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"This timely guide to kinase inhibitor drug development is the first to cover the entire drug pipeline, from target identification to compound development and clinical application. Edited by the pioneers in the field, on the drug development side this ready reference discusses classical medicinal chemistry approaches as well as current chemical genomics strategies. On the clinical side, both current and future therapeutic application areas for kinase inhibitor drugs are addressed, with a strong focus on oncology drugs.Backed by recent clinical experience with first-generation drugs in the battle against various forms of cancer, this is crucial reading for medicinal, pharmaceutical and biochemists, molecular biologists, and oncologists, as well as those working in the pharmaceutical industry."

"With its particular emphasis on the constitutive activity of G-protein-coupled receptors (GPCRs)s, this book comprehensively discusses an important biological process that has not yet been covered in such depth in any other existing books on GPCRs. The international team of highly distinguished authors addresses in detail current models and concepts, to introduce medicinal chemists, physiologists, pharmacologists, and medical researchers into the advances in the understanding of GPCR activation and constitutive activity. In addition, the book provides an overview on methods of investigating constitutive GPCR activity. The text is well illustrated by selected experimental data and schemes.The chapters are all cross-referenced with each other and cover general mechanisms, methodological approaches and cover selected important GPCR systems, the consequences for drug action, including, side effects, and rational drug design for GPCR targets. The text is backed by abundant case studies and methodological advice for analysing GPCRs, covering selected pharmacologically relevant GPCR systems, the consequences for drug action, including unwanted side effects, and rational drug design for GPCR targets. It is a highly practical reference for researchers in academia and industry."

"Opening with a general introduction on chemokine function and chemokine receptor biology, the handbook goes on to cover the known implications of these signaling molecules in human diseases, such as cancer, neural disorders, and viral infection, including HIV/AIDS. The second half of the book systematically surveys current drug development efforts at targeting individual chemokine receptors, as well as other chemokine interaction partners. Contributions in the first part of the book are mainly from academia, whereas the second part contains up-to-date reports from the pharmaceutical industry."

"This book provides an overview of different protein kinases, structure, function, regulation, and their role in cancer. It combines kinase biology with chemistry and pharmacology applications for discovery and development of cancer drugs. The text also describes existing and emerging kinase inhibitors, focusing mostly on small molecules but also alternative approaches like therapeutic antibodies. Provides an important resource that helps pharmaceutical researchers understand and work in this dynamic area of cancer drug research."

"Epidemi tuberkulosis masih menjadi beban Indonesia saat ini dimana tercatat sebanyak 845 ribu jiwa di Indonesia mengidap penyakit tuberkulosis dengan persentase terbanyak terdapat pada kelompok usia produktif, yaitu umur 15 – 64 tahun sebanyak 89,6%. Tuberkulosis adalah penyakit menular yang diakibatkan oleh infeksi Mycobacterium tuberculosis. Kemunculan Multi-drug Resistant Tuberculosis (MDR-TB) mendorong adanya pemanfaatan flavonoid sebagai sediaan Obat Anti Tuberkulosis (OAT). Flavonoid memiliki kemampuan untuk mengembalikan resistensi antibiotik dan meningkatkan performa OAT saat ini. Perkembangan dalam penemuan obat saat ini dilakukan dengan melakukan studi in silico melalui penambatan molekuler antara beberapa senyawa golongan flavonoid dengan protein pada Mycobacterium tuberculosis. Penelitian ini menunjukkan bahwa kuersetin menghasilkan nilai penambatan dan konstanta inhibisi terbaik dengan nilai penambatan pada protein β-ketoacyl-ACP reductase (PDB ID:1UZN), Enoyl-Acyl Carrier Protein Reductase (PDB ID:2X23), dan Protein Kinase G (PDB ID:2PZI) masing-masing sebesar -8,0 kkal/mol; -9,2 kkal/mol; dan -8,0 kkal/mol serta konstanta inhibisi masing-masing sebesar 1,345 µM; 0,177 µM; dan 1,345 µM. Kuersetin dari daun keji beling (Strobilanthes crispus L.) selanjutnya diperoleh menggunakan metode Ultrasound Enzymatic-Assisted Aqueous Two-Phase Extraction (UEAATPE) dengan sistem etanol/amonium sulfat. Adapun rancangan sistem Aqueous Two-Phase terbaik yaitu etanol 33% (w/w) dan amonium sulfat 14% (w/w) dengan konsentrasi kuersetin yang dihasilkan sebesar 44,717±0,295 mg/L. Selain kuersetin, senyawa 1,14-tetradecanediol yang teridentifikasi oleh Gas Chromatography-Mass Spectophotometer (GC-MS) juga memiliki aktivitas anti tuberkulosis

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Tuberculosis epidemic is still a burden for Indonesia. There are 845 thousand of Indonesian people suffer from tuberculosis with the highest percentage in the productive age which 15 - 64 years by 89.6%. Tuberculosis is an infectious disease that caused by Mycobacterium tuberculosis infection. The emergence of Multi-Drug Resistant Tuberculosis (MDR-TB) encourages the utilization of flavonoids as anti-tuberculosis drugs. Flavonoids have the ability to recover antibiotic resistance and improve current anti-tuberculosis drugs performance. Development of drug discovery is currently being carried out by in silico study through molecular docking between flavonoid compounds to protein targets in Mycobacterium tuberculosis. This study shows that quercetin produces the best docking score and inhibition constant with the docking score of β-ketoacyl-ACP reductase (PDB ID: 1UZN), Enoyl-Acyl Carrier Protein Reductase (PDB ID : 2X23), and Protein Kinase G (PDB ID: 2PZI) respectively are -8.0 kcal/mol; -9.2 kcal/mol; and -8.0 kcal/mol and the inhibition constants respectively are 1,345 µM; 0,177 µM; and 1,345 µM. Quercetin from Strobilanthes crispus L. is obtained using Ultrasound Enzymatic – Assisted Aqueous Two-Phase Extraction (UEAATPE) method with ethanol/ammonium sulfate system. The best proportion of the system is ethanol 33 wt% and ammonium sulfate 14 wt% with concentration of quercetin is 44.717±0,295 mg/L. Besides quercetin, 1,14-tetradecanediol compound identified by Gas Chromatography – Mass Spectophotometer (GC-MS) is also has an anti-tuberculosis."

"Fueled by the expertise of a team of international specialist authors, this first reference on the booming topic covers everything a drug researcher needs to know about targeting epigenetic mechanisms of disease. The first part of the book surveys current methodologies for finding and validating drug candidates that act via epigenetic mechanisms. The second part systematically surveys known and suspected drug targets within the epigenetic machinery, including the discovery and development of vorinostat, the first marketed epigenetic drug."

"The book covers a broad spectrum of topics, ranging from pioneering research in the field of classical steroid hormones to very recently discovered orphan receptors and their modulators. State of the art technologies are also discussed in the individual chapters that help to develop a deeper insight into the biochemical and pharmacological principles underlying the biological function of nuclear receptors.Edited by two experts working at the pioneering pharmaceutical company and major global player in hormone-derived drugs, this handbook and reference systematically treats the drug development aspects of all human nuclear receptors, including recently characterized receptors such as PPAR, FXR and LXR. Authors from leading pharmaceutical companies around the world present examples and real-life data from their own work."