstrates anti‐inflammatory activities, which have implications in cancer, neurodegeneration, and cardiovascular diseases. RNA‐seq illuminated detailed transcriptional profiles, and chemical reactions with cysteine‐containing compounds ...
Beau R. Brummel, Sofia Kokkaliari, Qiwen Gao, Jinjing Chen, Larissa Costa de Almeida, Srinivasarao Tenneti, Derek A. Leas, Eli Levit, Lewis S. Alexander, Khalil A. Abboud, Pingrong Wei, Michael D. Cameron, James R. Rocca, Ranjala Ratnayake, Donna D. Zhang, Hendrik Luesch, Robert W. Huigens III   +16 more
wiley   +1 more source

In Memory of Dr. Klaus Miczek, a prolific scientist, generous scholar, and cherished colleague. [PDF]

Psychopharmacology (Berl)
Maguire J, Weera M.
europepmc   +1 more source

Unraveling the Molecular Mechanisms Underlying Spontaneous Multipolar Mitosis Through CIN‐seq

Advanced Science, EarlyView.
Multipolar mitosis, a hallmark of chromosomal instability (CIN), drives tumor heterogeneity but is challenging to study in live cells. Using CIN‐seq, a single‐cell multiomics method, we profiled rare CIN events and identified mechanisms associated with viable multipolar mitosis, including PTEN attenuation, Rho GTPase‐driven cytokinesis failure, and ...
Pin‐Rui Su, Ting‐Chun Chou, Maria Teresa López‐Cascales, Junfeng Huang, Tsai‐Ying Chen, Sjoukje van Wieren, Chan Li, Cecile Beerens, Li You, Jelle Storteboom, Miao‐Ping Chien   +10 more
wiley   +1 more source

TB and HIV Therapeutics: Pharmacology Research Priorities. [PDF]

AIDS Res Treat, 2012
Dooley KE, Kim PS, Williams SD, Hafner R.   +3 more
europepmc   +1 more source

Genome‐Wide CRISPR Screen Identifies a microRNA Orchestrating Pleiotropic Resistance to Targeted Therapy and T Cell Immunity in Melanoma

Advanced Science, EarlyView.
A genome‐wide microRNA CRISPR screen identifies miR‐18a as a master regulator of cross‐resistance in melanoma. Loss of miR‐18a activates the AJUBA–YAP/Hippo axis to confer BRAFi resistance and enhances THBS1–CD47 interaction to impair CD8+ T cell immunity. hnRNP A1 is identified as an upstream regulator of miR‐18a processing.
Zhao Wang, Haotian Liu, Xueqi Wang, Jianjin Teng, Zihan Zheng, Jingya Zhang, Wanyi Xiao, Qian Liang, Jiaxin Li, Xiaomeng Jia, Xin Feng, Hongzhang Cui, Menghan Luo, Tielong Yang, Liuxing Wu, Ke Zhao, Weilong Yang, Mulin Jun Li, Dandan Huang, Jilong Yang   +19 more
wiley   +1 more source

The Gut Microbiome Dependency Continuum in Drug Discovery: A Unified Pharmacology Framework Linking Clinical Drugs, Natural Products, and Engineered Microbial Therapeutics. [PDF]

BioTech (Basel)
Habtemariam S.
europepmc   +1 more source

Adipocyte‐Derived Leptolin Enhances Energy Expenditure and Prevents Obesity

Advanced Science, EarlyView.
We identified a novel adipokine, which we named leptolin. In humans, leptolin levels in white adipose tissue were positively correlated with exercise and negatively associated with body mass index. We observed elevated leptolin in serum from athletes and lower leptolin in serum from obese individuals.
Jiarui Liu, Bingwei Wang, Zhijie Su, Xiaoxv Han, Miao He, Yun Zhao, Yujia Hou, Daotong Li, Weiguang Zhang, Lihua Qin, Ke Wang, Yanchun Li, Yi Yan, Siwang Yu, Xiaoshuai Huang, Tairan Yuwen, Jianyuan Luo, Ruimao Zheng   +17 more
wiley   +1 more source

Atypical respiration patterns of kratom alkaloids. [PDF]

J Pharmacol Exp Ther
Wells E, Paul B, Ramos-Gonzalez N, Majumdar S.   +3 more
europepmc   +1 more source

Agnuside Stabilizes the Complex I Assembly Factor NDUFAF6 to Reinforce Mitochondrial Efficiency and Thermogenic Responsiveness

Advanced Science, EarlyView.
ABSTRACT Brown and beige adipocytes dissipate energy as heat, yet effective strategies to enhance their mitochondrial efficiency remain limited. Here, we identify Agnuside (AGN) as a selective stabilizer of the complex I assembly factor NDUFAF6. AGN directly binds cytosolic NDUFAF6, suppresses its ubiquitination, prolongs its half‐life, and facilitates
Qingwen Zhao, Li Xie, Qianzhuo Wang, Shuying Dai, Bei Li, Yingjuan Zhang, Zhe Sun, Yue Gao   +7 more
wiley   +1 more source

Reimagining pharmacology education. [PDF]

Pharmacol Rev
Guilding C, Kelly-Laubscher R, Cunningham M, Dilles T, Kennedy D, Brinkman DJ, Eid AH, Quesnelle KM, Engels F, Maxwell S, Christopoulos A, White PJ.   +11 more
europepmc   +1 more source